Opioid drugs like morphine produce their pharmacological effects like analgesia by acting on neuronal cell membrane receptors. Morphine was first isolated in 1804 and is used to treat dull constant pain. It causes side effects like euphoria, nausea, constipation and respiratory depression due to binding to mu, kappa and delta opioid receptors in the brain and spinal cord. Several morphine analogs were developed as drugs, including codeine, heroin, methadone, levorphanol, fentanyl, dipipanone, sufentanil and tapentadol, by modifying functional groups on morphine. These analogs have varying degrees of potency and side effect profiles compared to morphine.
Atropine is a core medicine in the World Health Organization's (WHO) "Essential Drugs List", which is a list of minimum medical needs for a basic health care system.
MORPHINE AS A LEAD DRUG MOLECULE COMPOUNDShikha Popali
THE ADDICTED DRUG MORPHINE AN ALKALOID USED TO TREAT SOME DISEASE , HERE WE HAVE ATTEMPT ALL DATA ITS STURECTURE MECHANISM OF ACTION, SAR AND APPLICATIONS.
morphine- an analgesic drug which is obtained from opium has several other analogues also. The presentation gives a brief and important information regarding morphine- cultivation, collection, presentation, it's chemical structure and therapeutic uses.
Alongwith it, the slides also gives a brief account of the structure and uses of its analogues such as heroine, codeine etc.
Atropine is a core medicine in the World Health Organization's (WHO) "Essential Drugs List", which is a list of minimum medical needs for a basic health care system.
MORPHINE AS A LEAD DRUG MOLECULE COMPOUNDShikha Popali
THE ADDICTED DRUG MORPHINE AN ALKALOID USED TO TREAT SOME DISEASE , HERE WE HAVE ATTEMPT ALL DATA ITS STURECTURE MECHANISM OF ACTION, SAR AND APPLICATIONS.
morphine- an analgesic drug which is obtained from opium has several other analogues also. The presentation gives a brief and important information regarding morphine- cultivation, collection, presentation, it's chemical structure and therapeutic uses.
Alongwith it, the slides also gives a brief account of the structure and uses of its analogues such as heroine, codeine etc.
Ephedra is mostly used to treat the human diseases like asthama and its excess amount cause many side effects in man.Most chemicals used in medicine mainly obtained from herbal plants.The main constituent that we obtain from ephedra is ephedrine.
General Anaesthesia (Medicinal Chemistry)Yogesh Tiwari
General anaesthetics are group of drugs that produces loss of consciousness, and therefore, loss of all sensations.
The absolute loss of sensation is termed as anaesthesia.
Ephedra is mostly used to treat the human diseases like asthama and its excess amount cause many side effects in man.Most chemicals used in medicine mainly obtained from herbal plants.The main constituent that we obtain from ephedra is ephedrine.
General Anaesthesia (Medicinal Chemistry)Yogesh Tiwari
General anaesthetics are group of drugs that produces loss of consciousness, and therefore, loss of all sensations.
The absolute loss of sensation is termed as anaesthesia.
Definition of the word DRUG & introduction to our YouTube channel 'About Drugs'
To watch the video: https://www.youtube.com/watch?v=m8h-C4gDaZ0&feature=youtu.be
Deep Behavioral Phenotyping in Systems Neuroscience for Functional Atlasing a...Ana Luísa Pinho
Functional Magnetic Resonance Imaging (fMRI) provides means to characterize brain activations in response to behavior. However, cognitive neuroscience has been limited to group-level effects referring to the performance of specific tasks. To obtain the functional profile of elementary cognitive mechanisms, the combination of brain responses to many tasks is required. Yet, to date, both structural atlases and parcellation-based activations do not fully account for cognitive function and still present several limitations. Further, they do not adapt overall to individual characteristics. In this talk, I will give an account of deep-behavioral phenotyping strategies, namely data-driven methods in large task-fMRI datasets, to optimize functional brain-data collection and improve inference of effects-of-interest related to mental processes. Key to this approach is the employment of fast multi-functional paradigms rich on features that can be well parametrized and, consequently, facilitate the creation of psycho-physiological constructs to be modelled with imaging data. Particular emphasis will be given to music stimuli when studying high-order cognitive mechanisms, due to their ecological nature and quality to enable complex behavior compounded by discrete entities. I will also discuss how deep-behavioral phenotyping and individualized models applied to neuroimaging data can better account for the subject-specific organization of domain-general cognitive systems in the human brain. Finally, the accumulation of functional brain signatures brings the possibility to clarify relationships among tasks and create a univocal link between brain systems and mental functions through: (1) the development of ontologies proposing an organization of cognitive processes; and (2) brain-network taxonomies describing functional specialization. To this end, tools to improve commensurability in cognitive science are necessary, such as public repositories, ontology-based platforms and automated meta-analysis tools. I will thus discuss some brain-atlasing resources currently under development, and their applicability in cognitive as well as clinical neuroscience.
This pdf is about the Schizophrenia.
For more details visit on YouTube; @SELF-EXPLANATORY;
https://www.youtube.com/channel/UCAiarMZDNhe1A3Rnpr_WkzA/videos
Thanks...!
Comparing Evolved Extractive Text Summary Scores of Bidirectional Encoder Rep...University of Maribor
Slides from:
11th International Conference on Electrical, Electronics and Computer Engineering (IcETRAN), Niš, 3-6 June 2024
Track: Artificial Intelligence
https://www.etran.rs/2024/en/home-english/
(May 29th, 2024) Advancements in Intravital Microscopy- Insights for Preclini...Scintica Instrumentation
Intravital microscopy (IVM) is a powerful tool utilized to study cellular behavior over time and space in vivo. Much of our understanding of cell biology has been accomplished using various in vitro and ex vivo methods; however, these studies do not necessarily reflect the natural dynamics of biological processes. Unlike traditional cell culture or fixed tissue imaging, IVM allows for the ultra-fast high-resolution imaging of cellular processes over time and space and were studied in its natural environment. Real-time visualization of biological processes in the context of an intact organism helps maintain physiological relevance and provide insights into the progression of disease, response to treatments or developmental processes.
