Type Of Agonist Essay

Type Of Agonist Essay
Types of agonists
Receptors can be activated by either endogenous (such as hormones and neurotransmitters) or
exogenous (such as drugs) agonists, resulting in a biological response. A physiological agonist is a
substance that creates the same bodily responses but does not bind to the same receptor.
An endogenous agonist for a particular receptor is a compound naturally produced by the body that
binds to and activates that receptor. For example, the endogenous agonist for serotonin receptors is
serotonin, and the endogenous agonist for dopamine receptors is dopamine.[1]
A superagonist is a compound that is capable of producing a greater maximal response than the
endogenous agonist for the target receptor, and thus has an efficacy of more than 100%. This does
not necessarily mean ... Show more content on Helpwriting.net ...
Inverse agonists exert the opposite pharmacological effect of a receptor agonist, not merely an
absence of the agonist effect as seen with antagonist. An example is the cannabinoid inverse agonist
rimonabant.
A co–agonist works with other co–agonists to produce the desired effect together. NMDA receptor
activation requires the binding of both glutamate, glycine and D–serine co–agonists.
An irreversible agonist is a type of agonist that binds permanently to a receptor through the
formation of covalent bonds. A few of these have been described.[2][3]
A selective agonist is selective for a specific type of receptor. E.g. buspirone is a selective agonist
for serotonin 5–HT1A.
New findings that broaden the conventional definition of pharmacology demonstrate that ligands
can concurrently behave as agonist and antagonists at the same receptor, depending on effector
pathways or tissue type. Terms that describe this phenomenon are "functional selectivity", "protean
agonism",[4][5] or selective receptor modulators.[6]
Activity
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Opioid Agonists
Effects of opioids on the gastrointestinal tract
Dona Pham1, Annie Hua1 and Cindy Kaing1
1 BP311 B, School of Medical Sciences, RMIT University.
Background and Aims: Opioid agonists, such as morphine and codeine, causes a reduction in
acetylcholine (ACh) release from presynaptic ganglionic nerves. It is reported that tolerance
develops following prolonged exposure to these drugs. The aim was to compare two opiate agonists
and investigate the effects of opioid antagonist (naloxone) on morphine. This study also examines
whether or not prolonged exposure to morphine results in the development of tolerance.
Methods: A guinea pig ileum was suspended in an organ bath and superfused with oxygenated,
physiological salt solution. The twitch height changes were recorded using LabChart. Cumulative
concentration response curves (CRC) were constructed for codeine and morphine using bath
concentrations between 10–6 M to 10–4 M and between 10–8 M to 10–5 M, respectively. Naloxone
(10–7 M) was added before the experiment and after the first morphine CRC. Tissue desensitisation
was performed for morphine (5x10–6 M) while the effects of naloxone (10–7 M) on morphine were
observed. ... Show more content on Helpwriting.net ...
The twitch responses for codeine (–21.16% at 10–5 M) were lower than those in morphine (–
89.08% at 10–5 M). The electrically–induced ACh release decreased in both opioid agonists, thus
decreases twitch responses. Following tissue desensitisation with morphine, the twitch responses
decreased with increasing concentrations, from 18.66% at 10–8 M to –8.33% M at 10–5 M. The
change in twitch height of naloxone decreased from the beginning of the experiment (–5.16%) to the
end of the morphine CRC (–4.25%). In the presence of naloxone, however, there is no twitch height
change detected as morphine concentration

Safe Use of Long Acting Beta Agonist in Asthma Patients
Executive summary
There have been concerns among the safety of long acting Beta agonist referred to as LABA
therapy. This is after the long acting inhaled beta has been used in the treating of asthma since the
year 1990. In order to get information about the effect of long acting beta agonists, information was
extracted from authoritative journals that were written after the FDA's recommendation. These
journals were written in order to address the concerns that came after Asthma patients who had used
long term beta agonists when it came to the treatment of asthma (Lötvall, 2012: 32). This paper will
argue about the safe use of long acting beta agonist in asthma patients and the recommendations of
its use.
Research methodology
The material for this research was gotten from various journals such as US National library of
medicine as well as other databases such as Medical research journal. The information from these
journals is credible as the journals are peer reviewed and scholarly. Since the introduction of the
extensive acting beta agonists, there has been an improvement for many people that live with asthma
(Lötvall, 2012 39). The benefit to these people has been dramatic and consequently there have been
fewer asthma symptoms when it comes to rest with exercises, there are fewer night time awakenings
and less asthma burn ups. Source of concern
The source of concern when it comes to long acting beta agonists is the fact that it sometimes causes
severe asthma

Muscle Analysis: The Deltoid Muscles
The Deltoid Muscle
The deltoid muscle is in the shoulder area, towards the proximal end of the arm. The muscle itself is
rounded and triangular in shape, and consists of three main "heads" or muscles fibre strands; the
lateral, anterior, and posterior deltoids. It is used for arm extension in all angles and rotation, mainly
up and down straight out to the side.
The deltoid has three main functions that involve the three individual muscle "strands". The the
anterior deltoid rotates the humerus anteriorly, such as when you reach forward or throw a ball
underarm. The lateral deltoid rotates the arm directly out sideways using abduction. The posterior
deltoid extends the arm backwards and laterally rotates the arm by pulling the humerus toward ...
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Lift up to your chin keeping the barbell close to your body and keeping your back straight. Then
lower the bar back down slowly to the starting position.
The Agonist in this exercise is the Medial or Lateral Deltoid while lifting the bar up and the
antagonist is the Latissimus Dorsi and the Pectoralis Major. While lowering the bar the agonists and
antagonist swap around. The synergists are the Supraspinatus, Infraspinatus, Teres major and minor,
Subscapularis. The deltoid muscle contraction is Concentric upwards and eccentric downwards and
the types of movements are Shoulder Abduction and Adduction.
Shoulder Presses– Anterior Deltoid Exercise: Hold a dumbbell in each hand, sitting on a chair on
bench with back support. Lift the dumbbells to about shoulder height before propelling the
dumbbells upwards until reaching full contraction. Hold there briefly before slowly lowering them
back to shoulder

Opioid Agonist Therapy
Opiods are the group of drugs which act on the opioid receptor and cause relief from the pain. This
group consists of both prescription opioids used for moderate to severe pain relief and illicit drug
like heroin. According to CDC, from 2000 to 2015 more than half a million people died from opioid
overdose (CDC, 2017). According to National Institute on Drug Abuse, total economic burden of
prescription opioid overdose, abuse and dependence in the U.S tends to be around $78.5 billion
(Florence et al., 2016). Risk factor for opioid addiction tends to be substance abuse and high
prescribed dosage for a longer period of time. The use of opioid is seen common in both genders,
between 22–55 years, non–Hispanic whites, living in poor neighborhood and in rural areas (Rudd et
al., 2016; Hasegawa,Espinola, et al.,2014; Macarena C. Garcia,2017). Also it is common in patients
with HIV because they are prone to various opportunistic infections which tend to be very painful.
Thus, the study to understand the effect of opioids on patients with HIV is very important. ... Show
more content on Helpwriting.net ...
Moreover, various kinds of treatment process for opioid addiction are being developed; Opioid
agonist therapy tends to be one of the effective treatment procedures where opioid agonists like
methadone and buprenorphine are

