5-Hydroxytryptamine & it’s Antagonist is a Topic in Pharmacology which will defiantly Help You in pharmacy field All information is related to pharmacology drug acting and it's effect on body. it is collage project given by our department i would like to share with you.
Seretonin (5HT) and Its Antagonists PharmacologyPranatiChavan
Serotonin is a chemical that has a wide variety of functions in the human body. It is sometimes called the happy chemical, because it contributes to wellbeing and happiness.
The scientific name for serotonin is 5-hydroxytryptamine, or 5-HT. It is mainly found in the brain, bowels, and blood platelets.
Serotonin is used to transmit messages between nerve cells, it is thought to be active in constricting smooth muscles, and it contributes to wellbeing and happiness, among other things. As the precursor for melatonin, it helps regulate the body’s sleep-wake cycles and the internal clock.
It is thought to play a role in appetite, the emotions, and motor, cognitive, and autonomic functions. However, it is not known exactly if serotonin affects these directly, or if it has an overall role in co-ordinating the nervous system.
Autacoids - pharmacological actions and drugs related to them. SIVASWAROOP YARASI
Autacoids or "autocoids" are biological factors which act like local hormones, have a brief duration, and act near the site of synthesis. The word autacoids comes from the Greek "autos" (self) and "acos" (relief, i.e. drug).
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
Detailed information of all terms like Thyroid gland, Thyroxine, Triidothyronine, Calcitonine, growth and development , propylthiouracil, Calorigenesis, tadpole to frog, Oligomenorrhoea, snehal chakorkar, pharmacology, Cretinism, Myxoedema coma, Graves disease, Thiocynates, Perchlorate, Nitrates.
Radioactive iodine, I131
Seretonin (5HT) and Its Antagonists PharmacologyPranatiChavan
Serotonin is a chemical that has a wide variety of functions in the human body. It is sometimes called the happy chemical, because it contributes to wellbeing and happiness.
The scientific name for serotonin is 5-hydroxytryptamine, or 5-HT. It is mainly found in the brain, bowels, and blood platelets.
Serotonin is used to transmit messages between nerve cells, it is thought to be active in constricting smooth muscles, and it contributes to wellbeing and happiness, among other things. As the precursor for melatonin, it helps regulate the body’s sleep-wake cycles and the internal clock.
It is thought to play a role in appetite, the emotions, and motor, cognitive, and autonomic functions. However, it is not known exactly if serotonin affects these directly, or if it has an overall role in co-ordinating the nervous system.
Autacoids - pharmacological actions and drugs related to them. SIVASWAROOP YARASI
Autacoids or "autocoids" are biological factors which act like local hormones, have a brief duration, and act near the site of synthesis. The word autacoids comes from the Greek "autos" (self) and "acos" (relief, i.e. drug).
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
Detailed information of all terms like Thyroid gland, Thyroxine, Triidothyronine, Calcitonine, growth and development , propylthiouracil, Calorigenesis, tadpole to frog, Oligomenorrhoea, snehal chakorkar, pharmacology, Cretinism, Myxoedema coma, Graves disease, Thiocynates, Perchlorate, Nitrates.
Radioactive iodine, I131
Introduction to Physiological and pathological role of serotonin
Autocoids, Classification, synthesis ,Serotonergic receptors, Physiological actions, Pathophysiological role
Presented by
K.Firdous banu
Department of Pharmacology
Histamine, meaning ‘tissue amine’ (histos—tissue) is almost ubiquitously present in animal tissues and in certain plants, e.g. stinging nettle. Its pharmacology was studied in detail by Dale in the beginning of the 20th century when close parallelism was noted between its actions and the manifestations of certain allergic reactions. It was implicated as a mediator of hypersensitivity phenomena and tissue injury reactions. It is now known to play important physiological roles.
this will give brief about the peptic ulcer and give information about the drug used for peptic ulcer and classification of drugs including drugs and there use adverse effect.