Anterior Muscles: A Case Study
Briefly identify, list, and describe the action of at least two of the following muscle types:
Posterior muscles
The anconeus muscle is a small muscle on the posterior aspect of the elbow joint.
It facilitates in extension of the elbow. The triceps brachii is the main agonist supporting the elbow
into a full extension. The supinator is a broad muscle in the posterior compartment of the forearm
curved around the upper third portion of the radius. Its primary function is to supinate the forearm
(MJC, 2016).
Anterior Muscles
The pronator teres is a muscle located in the forearm. It functions to pronate the forearm. This action
is described as turning of the palm faces posteriorly when from the anatomical position. The flexor
digitorum profund ... Show more content on Helpwriting.net ...
The antagonist is the posterior deltoid, latissimus dorsi, and triceps brachii. When the shoulder
performs extension the agonist (prime mover) is posterior deltoid and latissimus dorsi. The
antagonist is anterior deltoid and pectoralis major. During shoulder adduction the agonist muscle is
the latissimus dorsi and pectoralis major; the antagonist muscle is the deltoid (middle). When
shoulder abduction is performed the agonist muscle is the deltoid (middle) and the antagonist
muscle is the latissimus dorsi and pectoralis major (FCG, 2016). In wrist flexion the agonist muscle
is flexor digitorum and the antagonist is extensor digitorum. When performing wrist extension the
agonist muscle is the extensor digitorum and the antagonist is flexor digitorum. In elbow flexion the
agonist muscle is the biceps brachii and the antagonist muscle is triceps brachii. During elbow
extension the agonist muscle is the triceps brachii and the antagonist muscle is biceps brachii. In
trunk flexion the agonist muscle is the rectus abdominis and the antagonist muscle is erector spinae.
When performing trunk extension the agonist muscle is the erector spinae and the antagonist muscle
is rectus abdominis (BBC, 2016). During hip flexion the agonist muscle is the illiopsoas/quadriceps
and the antagonist muscle are gluteus maximus/hamstrings. When performing hip extension the
agonist muscle is the glueteus maximus/hamstrings and the antagonist are lliopsoas/quadriceps.
During knee flexion the agonist muscle is the hamstring and the antagonist are quadriceps. When
performing knee extension the agonist muscle are the quadriceps and the antagonist are the
hamstrings. During dorsiflexion the agonist muscle are the tibialis anterior and the antagonist are
gastrocnemius/soleus. When plantar flexion is performed the agonist muscle is the
gastrocnemius/soleus and the antagonist are

The Relationship Between Grks And Arrestins
2.3.2 GRKs and –arrestins
GPCR desensitization is a deactivation of GPCR–elicited signaling following prolonged or repeated
agonist exposure. A major mechanism underlying desensitization is agonist–stimulated
phosphorylation and endocytosis of the receptor. The second messenger–dependent protein kinases
were originally regarded as the principal mediators of GPCR phosphorylation and desensitization.
However, following the discovery of G protein–coupled receptor kinases (GRKs, originally called
–adrenoceptor kinases), the GRKs have been shown to play a central role in the agonist–induced
desensitization of many GPCRs (Kelly 2008). The GRK family of serine/threonine kinases
comprises seven members. Based on sequence homology, vertebrate ... Show more content on
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For example, –arrestins can mediate sustained ERK phosphorylation or protective mGluR
signaling, which are G protein–independent processes (Emery 2010, Wang 2016). At the end of
GPCR cycles, a regulator of G protein signaling (RGS) acts as GTPase activating proteins (GAPs),
leading to GTP hydrolysis and reversing the receptor to an initial resting state (Sato 2015).
Different GRK subtypes combined with the action of –arrestins can contribute the endocytosis of
Group I mGluRs in an agonist–dependent manner; however, the results are inconsistent (reviewed in
Refs: Iacovelli 2013, Kim 2008). Both GRK2 and GRK4 induce the agonist–induced internalization
of mGluR1a, which appears to require GRK2–mediated phosphorylation of the S869–V893 region
of mGluR1a when expressed in HEK cells (Iacovelli 2003, Sallese 2000, Mundell 2003). These
agonist–induced internalization processes are –arrestin 1/2 and dynamin–dependent (Mundell
2001, 2002, 2003). –arrestin 1 appears to be important in mGluR1 endocytosis; however, the
agonist–stimulated internalization of mGluR1a is observed only when –arrestin 1 is co–expressed
with either GRK2 or GRK5 in HEK cells. GRK2, GRK5, –arrestin 1, or –arrestin2 individually
has no significant effect on the internalization of mGluR1a (Dale 2001). –arrestin 1, but not –
arrestin 2, selectively interacts with mGluR1a and is redistributed to the same

Comparing Inequality In Eve And Samson Agonist By...
Inequality is a struggle that women have felt since the beginning of time, and an issue that still
plagues women today. Women are consistently reduced to their looks or the tasks they are able to
complete, and often their intellect and talents are ignored. Milton grapples the topic in both of his
works, Paradise Lost with Adam and Eve, and Samson Agonists with Samson and Dalila. Both Eve
and Dalila are presented as unequal characters when compared to Adam and Samson, making them
both more susceptible to the advances of evil forces. Each woman individually faces temptation and
fails to supersede it, causing not only the fall for themselves, but the fall for their husbands as well.
For Eve, her fall fates not only Adam but the entire humanity ... Show more content on
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If Milton situated the woman as equal to their husbands and as helpmates instead of companions
then the likelihood of them falling would have decreased greatly. However, because of their
inequality it opened sin up to being a viable temptation. Milton had to present them as unequal
beings to be able to justify their fall and in return ultimately place the blame on God as a whole.
Milton's central theme seems to suggest that if God would have just created men and women equal
to begin with then they would not have fallen. This is easily seen in Paradise Lost, but when
examining Samson Agonists, it is evident there as well, since Dalila is part of the Philistinians, a
race that God sent Samson to destroy, making them unequal. Therefore, it can be assumed that
Milton presents Eve and Dalila the way he does in order to justify the fall and attempt to make sense
of why humanity had to fall even though it was created by an omnipotent

Symptoms And Diagnosis Of Schizophrenia
Schizophrenia is one of the most severe psychiatric disorders that affects both male and females,
respectively. This illness is characterized by gradual increase in changes of perception, thinking,
social activities, speech, feelings, and motivations. Many studies have shown that there is a clear
difference in outcome between genders including symptom severity, age–at–onset and functional
outcome (as cited in Gogos, Kwek and van den Buuse, 2011, p. 213). For example, schizophrenia
occurs on average 1.5–4.5 earlier in men compared to women. Further evidence suggests that
women who have a psychiatric disorder such as schizophrenia may have various levels of estrogen;
the most severe phase of the disorder will be when there is low level of ... Show more content on
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PPI is an indicator sensomotoric reflecting the ability of the central nervous system to filter sensory
information and is one of the best established translational paradigms that allows measuring
sensorimotor gating in both humans and rodents (Labouesse, Langhans and Meyer, 2015).
There have been many studies conducted on learning the causes of schizophrenia and its treatments.
Unfortunately, the treatments for complete recovery from this disorder still remain unsolved. Some
studies focused on a general context in terms of a role of sex hormones in schizophrenia, other
studies focused on a specific state such as cognition and role of hormones in schizophrenia. The aim
of this paper is to further analyze of the role of sex steroid hormones in schizophrenia in animal
models and human studies, compare different methodologies and possible treatments. Dopamine,
which plays a significant role in schizophrenia, regulates sensorimotor filtration information in
rodents and in humans as well. These findings fit the description of dopamine hypothetical
mechanisms of disease, possibly being associated with the processes of fragmentation and sensory
cognitive overload that may be involved in the pathology of schizophrenia (Gogos, Kwek and van
den Buuse, 2011). There are many research studies that focus on the effects of estrogen and
testosterone administration in schizophrenia. For

Agonists Essay
Agonists are drugs with affinity for a receptor that cause a specific response. (Colbert, 2016, pg26)
Beta2 adrenergic receptor agonists are a class of medications that cause muscle unwinding. It causes
smooth muscle widening of bronchial entries, vasodilatation in muscle and liver, unwinding of
uterine muscle and release of insulin. Inhaled salmeterol and formoterol, known as long‐acting
beta2‐agonists (LABAs), are widely used to manage the symptoms of COPD, so it is important to
understand their benefits and side effects. (PubMedHealth,2013) They are fundamentally used to
treat asthma and other pneumonic issues, for example, unending obstructive pulmonary ailment.
There are a few types of beta2 agonists' for example short acting and long ... Show more content on
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To help decrease the danger of side effects, your specialist may endorse more than one drug as
opposed to raising the current dose of your dose of your current medicine.
All medicines have symptoms and side effects. In any case, many people don't feel the symptoms
can oversee them. Get some data about the reactions of every drug you take. Indications are in like
manner recorded in the information that goes with your solution. Here are some basic things to
consider: Normally the benefits of the medication are more fundamental than any minor reactions.
Indications may leave after you take the medication for some time.
In the event that symptoms still affect the patient, he/ she should think about whether to proceed to
take the medicine, visit your physician. The physician can discontinue the dosage or change your
prescription. Do not immediately stop taking your medicine unless your specialist instructs you to.
While short–acting beta2 agonists might be the primary decision for treating side effects of mild
intermittent symptoms of COPD. Anticholinergic is typically viewed as the first line treatment for
persistent symptoms, by and large of COPD. Inhalation is the preferred technique for taking beta2–
agonists.
This strategy lessens the possibility of symptoms and makes the medicine more powerful. Pills and
injections are not used for the