Histamine is an endogenous substance that is amine synthesized, stored and released by the various cells of the body: (a) Mast cells, which are abundant in the skin, GI, and the respiratory tract,
(b) Basophils in the blood, and (c) Some neurons in the CNS and peripheral NS.
It is an “Autocoid” that is secreted locally and regulate the activity of various near lying cells and neurons.
Introduction to Physiological and pathological role of serotonin
Autocoids, Classification, synthesis ,Serotonergic receptors, Physiological actions, Pathophysiological role
Presented by
K.Firdous banu
Department of Pharmacology
Histamine, meaning ‘tissue amine’ (histos—tissue) is almost ubiquitously present in animal tissues and in certain plants, e.g. stinging nettle. Its pharmacology was studied in detail by Dale in the beginning of the 20th century when close parallelism was noted between its actions and the manifestations of certain allergic reactions. It was implicated as a mediator of hypersensitivity phenomena and tissue injury reactions. It is now known to play important physiological roles.
this will give brief about the peptic ulcer and give information about the drug used for peptic ulcer and classification of drugs including drugs and there use adverse effect.
Histamine is an endogenous substance that is amine synthesized, stored and released by the various cells of the body: (a) Mast cells, which are abundant in the skin, GI, and the respiratory tract,
(b) Basophils in the blood, and (c) Some neurons in the CNS and peripheral NS.
It is an “Autocoid” that is secreted locally and regulate the activity of various near lying cells and neurons.
This slideshare is about what is autocoid,and differences between harmone and autocoid and had expalined about an example which is an autocoid and also an chemical messenger.and it is also known as happy harmone.
5HT widely distributed in:
GIT enterochromaffin cells (90%)
myenteric plexus where it serves as a prokinetic agent
As a neurotransmitter in CNS
platelets where it diffuses inside from plasma by active transport, and is released at the site of damage after platelet aggregation,
In lungs, bone marrow, pineal gland (as a precursor of melatonin)
5- HT is then stored in 5-HT containing cells such as enterochromaffin cells and neurons as co-transmitter together with various peptide hormones such as somatostatin, vasoactive intestinal peptide and substance P
5-HT is stored within storage vesicles, and its uptake at the vesicular membrane by vesicular monoamine transporter (VMAT-2) is inhibited by reserpine.
Degradation occurs through oxidative deamination by MAO, to 5-hydroxyindole acetaldehyde followed by its oxidation to 5-hydroxyindole acetic acid (5-HIAA)
5- HIAA is excreted in urine
Gaddum and Picarelli (1957) classified 5-HT receptors into musculotropic (D type) and neurotropic (M type) on the basis of their blockade by Dibenzyline (phenoxybenzamine) and Morphine.
5- HT Receptors: there are seven main types (5-HT1, to 5- HT7) of serotonin receptors. Of these, 5-HT1, and 5- HT2, are subdivided further. With a total of 14 (types plus subtypes) receptors.
5-HT Receptors Location: 5-HT, receptors are located mainly in CNS. They function as inhibitory presynaptic receptors (auto receptor) and belong to the family of G-protein coupled receptors linked to adenylate cyclase
5-HT1 : Auto receptors; inhibit serotonergic neural activity in brain.
5-HT1A—present in raphe nuclei and hippocampus; buspirone (antianxiety) may act through these receptors.
5-HT1D/1B—Constricts cranial blood vessels and inhibits release of inflammatory neuropeptides in them; sumatriptan (antimigraine) acts through these receptors.
5-HT2A : Previously D type receptor; most important post junctional receptor mediating direct actions of 5-HT like vascular and visceral smooth muscle contraction, platelet aggregation, neuronal activation in brain; ketanserin blocks these receptors.
5-HT3 : Previously M type receptor; depolarizes neurones by gating cation channels; elicits reflex effects of 5-HT—emesis, gut peristalsis, bradycardia, transient hypotension, apnoea, pain, itch; ondansetron (antiemetic) acts by blocking these receptors.
5-HT4 : Mediate intestinal secretion, augmentation of peristalsis. Renzapride (prokinetic) is a selective 5-HT4 agonist.Central Nervous System : 5-HT is an important neurotransmitter in CNS
5-HT is involved in the regulation of mood, behaviour, sleep, depression, pain perception, sexual activity, thermoregulation
in the hypothalamic control of the release of pituitary hormones.
Serotonin is one of the most important Neurotransmitter and made up of amino-acids. Including L-tryptophan, only the L-isomer is used in protein synthesis and can pass across the blood-brain. Serotonin concentration in organisms is among the lowest of all amino acids and it has relatively low tissue. In this paper a brief review has done pertaining to history of serotonin, and potential cognitive aspects including CNS and PNS modulation of serotonin. Major focus of paper is to review subtypes of serotonin receptors. It’s gathered up-to-date information about other pharmacological agents such as agonist and antagonist of serotonin.
This presentation is about the neurotransmitter 5-HT (serotonin), we focused on its definition, biosynthesis, storage and destruction, with mentioning its both central and peripheral effects, and lastly the serotonin receptors in the human body, as well as their agonist and antagonists.
Serotonin is major neurotransmitter and affects the physiology of our body. Serotonin antagonists are used in various pathological conditions of body. This is a small presentation showing feature of serotonin.
Gastro retentive drug delivery systems by shubham patilShubham Patil
General Discussion on Drug delivery System specially focused on Gastro-Retentive. I've covered various types and theories & understandably prepared this presentation for everyone who reads it.
Overview of means & methods used in structural elucidation of natural products. Presentation Topic Given by Faculty, It is compulsory because for this we are having our internal marks.
"DRUG RESPONSE CURVE & THERAPEUTIC" it's a topic in which detail information about How Drug Response when taken in body & effect of various drugs on body with there Response Curve is Given.
The Topic PHARMACOKINETICS & METABOLISM gives you detail information about (1st pass metabolism of drug, organs & enzymes involed in drug metabolism, All Phases of Drug) & All you need to know about BIO-TRANSFORMATION.
DRUG DISCOVERY & DEVELOPMENT PROCESS, it's a detail description about how drug is made available in market it's development and discovery of drug The Hole Study is given in This Topic.
It's a Beautiful Topic Called ERGASTIC CELL CONTENT & METABOLITES, gives you information about metabolites, plant constituents, crystal system, crystal forms & a detail information abut primary & secondary metabolites.
Operation “Blue Star” is the only event in the history of Independent India where the state went into war with its own people. Even after about 40 years it is not clear if it was culmination of states anger over people of the region, a political game of power or start of dictatorial chapter in the democratic setup.
The people of Punjab felt alienated from main stream due to denial of their just demands during a long democratic struggle since independence. As it happen all over the word, it led to militant struggle with great loss of lives of military, police and civilian personnel. Killing of Indira Gandhi and massacre of innocent Sikhs in Delhi and other India cities was also associated with this movement.
2024.06.01 Introducing a competency framework for languag learning materials ...Sandy Millin
http://sandymillin.wordpress.com/iateflwebinar2024
Published classroom materials form the basis of syllabuses, drive teacher professional development, and have a potentially huge influence on learners, teachers and education systems. All teachers also create their own materials, whether a few sentences on a blackboard, a highly-structured fully-realised online course, or anything in between. Despite this, the knowledge and skills needed to create effective language learning materials are rarely part of teacher training, and are mostly learnt by trial and error.
Knowledge and skills frameworks, generally called competency frameworks, for ELT teachers, trainers and managers have existed for a few years now. However, until I created one for my MA dissertation, there wasn’t one drawing together what we need to know and do to be able to effectively produce language learning materials.
This webinar will introduce you to my framework, highlighting the key competencies I identified from my research. It will also show how anybody involved in language teaching (any language, not just English!), teacher training, managing schools or developing language learning materials can benefit from using the framework.
Model Attribute Check Company Auto PropertyCeline George
In Odoo, the multi-company feature allows you to manage multiple companies within a single Odoo database instance. Each company can have its own configurations while still sharing common resources such as products, customers, and suppliers.