Pimavanserin
The classifications of serotonin receptors, as well as drug classes that act upon serotonergic
transmission are discussed below. This includes serotonin (5–HT) agonists, antagonists and
medications that modulate 5–HT at the presynaptic level, all of which are of significant clinical
relevance.
Nuplazid (pimavanserin), is a selective serotonin inverse agonist (SSIA). Pimavanserin is a non–
dopaminergic atypical antipsychotic drug with primarily selective inverse agonistic and minor
selective inverse agonistic properties on the 5–HT2A and 5–HT2C receptors, however it has no
substantial affinity on the 5–HT2B or dopamine receptors. Pimavanserin was discovered and
developed for the treatment of Parkinson's disease Psychosis (PDP) by Acadia Pharmaceuticals. ...
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Another 5–HT2A and 5–HT2C antagonist with high affinity for dopamine receptors is the
therapeutically used atypical antipsychotic clozapine. Its significant clinical advantage is its reduced
incidence of extrapyramidal symptoms relative to first generation typical antipsychotics (Sansone,
2014).
5–HT3 antagonists include odansetron and palonosetron, which are particularly useful in the
treatment of chemotherapy–induced nausea and vomiting (Sansone, 2014).
Lysergic acid diethylamide (LSD) is a 5–HT1A, 5–HT2A, 5–HT2C, 5–HT5A and 5–HT6 agonist
demonstrating psychedelic properties. It is generally used recreationally however there is ongoing
research into it's application in LSD–assisted psychotherapy (Müller, 2015)
Pimavanserin (marketed as Nuplazid) is a drug developed and approved for the treatment of PDP by
the FDA in April 2016. Its mechanism of action and therapeutic relevance is quite significant. As
previously mentioned it is a non–dopaminergic second generation antipsychotic. It primarily
exhibits selective inverse agonistic behaviours due to its high affinity on the 5–HT2A receptors (Ki
0.087nM) albeit low affinity on the 5–HT2C receptors (Ki 0.44nM) (Meltzer et al., 2012). Although
it displays anti–hallucinogenic properties that assist in the overall alleviation of PDP, its mechanism
of action is not completely understood to

Extracellular Loop
The extracellular loops of GPCRs are important for receptor function. They contribute to protein
folding, provide structure to the extracellular region and mediate movement of the TM helices on
activation. The second extracellular loop (ECL2) is of significance for ligand binding and receptor
activation. In family B (or secretin–like) GPCRs, it is the most conserved and often the longest of all
the ECLs, and so is in a good position to interact with the endogenous peptide agonists for these
receptors and is in a prominent central position to mediate conformational changes 17. Mutations
within ECL2 have been shown to affect GLP–1 binding and efficiency, indicating an important role
in GLP–1R activation. Interestingly, some mutations ... Show more content on Helpwriting.net ...
The structural features of ECL2 and high lipophilicity of TAK–875 (which shows approximately
380–fold preference for lipophilic phase over aqueous phase) suggest that TAK–875 most probably
enters the binding pocket of hGPR40 through the lipid bilayer14. Looking at Figure 3, the crystal
structure of FFA1 provides a good starting point for understanding ligand docking which predicts
the preferred orientation of one molecule to a second molecule when bound to each other to form a
stable complex. Although docking of flexible Linoleic acid which is a natural ligand is the least
reliable, it helps to generate hypotheses as to how agonistic activity of Linoleic acid could be
amplified by synthetic agonists, like TAK–875, at a structural level. For example, targeting
Arginines, which are α–amino acids that are used in the biosynthesis of proteins, from the
extracellular side by substituting existing water–mediated contacts could still leave a possibility of
targeting the Arginines from the side involved in interactions with amino acids Tyrosines. The fact
that the ligands could have different binding modes and occupy different binding sites at FFA1 can
be also seen from a site map search (Schrodinger, LLC, New York, NY, USA 2014b) (Fig. 3, E)11.
Tikonova et al.26 validated a docking protocol of the Glide

Role Of Phosphorylation Of Second Messenger Dependent On...
1. What is the role of the phosphorylation of GPCRs in the process known as "receptor
desensitization?" First describe the process, or what is meant, by the term "receptor desensitization."
What does it mean when we say that the receptor is "uncoupled" versus "down–regulation" of the
receptor? Define and contrast the roles of the "second messenger–dependent" protein kinases versus
the "G protein–coupled receptor" kinases in the process of receptor desensitization. What do the
terms "homologous" versus "heterologous" desensitization refer to? (Ferguson, Pharmacological
Reviews 53:1–24, 2001; Gainetdinov et al., Annual Review of Neuroscience 27:107–144, 2004;
Vasudevan et al., Cell Cycle 10:3684–3691, 2011).
Receptor desensitization: ... Show more content on Helpwriting.net ...
This process called the "uncoupled". "Down regulation" means the receptor mRNA and protein
synthesis decrease and the preexisting receptor degradation. The "uncouple" and "down regulation"
are both involved in the receptor desensitization, but in different steps. These steps are following
described. First, the receptor uncouple from heterotrimeric G proteins; Second, cell surface
receptors internalize into intracellular membranous compartments; Third, receptor mRNA and
protein synthesis decrease result in the down regulation of the total cellular complement of
receptors, as well as both the lysosomal and plasma membrane degradation of pre–existing
receptors. There are two generally kinases which are G protein coupled receptor kinase GRKs and
second messenger–dependent protein kinases(e.g., PKA and PKC). The G protein coupled receptor
kinase only act on the phosphorylate agonist activate receptor. For example, GRK family members
work on activated receptors, and then promote the binding of cytosolic arrestins, which sterically
uncouple the receptor from heterotrimeric G protein. In contrast, second messenger–dependent
proteins kinases act on both phosphorylate agonist–activated GPCRs and other phosphorylates
receptors that have not been exposed to agonist. Thus, agonist–independent phosphorylation can
only happen with the second messenger–dependent protein kinases, but GRKs cannot do it. When
we recognize the

Case Study : New Ob Visit
Date: 08/22/16 Formal Write–Up #2 CC: New OB HPI: YM is a 24 year old G2P1 who presents for
New OB Visit at 28 weeks 6 days. Her concerns are the following: 1. Diarrhea – The patient reports
traveling to Hawaii approximately 3 weeks ago. She returned home with loose stools. She had a
stool sample that showed positive parasites, and was subsequently started on Metronidazole. She
finished that course of antibiotics. After that, she continued to have persistent diarrhea. She was
worked up for C. diff which was found to be negative. She states that she had bloody stools initially,
but none currently. She states now she is just having watery stools, approximately 30 times per day.
2. Abdominal cramping – She attributes this to her GI symptoms as above. She denies regular and
frequent contractions but reports irregular contractions prior to her visit today. Her cramping is
cyclic in nature and persists throughout the day. 3. UTI – She is wondering if she has a UTI. She
recently had a UTI but reports taking an alternative medicine approach to its treatment. Today she
denies dysuria, hematuria, increased frequency or hesitancy of urination. 4. Weight Loss – She
reports an inability to gain and maintain weight during pregnancy. She reports that her diarrhea has
led to water loss. She also finds it hard to find foods she can tolerate. Review of Systems:
Constitutional: negative Eyes: negative Ears, Nose, Mouth, Throat: negative Cardiovascular:
negative

Antagonist Synthesis Essay
An organ bath experiment was carried out to examine different types of antagonistic (competitive
reversible (CRA), non–competitive (NCA), and physiological antagonisms) mechanisms for
regulating the VSM tone by using NA with prazosin (Praz), serotonin (5HT) with methysergide
(Meth) and verapamil (Ver), and KCl with carbachol (Carb) on isolated rat aorta tissue. The
hypothesis is the CRA mechanism will reach max contraction, but higher concentration of agonist is
needed to reach max contraction in presence of antagonist, the NCA mechanism will show decrease
in max contraction of agonist with presence of antagonist, and physiological antagonism will show
relaxation of tissue due to the action of antagonist during presence of agonist.
Each agonist ... Show more content on Helpwriting.net ...
Antagonistic effect of Praz (10–8M) on range of NA concentrations (10–4M to 10–9M). A rat's
thoracic section of descending aorta (VSM) was used to demonstrate antagonistic mechanism of
Praz (orange) to NA's (10–4M to 10–9M) agonistic action. NA–induced contraction of VSM (blue,
10–5M to 10–9M) was measured for comparison with Praz. The NA's agonistic action and Praz's
antagonistic action toward NA were measured as force of contraction with 1.5g of baseline
contraction force. The data points in the graph are mean value of 5 groups, standard deviation as
error bar. Real contraction values were converted into percentage by using highest contraction force
value as

Drug Experiment
A.
Drug A: After the cells are exposed to drug A, an increase in the amount of cyclic AMP is seen on
the diagram. Since A increased the amount of cAMP above the basal level, A is an agonist. In this
particular experiment, we do not see an agonist that leads to a higher increase in activity; we can
thus assume that A is a full agonist.
Drug B: When the cells were exposed to drug B at two different concentrations (10uM and 10 µM),
no change in activity was noticed and it was equal to basal activity. This clearly signals that B is an
antagonist. Then we examine the effect of drug B when used in combination with drug A. The
amount of cyclic AMP has decreased as the concentration of drug B increased from 10 uM to 10 µM
while the concentration ... Show more content on Helpwriting.net ...
However, drug D in combination with drug A does produce a lower activity than drug A alone, but
this change is not concentration dependent (higher concentration of B does not lead to a decrease in
activity). One way to explain this decrease is that drug D is a partial agonist. Partial agonists act as
competitive antagonists in the presence of a full agonist (drug A in our case), depressing its ability to
achieve the maximum possible effect.
Alternatively, drug D could indeed be a competitive antagonist; we know that the parallel shift
depends only on the Ka, the dissociation constant for an antagonist and [A], the concentration of the
antagonist. The fact that the activity readings are equal at two different concentrations of Drug D
(and thus no shift in the effect curve) could thus be explained by a very large dissociation constant.
Mathematically, this scenario would lead to a ratio of [A] to Ka being close to zero for both drug D
concentrations, eliminating the shift in effect curve and showing the same activity for both
concentrations.
Drug E: The data shows the decrease in basal signaling when the cells are exposed to drug E. Thus,
we could assume that drug E is a inverse agonist. However, there is an alternative scenario where
drug E is interfering with an endogenous agonist and leads to a decrease in background activity. (a)
From the analysis above, we concluded that drugs B and C are competitive antagonists. Although to
compare

Rat Ileum Agonist Concentration: Response Relationship...
Rat ileum agonist concentration–response relationship experiment 001004296 Abstract: This
experiment involved testing the result of applying different concentrations of carbachol to a rat
ileum that was in Tyrode's solution to create an isotonic environment. Carbachol is an agonist that
will interact with a receptor to cause a biological response because of the agonist changing the state
of the receptor. Receptors are directly involved with chemical signalling so when the agonist
carbachol changes the shape of the receptor a chemical signal takes place causing a biological
response. The extent of the biological response depends on the affinity of the agonist to the receptor
and the efficacy of the agonist, which is the likeliness of the agonist ... Show more content on
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A stock solution of carbachol was provided with a concentration of 10mM. a serial dilution was
carried out to create three solutions of carbachol with concentrations of 1mM, 0.1mM and 0.01mM.
the six concentrations were 10nM, 30nM, 100nM, 300nM, 1µM and 3µM. The six carbachol FBC's
were worked out using this equation [FBC]=([drug concentration]×volume aded )/(volume in tissue
vessel) the FBC's were then calculated to be: 1x10–8 , 3x10–8 , 1x10–7 , 3x10–7 , 1x10–6 , 3x10–6.
The six carbachol concentrations were created from adding 50µl or 150µl from each of the three
serial dilutions. A chart recorder was attached to the rat ileum to record any biological responses.
The chart recorder was started before the concentrations of carbachol were applied to create a
baseline. The first concentration of carbachol (10nM) was applied to the rat ileum by adding 50µL
of the 0.01mM solution while the chart recorder was run for 30 seconds and then stopped. The
Tyrode's solution around the rat ileum was changed and left for 2 minutes between each
concentration that was applied. The second concentration of carbachol (3µM) was applied to the rat
ileum by adding 150µL of the 0.01mM solution. all the solutions were applied to the rat ileum using
a pipette. This process was then repeated until all six concentrations of carbachol had been applied
to the rat

Agonist-Induced Desensitization Case Study
Agonist–induced desensitization of G–protein coupled receptors (GPCRs) is well documented. In
particular, agonist–induced desensitization of the beta–1 adrenoceptor, beta–2 adrenoceptors,
dopamine, and opioid receptors are well studied. For many diseases processes, GPCR
desensitization is thought to contribute to the disease process or limit the effect of therapeutic
agents. Constant exposure of the receptor system molecule to a drug may result in receptor
desensitization and down–regulation. Down–regulation occurs when there is a decrease in the
number of receptor system molecules in the cell, thus decreasing the response to continued
administration of the therapeutic agent. In addition, more drugs may often be needed over time to
achieve the same therapeutic response. ... Show more content on Helpwriting.net ...
The question arises whether chronic long–term use of a beta–3 adrenoceptor agonist may be limited
by beta–3 receptor desensitization. It is conceivable that like the beta–2 adrenoceptor in airway
smooth muscle, continuous, prolonged administration of a beta–3 adrenoceptor agonist will elicit
beta–3 adrenoceptor desensitization in bladder smooth muscle. Continuous exposure of a beta–3
adrenoceptor agonist may result in a decrease in the number of beta–3 adrenoceptors, a decrease
binding affinity or diminished post–receptor signal transduction mechanisms and second messenger
signaling, resulting in a diminished therapeutic response. This study was designed to assess whether
the beta–3 adrenoceptor agonist mirabegron produce desensitization in rat–isolated urinary bladder
during electrical field stimulation (EFS) contractions by varying the time of incubation of
mirabegron with the bladder tissue. A further objective was to understand the time–course for the
re–sensitization and recovery of the functional response by varying the washout time of mirabegron
from the bladder

Albuterol Research Paper
Beta–2 Adrenergic Agonists Are Substrates and Inhibitors; Albuterol is a beta–adrenergic agonist
called also sympathomimetic. It mimics the effect of sympathetic nervous systems. Anwalla et al.
(2011) explained that Albuterol is a rescue medication in the treatment of airway disease. Albuterol
bronchodilators use and it transport exerts a significant impact on the rate of onset and the clinical
outcomes. To demonstrate the importance of the Albuterol (beta2), the National Center for Health
and the Center for Disease Control (CDC) 2014 statistics show the morbidity in the United States as,
– Adults(18 years and older) is 18.4 million – 7.6% – Children 6.2 million – 8.4 – Number of
deaths: 6.651 per year. Albuterol especially inhaled ... Show more content on Helpwriting.net ...
It is also related that the oral and inhaled long–acting beta2 agonists are used for maintenance
therapy. However, systemic or parental and oral are contraindicate for high–risk patients with
tachycardia associated with digitalis toxicity, diabetes, hyperthyroidism, organic heart disease,
hypertension or angina pectoris. Although the unstatutable albuterol majority of total flux is
paracellular, the cellular uptake; on the other hand, is saturable and its action contributes to the net
flux. If administered in large doses, it has adverse effects and this last can activate Beta 1 receptor
which action causes nefast cardiac stimulation. The writers' group also studied whether b2–agonist
interact with organic cation transporters (OCT) and whether this interaction exerted an influence on
their passage across the respiratory epithelium to their target receptors. They studied the OTC drugs
salbutamol sulfate, formoterol fumarate, and salmeterol xinafoate in vitro by [C–14}–TEA uptake
into Proxima(Calu–3) and distal (A549 and NCI–H441) lung epithelial cells and found that it was
significantly reduced by the attendance of these OTC drugs. They also confirmed that these drugs
make the transport responsible for the beta 2 agonist interaction challenging. "the expression of all
five members of the OCT/N family has been confirmed in human pulmonary epithelial cells in situ
and in