Unit 8 - Information and Communication Technology (Paper I).pdfThiyagu K
This slides describes the basic concepts of ICT, basics of Email, Emerging Technology and Digital Initiatives in Education. This presentations aligns with the UGC Paper I syllabus.
How to Make a Field invisible in Odoo 17Celine George
It is possible to hide or invisible some fields in odoo. Commonly using “invisible” attribute in the field definition to invisible the fields. This slide will show how to make a field invisible in odoo 17.
Ethnobotany and Ethnopharmacology:
Ethnobotany in herbal drug evaluation,
Impact of Ethnobotany in traditional medicine,
New development in herbals,
Bio-prospecting tools for drug discovery,
Role of Ethnopharmacology in drug evaluation,
Reverse Pharmacology.
The Roman Empire A Historical Colossus.pdfkaushalkr1407
The Roman Empire, a vast and enduring power, stands as one of history's most remarkable civilizations, leaving an indelible imprint on the world. It emerged from the Roman Republic, transitioning into an imperial powerhouse under the leadership of Augustus Caesar in 27 BCE. This transformation marked the beginning of an era defined by unprecedented territorial expansion, architectural marvels, and profound cultural influence.
The empire's roots lie in the city of Rome, founded, according to legend, by Romulus in 753 BCE. Over centuries, Rome evolved from a small settlement to a formidable republic, characterized by a complex political system with elected officials and checks on power. However, internal strife, class conflicts, and military ambitions paved the way for the end of the Republic. Julius Caesar’s dictatorship and subsequent assassination in 44 BCE created a power vacuum, leading to a civil war. Octavian, later Augustus, emerged victorious, heralding the Roman Empire’s birth.
Under Augustus, the empire experienced the Pax Romana, a 200-year period of relative peace and stability. Augustus reformed the military, established efficient administrative systems, and initiated grand construction projects. The empire's borders expanded, encompassing territories from Britain to Egypt and from Spain to the Euphrates. Roman legions, renowned for their discipline and engineering prowess, secured and maintained these vast territories, building roads, fortifications, and cities that facilitated control and integration.
The Roman Empire’s society was hierarchical, with a rigid class system. At the top were the patricians, wealthy elites who held significant political power. Below them were the plebeians, free citizens with limited political influence, and the vast numbers of slaves who formed the backbone of the economy. The family unit was central, governed by the paterfamilias, the male head who held absolute authority.
Culturally, the Romans were eclectic, absorbing and adapting elements from the civilizations they encountered, particularly the Greeks. Roman art, literature, and philosophy reflected this synthesis, creating a rich cultural tapestry. Latin, the Roman language, became the lingua franca of the Western world, influencing numerous modern languages.
Roman architecture and engineering achievements were monumental. They perfected the arch, vault, and dome, constructing enduring structures like the Colosseum, Pantheon, and aqueducts. These engineering marvels not only showcased Roman ingenuity but also served practical purposes, from public entertainment to water supply.
2. 5-Hydroxytrptamine Receptor Antagonists
{5HT3RAs}
Introduction :-
They are a group of drugs which are
used to control, prevention, treatment of nausea &
vomiting partially that caused by Chemotherapy,
radiation therapy or postoperatively.
They get their name through their
ability to block 5-HT (also known as Serotonin)
from activating nerves that bring about the vomiting
reflux.
3. History
Overview of important finding in the History
of Serotonin before & around the period in which Serotonin
was identified as Neurotransmitter, associated with the central
Nuclei of the Autonomic Nervous System.
5-Hydroxytryptamine or Serotonin Blockers,
were originally discovered in the 1990s & are one of the
newest types of anti-vomiting drugs on market.
Identification of Serotonin’s vascular properties
(publication year : 1912) as an ‘adrenaline mimicking
substance’ without attempt to isolate it) by O'Connor preceded
the discovery of Serotonin in the gastrointestinal tract by
Erspamer (1937) & in Blood by Rapport (1948,1949), Who
identified it’s structure as 5-HT [1949].