Agonist Maintenance Treatment Essay
You are in great trouble if you are addicted or live with an addict. Due to addiction, most of the
addicts die and also take down their family members with them. But if an addicted person really
wants to recover, he must remain honest to himself. Addiction treatment can comprise medications,
behavioral therapy (such as cognitive therapy, counseling or psychotherapy) or their combination.
Drug Addictions can be broken through several Addiction treatments.
Agonist Maintenance Treatment is a kind of addiction treatment which is mainly provided to the
opiate addicts. This addiction treatment helps to reduce the patients craving for the opiate. Due to
the sustained and adequate dosage of methadone, a well tested medication, the patient becomes
stabilized and can function normally.
Narcotic ... Show more content on Helpwriting.net ...
Addiction is viewed regarding an individual's mental and social deficits, and this addiction treatment
mainly aims in developing the socially creative life of the addicted.
Short–Term Residential Programs originally aimed to deal with alcohol problems, but after the
cocaine epidemic in 1980's, many started to deal with addiction treatment and illicit drug abuse.
In case of Medical Detoxification treatment, an individual is withdrawn from an addicting drug
under a physician's care. In case of some types of drugs, like alcohol, barbiturates and other
sedatives, detoxification may be medically necessary, and if it is withdrawn suddenly it may be
deadly or medically dangerous.
From several researches, it is evident that, if we combine criminal justice sanction along with drug
treatment, it can be effective in reducing drug use and other crimes.
In case of Prison Based Treatment Program, those under the addiction treatment should be separated
from the prison population so that, the "prison culture" is not able to overcome the progress towards

Dopamine Agonist Case Study
DOPAMINE AGONISTS AND IMPULSIVE AND COMPULSIVE DISORDERS IN
PARKINSONS DISEASE PATIENTS AND TARGETED THERAPEUTICS
INTRODUCTION
Dopamine agonists, pharmaceutical drugs utilized to treat motor symptoms of Parkinson's disease
have recently revealed to be strongly associated with the development of adverse pathological
impulsive compulsive disorders (ICD) in Parkinson's disease patients. Parkinson's disease is a
chronic neurodegenerative disorder linked with the loss of dopamine in the substantia nigra within
the midbrain. Dopamine is a salient chemical neurotransmitter which relays signals between
adjacent neurons involved in the initiation and control of voluntary motor movement, mood and
behavioural aspects such as reinforcement, motivation, repeated actions and ... Show more content
on Helpwriting.net ...
alcoholism, prior to Parkinson's disease diagnosis (Weintraub et al., 2009).Low dopamine levels in
the substantia nigra not only pose serious implications in the voluntary movement and walking of
Parkinson's disease patients but also in reward processing, motivation and positive emotions.
Impulsive behaviours are described as the inability to resist temptation to carry out certain activities
e.g. compulsive shopping which provide an immediate feeling of satisfaction and gratification for
the sufferer and can lead to adverse financial and social consequences. In contrast, compulsive
behaviour is characterized by an urge to perform certain action (Reference and Reference).
Impulsive compulsive behaviours linked with the use of prescribed dopamine agonists include
pathological gambling, compulsive shopping, punding, binge eating and hypersexuality, while
dopamine dysregulation syndrome(DDS) stems from the compulsive use of levodopa (Raja &
Bentivoglio,

Relevance Of Study And Scientific Background
Relevance of Study and Scientific Background
G–protein–coupled receptors (GPCRs) are crucial for multiple areas of human physiology including
vision, olfaction, taste, hormone control, and neurotransmitter control (1). As a result of its wide–
spanning functions, it is a popular area of study for therapeutic targets for many diseases (1). GPCRs
are composed of seven –helices that run through the membrane with parts both inside of the cell and
outside of the cell (1).
The widely accepted model for GPCRs work is outlined in Figure 1 of this paper (2) and is essential
for understanding the rest of the paper. An agonist binds to 2AR.Then changes occur to 2AR such
that a Gs heterotrimer complex can bind to the 2AR better. The Gs ... Show more content on
Helpwriting.net ...
T4 lysozymes (T4L) were added to 2AR to stabilize 2AR– Gs. A previous paper referenced by the
Kobilka group (3) used this approach to put T4L between TM 5 and TM 6. In it this Science paper,
they expressed concern about T4L addition modifying WT 2AR. What they found were minimal
differences in the modified 2AR compared to WT (normal antagonist binding and slightly elevated
agonist binding) (3). I would have liked to have seen a similar functional comparison done for the
WT–2AR compared to the T4L modified 2AR for this paper as well for completeness to ensure T4L
addition does not change function. Another problem was the variability in the position of GsAH. A
nanobody (Nb35) was bound to the complex to help reduce this variability. As with T4L addition, I
would have liked to have seen additional data included to show that the Nb35 addition does not
significantly alter the function of the protein complex. While Figure 2c) in the paper shows the
structure of the structure of the 2AR– Gs complex without the aids, I would have liked to have seen
some functional tests performed on the complex, both with the aids for crystallization and without
the aids for crystallization.
A key result of this paper was finding the structure of the active–state of 2AR. To find this, the
agonist–bound receptor of 2AR– Gs was compared to the inactive 2AR. A few differences were
noted. Namely, there is a 14 angstrom movement of TM 6 in the active form compared to

The, Atheists, Or Agonists
I find it interesting that for people who have no religious affiliation, or belief in God, form these
groups of "nones", atheists, or agonists. What strikes me as interesting is that while they may not
believe or struggle to believe or support a particular faith or religion, they feel the need to form large
groups or organizations that defends their right not to believe. We all have our basic human rights
and freedoms to express ourselves as we see personally fit. So why do people feel the need to
defend that or even hide it? I found this article interesting for various reasons. It really did not
surprise me to learn that almost a quarter of the population in the United States makes up this group
of "nones." While that may not seem like the majority of the population, I feel like that number will
begin to climb as our future generations grow up. I think for the longest time our culture and politics
were based heavily on religious influences for fear of backlash and disapproval from the general
population. Today people are encouraged to be open and to be themselves. We are encouraged to
accept all people regardless of their religion, color, sex, or even their sexual preference. I think
because of these things, people no longer feel like they have to hide their true identity for fear that
their religious communities or even the social community will not accept them. Maybe for these
reasons people lost faith in the religious community as well. Many of these beliefs

Melatonin Agonists
Discussion There have been studies conducted that show that targeting melatonin receptors may be a
novel way of reducing the threshold of seizure propensity. Currently, progabide is an established
drug that is used to control epileptic seizures. However, there are no studies conducted that combine
both melatonin agonists and GABA agonists together to treat epileptic seizures. Our results showed
that there was a decrease in seizure propensity when treating the mice with melatonin and GABA
agonists, however, there was an even significant decrease in seizure propensity when these two
treatments were combined together. The two–way ANOVA test also revealed that treatment and
seizure propensity had a significant difference that was ... Show more content on Helpwriting.net ...
Progabide is not a relatively popular drug for the treatment for epilepsy, so there are no concrete list
of symptoms for this drug. However, central nervous system depressants in general tend to produce
symptoms such as drowsiness or dizziness. It can also lead to suicidal thoughts or depression.21
Thus, when combined with melatonin agonists, it may produce more intense feelings of drowsiness
because melatonin also causes increased drowsiness in humans. This experiment could have been
improved if we had used rats that were genetically engineered or born with a proclivity towards
seizures. This way, we could have seen the effects of GABA and melatonin agonists on rats that had
organic long–term seizures rather than short–term seizures that were induced artificially by kainic
acid. It was found that rats purchased from a group of Crj:Wistar rats from the company Charles
River Japan spontaneously exhibited seizures. These rats were then inbred and their seizure
susceptibility loci (Ner1 and Ner2) were mapped out on chromosomes 1 and 3.22 Perhaps by using
these rats, we can truly mimic seizures that are more closely related to the ones produced