4. History of Serotonin
1932 - Bayliss, Ogden
“Vasotonins”- Can be removed by interposing lungs
1946-1949 - Joint work of Page, Green, Rapport.
1951 - Hamlin, Fischer (Synthesis of Serotonin)
1953 - Twarog, Page (Serotonin in Human brain)
1956 - Bogdanski, Pletcher, Brodie, Udenfriend
First identification of Serotonin in the brain
by fluorescence.
1957 - Serotonin as chemical mediator.
1979 - Peroutka, Snider
Radioligand binding technology
5HT1, 5HT2 binding sites.
5. Serotonin Acts As :-
• Neurotransmitter
• Local Hormone
• Component of platelet clotting process
• Role in migraine (Headache)
• Mediator of Signs & Symptoms of Carcinoid
syndrome (carcinoid Tumor)
(Serotonin antagonists as TREATMENT)
6. 5-HYDROXYTRYPTAMINE (5HT, Serotonin)
Synonyms :-
5-HT,
5-Hydroxytryptamine,
Enteramine,
Thrombocytin,
3-(β-Aminoethyl)-5-
hydroxyindole,
Thrombotonin
Chemical Formula :- C10H12N2O
Approximately 90% of Human body’s total serotonin is located in the
enterochromaffin cells in the GI tract, where it is used to regulated
intestinal movements.
7. 1.) Serotonin was the name given to the
vasoconstrictor substance which appeared in serum
when blood clotted & Enteramine to the Smooth
muscle.
2.) In the early 1950’s both were shown to be
5-hydroxytryptamine (5HT).
3.) About 90% of body’s Content of 5-HT localized in
the intestines; most of the rest is in platelets &
brain.
4.) It is also found in wasp (Flying insect) & Scorpion
sting & widely distributed in invertebrates & plants
(banana, pear, pineapple, tomato, stinging nettle,
cowage).
9. 1.) 5-Hydroxytryptamine β-aminoethyl-5-
hydroxyindole.
2.) It is Synthesized from the amino acid
tryptophan & degraded primarily by MAO & to
a small extent by a dehydrogenises.
3.) The decarboxylase is non-specific, acts on
DOPA as well as 5-HTP to produce NA and 5-
HT respectively.
11. - Cells lining the gastrointestinal tract release
serotonin when damaged by Chemotherapy and Radiation therapy.
This Serotonin binds to Serotonin receptors on nerves that transmit
impulses to turn stimulates other nerves involved in the vomit
reflex. 5-HT3 receptor antagonists prevents serotonin from binding
to 5-HT3 receptors in the small intestine thereby reducing the
likelihood of nausea & vomiting. The way 5-HT3 receptor
antagonists work to prevent postoperative nausea &vomiting is less
well understood.
- Vomiting & nausea are brought about by a
complex pathway that involves several steps. Ultimately this
pathway involves activation of an area within the brain known as
the “vomiting centre”. This centre is responsible for co- ordinating
signals from the body, processing them, & activating the vomiting
reflex. The vomiting centre receives signals from different parts of
the brain, including the balance centre, in addition to the stomach
& throat.
13. 1.) Gaddum & Picarelli (1957) Classified 5-HT receptors
into musculatropic (D type) Neurotropic (M type).
2.) Four Families of 5-HT receptors (5-HT1, 5-HT2, 5-HT3,
5-HT4-7).
3.) All 5-HT receptors (except 5-HT3) are G protein
Couples receptors which function through decreasing
(5-HT1) or increasing (5-HT4, 5-HT6, 5-HT7).
- Based on biochemical & pharmacological
Criteria, Serotonin receptors are classified into seven
main receptor subtypes 5-HT1-7.
- Major pharmacotherapeutic importance are
those designated 5-HT1, 5-HT2, 5-HT4 & 5-HT5-7. All
which are G-protein-Coupled where as the 5-HT3
subtypes represents a ligandgated ion channel.