The Crystal Structure of Sphingosine
In the PDBID 3V2Y, the crystal structure of the sphingosine–1–phosphate receptor subtype 1 is
fused to T4–lysozyme. Fusion of the third intracellular loop to the T4–lysozyme rendered soluble
crystal junctions (Rosen H et al, 2013) for the rapidly disintegrating microcrystals (Hanson MA et
al, 2012).
Structure elements of S1PR1
The structural observations gained from antagonist–preserved structures of Rhodopsin–like GPCRs
show that the typical orientation of the seven transmembrane domains have significant overlap. The
minute overlap is produced depending on the helix bundle, tilt and the specific interactions
(hydrophobic and electrostatic). This specific overlap is important for co–ordinated signaling by the
different GPCRs (Rosen H et al, 2013).
GPCRs possess an extracellular domain consisting of the N terminus and three extracellular loops.
However, a number of prominent features are associated with the Ligand Binding Pocket in the
S1P1 receptor. The extracellular region of S1PR1 is significantly ordered. This is due to the N
terminus comprising a well–ordered α–helix that projects the top of the receptor. This contributes to
binding interactions and forms a helix–cap, which occludes access to the amphipathic binding
pocket (Hanson MA et al, 2012). The three loops, namely, ECL1 amidst helices II and III, ECL2
formed between helices IV and V and ECL3 in helices VI and VII, also make up the extracellular
region. Both ECL1 and ECL2 are tightly packed against the

Agonist Muscles
Example 1: javelin
Preparatory phase
Joints involved Articulating bones Action Agonist Muscle
Shoulder Humerus & scapula Horizontal hyperextension
Posterior deltoids and latissimus dorsi
Elbow Humerus & ulna Extension
Triceps brachii
Throwing contains of two phases, the preparatory phase and the throwing phase. predominantly the
majority of actions are rotational in the transverse plane and longitudinal axis and also both joints
mainly involved are the elbow, the elbow is a type of joint called a hinge joint made up by the
humerus and ulna, and the shoulder, the shoulder is different to the elbow as it's a ball socket this is
found between the humerus and the scapula.
Preparatory phase
Before throwing the javelin the arm that isn't holding ... Show more content on Helpwriting.net ...
your calf must contract to extend your ankle this is called plantar flexion, while the muscles on the
front of your shin contracts to hold your ankle rigid. The action muscle in place there is called an
isometric contraction, where the muscles create tension but, they are not causing any actual joint
movement they are just holding the ankle in place.
The power of kicking a ball predominantly comes from the knee straightening. This knee extension,
can only happen if the top thigh muscles contract. These muscles are called your quadriceps, that
have four individual components; the vastus lateralis, vastus medialis rectus femoris and vastus
intermedius. these all join just above the shin therefore being able to lift the lower leg
Moving your leg forward from your hip is a movement called hip flexion. This is the biggest joint
action in football, as it starts as an extension and finishes with a significant push forward going past
the body's midline. To allow hip flexion to occur, your three hamstring muscles –– semitendinosus,
semimembranosus and biceps femoris –– must relax. Tight hamstrings may effect your tecniwue and
ability to

Therapy For Diabetes : Conclusion Or Illusion? Essay
GLP–1–GASTRIN AGONIST BASED THERAPY FOR DIABETES: CONCLUSION OR
ILLUSION?
Keywords: diabetes mellitus, dual agonist, gastrin, GLP–1, glucose tolerance
Abbreviations: β–cell, pancreatic beta–cell; DDP–4, dipeptidyl peptidase–4; GLP–1, gluacgon–like–
peptide–1; OGTT, oral glucose tolerance test; PPAR–γ, peroxisome proliferator–activated receptor–
γ
TABLE OF CONTENTS
1. Revised Commentary 2
1.1 Main Findings 2
1.2 A Repeat of History 4
References 6
2. Feedback Received from Peers 7
2.1 First feedback form 7
2.2 Second feedback form 8
3. Response to Feedback 10
Characterised by impaired β–cell and insulin function, diabetes mellitus is undoubtedly becoming a
hallmark point of interest in science and pharmacology. Indeed, a wide array of antihyperglycaemic
agents have been successfully developed and used for the treatment of diabetes including Type 1,
Type 2, and gestational varieties. However, many of these drugs have traditionally been targeted at
single molecular targets and have unknown effects on the direct turnover of β–cells (Finan et al.,
2015). GLP–1 agonists are one new class of drugs used to treat Type 2 diabetes and target the
incretin hormone group to increase their levels in the body, thereby stimulating insulin release.
GLP–1 agonists have been shown to display additional positive effects on gastric emptying and
satiety following meals. Fosgerau et al., (2013) used GLP–1 agonists in conjunction

Neurotransmitters And Its Effect On The Brain
Neurotransmitters communicate by transmitting signals from a neuron to a target cell through a
synapse. Before this communication can happen, the neurotransmitter must be synthesized and
stored in vesicles so that when an action potential arrives, the cell is ready to fuss with the
membrane of the neuron. When the synaptic vesicle is ready, the final triggering of vesicle fusion
with the presynaptic terminal membrane occurs rapidly in response to the action potential invasion
of the terminal. This step is highly dependent on calcium ions, which enter the terminal through
voltage–gated calcium channels (Steinberg & Walton, 1978; Westenbrock, 1981). This action
potential causing the opening of calcium channels for calcium ions to stream into the presynaptic
cleft. The presence of calcium ions cause the synaptic vesicle to open and release neurotransmitters
which fuses into the cleft. Miledi (1967) suggested that the idea that calcium entry into the terminal
is a key step in the neurotransmitter release process formed the basis of what is known as the
"calcium hypothesis." Next, when an action potential does arrive at the terminal, the
neurotransmitter is released from the terminal into the synaptic cleft. When the neurotransmitter
arrives into the synaptic cleft, it must be recognized by its own receptors in the postsynaptic cell to
create the binding action, causing ion channels to open, thus changing membrane potential and
initiating another action potential. After the

Lysergic Acid Diethlyamide Essays
Lysergic Acid Diethlyamide The psychedelic effects of d–Lysergic Acid Diethylamide–25 (LSD)
were discovered by Dr. Albert Hoffman by accident in 1938. In the 1950s and 1960s, LSD was used
by psychiatrists for analytic psychotherapy. It was thought that the administration of LSD could aid
the patient in releasing repressed material. It was also suggested that psychiatrists themselves might
develop more insight into the pathology of a diseased mind through self experimentation. 1,2 During
the late 60s, LSD became popular as a recreational drug. While it has been suggested that
recreational use of the drug has dropped, a recent report on CNN claimed that 4.4% of 8th graders
have tried it. LSD is considered to be one of, if not the, most ... Show more content on
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A Brief Foray Into Philosophy and the Cognitive Sciences Modern physics is divided by two
descriptions of the universe: the theory of relativity and quantum mechanics. Many physicists have
faith that at some point a "Grand Unified Theory" will be developed which will provide a unified
description of the universe from subatomic particles to the movement of the planets. Like in physics,
the cognitive sciences can describe the brain at different levels of abstraction. For example,
neurobiologists study brain function at the level of neurons while psychologists look for the laws
describing behavior and cognitive mechanisms. Also like in physics, many in these fields believe
that it is possible that one day we will be able to understand complicated behaviors in terms of
neuronal mechanisms. Others believe that this unification isn't possible even in theory because there
is some metaphysical quality to consciousness that transcends neural firing patterns. Even if
consciousness can't be described by a "Grand Unified Theory" of the cognitive sciences, it is
apparent that many of our cognitive mechanisms and behaviors can. While research on the level of
neurons and psychological mechanisms is fairly well developed, the area in between these is rather
murky. Some progress has been made however. Cognitive scientists have been able to associate