14. Drug acting on Serotonergic
Neurotransmission :-
- The Figure above depicts how Serotonin
neurotransmission may be modified at the presynaptic level by
inhibiting degradation storage or reuptake.
15. 5-HT1 Receptors
1.) Five Subtypes (5-HT1A,B,D,E,F) have been identified.
2.) The 5-HT1C receptor is now designated 5-HT2C.
3.) All Subtypes of 5-HT1 receptor inhibits
adenylcyclase.
4.) The Most important location of 5-HT1A receptor are
Raphe Nuclei of brain stem & hippocampus.
5-HT1 Receptors Agonists
The 5-HT1 receptors agonists are a subfamily of the 5-
HT Serotonin receptors that binds to the endogenous
neurotransmitter Serotonin.
16. - Mediate inhibitory neurotransmission, including 5-
HT1A, 5-HT1B, 5-HT1D, 5-HT1E & 5-HT1F.
- There is no 5-HT1C receptors, as it was reclassified as
the, 5-HT2C receptor.
5-HT1AAgonists :-
Busirone is a partial 5-HT1A agonist used
clinically for the treatment of anxiety & depression.
5-HT1B & 5-HT1D Agonists :-
The ‘Triptans’ are as drug
class useful as abortive medication for the treatment of acute migraine
headaches.
They are very effective
medication that bind to 5-HT1B & 5-HT1D receptors in cranial vessels
which leads to vasoconstriction & decreased releases of nuropeptides
involved in ‘Sterile Inflammation’.
17. 5-HT2 Receptors
1.) There are 3 Subtypes of 5-HT2 receptors; all are
coupled to phospholipids C.
2.) 5-HT2A receptor also inhibits K+ Channels resulting
is slow depolarization of neurons.
5-HT2C Agonist
Trazodone was previously believed to be a 5-HT2C
receptor antagonist. However, recent publications
report that trazodone would behave as a 5-HT2C
agonist. This drug is used generally as Somnorific.
19. 5-HT3 Receptor
The 5-
Hydroxytryptamin
e3 (5-HT3)
receptor is a
member of the
cys-loop family of
legend gated ion
channels, of which
the nicotinic
acetylcholine
receptor is the
prototype.
Fig.1 :- Representative traces of
inward currents evoked by
25mM 5-HT in mouse
5-HT3A & 5-HT3A/B receptors.
20. 1.) This is the neuronal 5-HT receptor which rapidly
depolarize nerve ending by opening the cation
channel located within it.
2.) Somatic & autonomic nerve endings pain, itch,
coronary chemo reflux, Fall in BP due to
withdrawal of sympathetic tone.
3.) Nerve endings in myentaic plexus
augmentation of peristalsis, emetic reflux.
4.) Area postrema & nucleus tracts solitaries in brain
stem nausea, vomiting.
5-HT3 Antagonists :-
This class included drugs such as
Ondansetron, palonosetron & others. There agents are
particularly useful in the treatment of chemotherapy induced
nausea & vomiting(CINV).
21. 5-HT4-7 Receptors
5-HT4 Agonist :-
Cisapride is a Serotonin and cholinergic
agonist used as a prokinetic drug. Its was withdrawn from
the U.S. market because of cardiovascular toxicity.
1.) The 5-HT4 receptor has been demonstrated in the
mucosa, plexuses & smooth muscle of Gut
probably involved in augmenting intestinal secretion
& peristalsis.
2.) It is also located in brain.
22. Reference :-
• https://www.myvmc.com/treatments/5-ht3-receptor-antagonists-serotonin-
blockers/
• (Date :- 08/11/2017 Time :- 5.23pm)
• http://pharmacologycorner.com/serotonin-5ht-receptors-agonists-antagonist/
• (Date :- 08/11/2017 Time :- 9.30pm)
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3103470/
• (Date :- 09/11/2017 Time :- 7.30am)
• Essential of Medical Pharmacology
By K.D. Tripathi
5th edition, 2003
Reprint – 2004
Page no. : 145 to 155