The Complexity Of Endogenous Ligands For P2YR
Endogenous ligands for P2YR The most abundant and best–characterized endogenous ligand for
P2YR is the nucleotide ATP. ATP binds to all P2YRs except P2Y6R and P2Y14R12. Its binding
characteristics exemplify the complexity of P2YR signalling: at low concentrations it is the only
native agonist for P2Y11R, but at higher concentrations it functions as a partial agonist for P2Y1R
and P2Y13R, or as an antagonist for human P2Y4R or P2Y12R11, 12, 15. Other nucleotides, such
as ADP, UTP, UDP or UDP–glucose, exhibit more specificity for individual P2YRs. For example,
ADP activates P2Y1R, P2Y12R and P2Y13R, whereas UTP primarily binds to P2Y2R and P2Y4R,
and to a lesser extent to P2Y6R, for which UDP is its preferred native ligand. P2Y14R is ... Show
more content on Helpwriting.net ...
Functional roles of P2YR in unchallenged mice Mice with genetic deletions for human P2YR
homologous genes have been generated and characterized, with the exception of P2RY11, which is
not expressed in mice12. Despite their widespread expression and their functional involvement in
many diseases, mice with global deletions for individual P2YRs display only mild phenotypical
alterations when maintained unchallenged in a germ–free environment. For instance, P2ry2−/− mice
have slightly lower plasma concentrations of aldosterone, renin and potassium20, whereas global
deletion of P2ry4 is associated with lower exercise capacity and reduced myocardial hypertrophy
during a swimming exercise21. These findings indicate the likelihood of some redundancy in the
signalling system, or compensatory mechanisms following global P2ry gene deletion. P2YR
signalling during inflammatory disease states Introduction Cellular ATP release during inflammatory
conditions P2YR signalling during inflammatory disease states P2XR signalling during
inflammation Termination of ATP signalling Functional role of P1 signalling during inflammation
Conclusions Change history References Acknowledgements Author information Supplementary
information Several studies over the past decade have highlighted fundamental roles for P2YRs
during inflammatory

Feasibility Of Designing Partial Agonists Of The Human...
This article presents a study performed to demonstrate the feasibility of designing partial agonists of
the human muscarinic M1 receptor that would modulate the receptor in two distinct ways
simultaneously. It also explains the signaling behavior of the receptor.
The muscarinic M1 receptor was described as the one of five subtypes of the muscarinic G protein–
coupled receptors (GPCRs) with the highest expression in the central nervous system. Two
downstream effects of activating the M1 receptor were identified, activating of phospholipase C
mainly by Gq/G11–proteins and influencing ion channels like the N–methyl–D–aspartate (NMDA)
receptor and voltage–gated Ca2+ channels. These two ion channels were reported to be therapeutic
importance in ... Show more content on Helpwriting.net ...
The hybrids synthesized were classified into four main groups (2, 3, 4, and 5) based on the
orthosteric agonist, the allosteric moiety and the number of carbon atoms in the linker moiety.
Derivatives of benzyl quinolone carboxylic acids (BQCA), that function as positive allosteric
modulators and allosteric agonists of M1 receptors were linked with the M2 selective orthosteric
superagonist, Iperoxo in hybrids 2 and 3. In hybrid 4, another derivative of BQCA was linked with
the compound 1 (AF292), a M1 selective agonist. Hybrid 5 was synthesized with compound 1
linked to the allosteric binding moiety of an allosteric agonist, 1–(1′–(2–methylbenzyl)–1,4′–
bipiperidin–4–yl)–1H–benzo[d]imidazol–2(3H)–one (TBPB) using linker moieties of three different
lengths.
The response obtained when the receptors were saturated with Acetylcholine, the endogenous
muscarinic ligand, was defined as the system's maximal response. The data obtained from the DMR
measurements were reported to have been analyzed using the operational model of agonism for
dynamic ligands. From the results, iperoxo did not function as a superagonist at the M1 receptor.
The synthesized hybrid compounds in the groups 2 and 3 were observed to act as partial agonists at
the M1 receptor. The substitutions on the quinolone moiety of group 2 compounds were said to have
no

Salbutamol
Bronchodilator Response of Nebulized Salbutamol versus Salbutamol and Ipratropium Bromide in
Adult Patients with Acute Severe Asthma
Introduction:
Acute severe asthma previously called status asthmaticus is a life threatening medical condition
characterized by bouts of repeated and worsening cough, wheezing, chest recession and inability to
speak or drink that may result in acute respiratory failure and even death.1 These patients are also at
risk for developing serious complications like aspiration pneumonia, pneumo–mediastinum,
pneumothorax and hypoxic brain injury etc. 1Inhaled high dose short acting β2 agonists like
salbutamol along with systemic steroids and supplemental oxygen are considered as first line
treatment in all patients who ... Show more content on Helpwriting.net ...
Rationale:
Although there are local studies on various aspects of asthma, there is no local study in Pakistan
published so far which compares the response of nebulised salbutamol alone with combination of
ipratropium bromide in adult population with acute severe asthma. This study has been planned to
compare these two approaches. My study will help for better management of patients who report to
emergency department with this potentially life threatening

Effects Of Exposure Of Females To Androgen Agonists
Exposure of females to androgen agonists imbalances sex hormones in the brain. Anxiety, mood
disorders, and pathopsychological behaviors are the resultant effects 1. These presentations are
caused by alteration in the amygdala region of the brain. For example, the expression of AR gene
inhibits anxiety is suppressed while increasing the expression of the serotoninergic GABAergic
receptor1. Exposure also causes infertility in some females. Where children are born, males are
prone to insulin resistance and obesity while females develop high androgen secretion that may lead
to PCOS and psychopathological disorders1. Studies also show that exposure at a prenatal stage
affects sexual orientation where such females tend to be sexually drawn to ... Show more content on
Helpwriting.net ...
This hormone restores bleeding during the withdrawal intervals. For those still with a uterus,
progesterone is also administered to curb endometrial growth that may cause cancer. Estradiol is
given for oral use or through transdermal injection. Annual review is conducted to analyze benefits
and side effects and also adjust treatment appropriately. Estrogen in the therapy has a lot of clinical
benefits. Results from studies indicate that it reduces atherosclerosis and low–density cholesterol. It
elevates high–density cholesterol and improves coronary vasodilation. Platelet aggregation
prevented and reduced fracturing is also observed in HRT use. HRT was also reduced cardiovascular
event and related mortalities. HRT also does not increase the risk to stroke, common in old age as
supported by the Schierbeck study in 1993 and follow up for the next sixteen years4. In women
where menstruation occurs prematurely, osteoporosis is prevented through HRT. HRT also improves
mood as it is neuroprotective, it preserves cognitive functioning and reduces the incidence of
Alzheimer's disease4. HRT has also negative effects. In some women, it predisposes them to cancer
with the risk reverting to that of the population after withdrawal. Muscular cramps, bloating,
headaches and tenderness are the most common symptoms. Tibolone causes recurrence of breast
cancer in women who are ER+ 4. Obesity and Early Puberty Obesity is a condition of overweight
and in children, it is highly associated

The Role Of Endothelin Receptor Populations On Ventricular...
Use of Competitive Radioligand Binding to examine Endothelin Receptor Populations on
Ventricular Cardiomyocyte Membranes of Spontaneous Hypertensive Rats. Abstract
This investigation concerned the relationship between endothelin receptor populations on the
ventricular cardiomyocyte membrane of spontaneous hypertensive rats at 16 weeks old. The use of
radioligand competitive binding assay method, involving the displacement of [125I]ET–1 by 3
competitive, cold ligands, ET–1, ET–3 and BQ123, allowed for the generation of competition
binding curves, that adopted either a one–site or two–site model and allowed the determination of
relative IC50s and identification of receptor proportions. ET–3 produced a two site model
suggesting the existence of ET–A and ET–B receptors on cardiomyocyte membranes in SHRs and
calculated that around 29% of receptors were ET–B, whereas ET–1 and BQ123 both produced one–
site models.
Introduction
Endothelin peptide family is a group of 3 isoforms of a peptide, comprising of 21 amino acids, all of
which are formed from the same larger precursor, pro endothelin–1 by endothelin converting
enzyme. (Inoue A et al,1989) Each isoform is distinguished from the others by a differing gene, with
endothelin 2 and 3 differing from endothelin 1 by 2 and 6 amino acids, respectively. (Inoue A et
al,1989) Endothelin is known mostly as a potent vasopressor, but is also known to have a positive
inotropic effect on the heart, act as a proliferator of vascular smooth

Blood Doping, Human Growth Hormones, Steroid, Beta 2 Agonists
Erythropoietin (EPO), blood doping, human growth hormones, steroid, beta–2 agonists. These are a
few substances that come into mind when discussing the topic 'performance enhancing drug ' also
known as doping. Doping is defined as the use of drugs to enhance performance and gain advantage
over the other competitors, and it has been an ongoing problem in the sport community since the
early centuries, with an increasing trend showing today. Envision yourself competing against an
opponent who has been doping! How would you feel about that? Would you feel cheated? I know I
would. As all the hard work, dedication, and effort I have put into my training has been reduce down
to nothing. Can you also imagine what doping would do to the integrity of sport! The intrinsic worth
that make sports so unique and important to society, such as the capability to challenge and push
ourselves beyond our own limits, the honesty and sportsmanship qualities athletes learn and gain.
So, does doping destroy the integrity of sport? Some may argue yes and some may say no for a few
reasons that will be examined further into the essay. However, my response would be "yes", as I
personally believe those qualities that creates the uniqueness of sport would be eliminate when
doping is involved. The manipulation of performance enhancing drugs will impact the sporting
community in an unnecessary manner, by giving it an appalling reputation. This appalling reputation
will develop as doping conveys a

Body Movement Analysis
I am going to analyze the complex movement of throwing a football I am going to be focused on the
upper body movement of throwing a football. I am going to be talking about all the muscles
involved in the movement. I am also going to be talking about the muscles origin and insertion,
there primary action, and which muscles are the agonists, antagonists, stabilizers, synergists and
neutralizers. I will also be talking about what plane the movement takes place in and what type of
lever system the prime movers are. I am first going to talk about the movement of throwing a
football I will then talk about the primary action of each muscle involved and then the origin,
insertion and which muscles are the agonists, antagonists, stabilizers, synergists ... Show more
content on Helpwriting.net ...
The anterior deltoid is an agonist in the acceleration part of the throw its origin is the anterior border
and upper surface of the lateral third of the clavicle its insertion is the deltoid tuberosity of humerus.
The pectoralis major is also an agonist in the acceleration part of the throw its origin is the clavicle,
the sternumand upper ribs, and the tendon of the external oblique muscle the insertion is the lateral
lip of the bicipital groove of the humerus. The triceps brachii is an agonist in the acceleration part of
the throw and an antagonist when the ball is being drawn back. Its long head origin is the
infraglenoid tubercle of scapula, its lateral heads origin is above the radial sulcus, and its medial
head is below the radial sulcus and its insertion is the olecranon process of ulna. The Infraspinatus is
a synergist for the rotator cuff during the acceleration phase. Its origin is the infraspinous fossa of
the scapula and its insertion is the middle facet of greater tubercle of the humerus. The biceps
brachii is an agonist when the ball is being drawn back and an antagonist when the ball is
accelerated forward. The origin of its short head is the coracoid process of the scapula and the origin
of its long head is the supraglenoid tubercle of the scapula and its insertion is the tuberosity of the

A Short Story : A Good Man Is Hard To Find
The short story " A Good Man is Hard to Find" is a story that quite frankly left me perplexed the
first time I read it. The story is written in a third person perspective that follows the road trip of a
grandmother and her son Baileys family, which is comprised of Baileys wife whose name is never
mentioned in the story and their three children John Wesley, June Star and a baby that's name is not
mentioned either. The story is set mainly in the family car, with a stop at a local diner and ultimately
on an abandoned highway. My original idea of what the story would be from the title and the first
few paragraphs would be a classic love story, where the grandmother tells her grandchildren about
the love of her life especially when she starts telling a story of a boy who used to bring her
watermelon and carved his initials into the watermelon for her every weekend (par. 26).
The story starts off with the Grandmother trying to talk her son Bailey out of taking the family to
Florida for their vacation by bringing up the misfit a man who had just escaped from a federal prison
by saying she could not in her good conscience bring her children in any direction the misfit may be
as it would not be safe (par. 1). The real reason for the grandmothers disapproval of the trip to
Florida was because she personally wanted to go to Tenasee to visit some people from past. Which I
believe is the beginning to the author foreshadowing her personality, which is a crucial part for
readers to

The Role Of 3, 4-Methylenedioxymethamphetamine In The...
The role of 3,4–Methylenedioxymethamphetamine (MDMA) in the scientific community is
controversial, but recent findings suggest that it could be a promising aid in psychotherapy
(Mithoefer et al., 2013). MDMA is a popular recreational drug that has both stimulant and
hallucinogenic properties and is known to promote positive mood and enhanced overall sociability
in users (Liechti et al., 2001). An overwhelming amount of past research on MDMA raises concerns
about its neurotoxicity, but there is no present consensus on the topic due to both the lack of
translatability across species and inconsistent findings (Mueller et al., 2013). Despite the uncertainty
about its neurotoxicity, MDMA is presently undergoing trials to test its efficacy as a ... Show more
content on Helpwriting.net ...
A 5–HT2A receptor antagonist blocked the social effects of MDMA. A 5–HT2C agonist decreased
huddling but did not affect social vocalizations, and a 5–HT1A agonist decreased huddling (Pitts et
al., 2017). The researchers concluded that MDMA and its enantiomers increase the frequency of
affiliative behaviors and vocalizations in a dose–dependent fashion, and the behavioral effects of
MDMA are 5–HT2A receptor dependent (Pitts et al., 2017). This study has many strengths. Squirrel
monkeys are an excellent model because they are behaviorally well–characterized and metabolize
MDMA quite similarly to humans, which gives the results better translatability to humans than
rodent models (Mueller et al., 2013). LMMs were a strong choice for analysis, as they are capable of
identifying a relationship between several variables while also reducing the risk of a type I error.
Testing both racemic MDMA and its individual enantiomers was critical to improve understanding
of each enantiomer's distinct behavioral effects, which was seldom considered in past studies.
Controlling doses by subject mass was also essential–the effects of MDMA are heavily dose–
dependent, and skew from dosing error could alter the size of the observed behavioral effect
between individuals (Liechti et al., 2001). The use of antagonists and agonists to observe the
function of individual receptor subtypes in relation to the behavioral effects of MDMA was critical
for improving the pharmacological

Gpr Structure
The understanding and studying of the GPCR structure is very important for designing the right
drugs. Studies have shown that some of the GPCRs are not pоtential drug targets because their
physiological function cannot be related to disease. Such GPCRs include the sensоry (olfactory,
taste) receptоrs and thus, leave 369 GPCRs that are pоtential drug targets (Gloriam et al., 2007). 46
of these are being targeted successfully by drugs – the rhodopsin–, secretin– and glutamate–like
receptor families. β–adrenergic, angiotensin II and vasopressin receptors are examples of GPCRs
that are lоcated in the membranes of cardiac cells and play key role in regulatiоn of the cardiac
functiоn (for example, cardiac muscle contractility, blood pressure, etc.). ... Show more content on
Helpwriting.net ...
Rimonabant is an agent that is an inverse agonist of the CB1 receptor but is known to have
antagonist actions. As a result of those actions it reduces obesity and smoking cessation but has side
effects such as nausea, emesis, depression and anxiety (Despres et al., 2005) which were shown to
be the opposite effects of CB1 agonists. Therefore, novel drugs might be neutral antagonists and it
has been suggested that they would not cause such side effects. Laboratory studies provided
evidence that inverse agonists (e.g. rimonabant) reduce fооd intake and body weight, but cause
gastrointestinal side effects in rats, while neutral antagonists (e.g. AM6545, AM4113) also reduce
fооd intake and weight, but do not cause such adverse side effects in the same animal models (Cluny
et al., 2010; Cluny et al., 2011). Therefore, neutral antagonists are thought to be potential drugs for
GPCRs, if acting without any side effects (in the case of CB1 – provide action like rimonabant but
do not cause gastrointestinal irritation or alter mood), but more studies and experiments need to be
done in order to provide evidence and release such drugs on the

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