In this webinar we give an overview of advanced applications of the IVM system in preclinical research. IVIM technology is a provider of all-in-one intravital microscopy systems and solutions optimized for in vivo imaging of live animal models at sub-micron resolution. The system’s unique features and user-friendly software enables researchers to probe fast dynamic biological processes such as immune cell tracking, cell-cell interaction as well as vascularization and tumor metastasis with exceptional detail. This webinar will also give an overview of IVM being utilized in drug development, offering a view into the intricate interaction between drugs/nanoparticles and tissues in vivo and allows for the evaluation of therapeutic intervention in a variety of tissues and organs. This interdisciplinary collaboration continues to drive the advancements of novel therapeutic strategies.
Nutraceutical market, scope and growth: Herbal drug technologyLokesh Patil
As consumer awareness of health and wellness rises, the nutraceutical market—which includes goods like functional meals, drinks, and dietary supplements that provide health advantages beyond basic nutrition—is growing significantly. As healthcare expenses rise, the population ages, and people want natural and preventative health solutions more and more, this industry is increasing quickly. Further driving market expansion are product formulation innovations and the use of cutting-edge technology for customized nutrition. With its worldwide reach, the nutraceutical industry is expected to keep growing and provide significant chances for research and investment in a number of categories, including vitamins, minerals, probiotics, and herbal supplements.
THE IMPORTANCE OF MARTIAN ATMOSPHERE SAMPLE RETURN.Sérgio Sacani
The return of a sample of near-surface atmosphere from Mars would facilitate answers to several first-order science questions surrounding the formation and evolution of the planet. One of the important aspects of terrestrial planet formation in general is the role that primary atmospheres played in influencing the chemistry and structure of the planets and their antecedents. Studies of the martian atmosphere can be used to investigate the role of a primary atmosphere in its history. Atmosphere samples would also inform our understanding of the near-surface chemistry of the planet, and ultimately the prospects for life. High-precision isotopic analyses of constituent gases are needed to address these questions, requiring that the analyses are made on returned samples rather than in situ.
Richard's aventures in two entangled wonderlandsRichard Gill
Since the loophole-free Bell experiments of 2020 and the Nobel prizes in physics of 2022, critics of Bell's work have retreated to the fortress of super-determinism. Now, super-determinism is a derogatory word - it just means "determinism". Palmer, Hance and Hossenfelder argue that quantum mechanics and determinism are not incompatible, using a sophisticated mathematical construction based on a subtle thinning of allowed states and measurements in quantum mechanics, such that what is left appears to make Bell's argument fail, without altering the empirical predictions of quantum mechanics. I think however that it is a smoke screen, and the slogan "lost in math" comes to my mind. I will discuss some other recent disproofs of Bell's theorem using the language of causality based on causal graphs. Causal thinking is also central to law and justice. I will mention surprising connections to my work on serial killer nurse cases, in particular the Dutch case of Lucia de Berk and the current UK case of Lucy Letby.
Cancer cell metabolism: special Reference to Lactate PathwayAADYARAJPANDEY1
Normal Cell Metabolism:
Cellular respiration describes the series of steps that cells use to break down sugar and other chemicals to get the energy we need to function.
Energy is stored in the bonds of glucose and when glucose is broken down, much of that energy is released.
Cell utilize energy in the form of ATP.
The first step of respiration is called glycolysis. In a series of steps, glycolysis breaks glucose into two smaller molecules - a chemical called pyruvate. A small amount of ATP is formed during this process.
Most healthy cells continue the breakdown in a second process, called the Kreb's cycle. The Kreb's cycle allows cells to “burn” the pyruvates made in glycolysis to get more ATP.
The last step in the breakdown of glucose is called oxidative phosphorylation (Ox-Phos).
It takes place in specialized cell structures called mitochondria. This process produces a large amount of ATP. Importantly, cells need oxygen to complete oxidative phosphorylation.
If a cell completes only glycolysis, only 2 molecules of ATP are made per glucose. However, if the cell completes the entire respiration process (glycolysis - Kreb's - oxidative phosphorylation), about 36 molecules of ATP are created, giving it much more energy to use.
IN CANCER CELL:
Unlike healthy cells that "burn" the entire molecule of sugar to capture a large amount of energy as ATP, cancer cells are wasteful.
Cancer cells only partially break down sugar molecules. They overuse the first step of respiration, glycolysis. They frequently do not complete the second step, oxidative phosphorylation.
This results in only 2 molecules of ATP per each glucose molecule instead of the 36 or so ATPs healthy cells gain. As a result, cancer cells need to use a lot more sugar molecules to get enough energy to survive.
Unlike healthy cells that "burn" the entire molecule of sugar to capture a large amount of energy as ATP, cancer cells are wasteful.
Cancer cells only partially break down sugar molecules. They overuse the first step of respiration, glycolysis. They frequently do not complete the second step, oxidative phosphorylation.
This results in only 2 molecules of ATP per each glucose molecule instead of the 36 or so ATPs healthy cells gain. As a result, cancer cells need to use a lot more sugar molecules to get enough energy to survive.
introduction to WARBERG PHENOMENA:
WARBURG EFFECT Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside.
Otto Heinrich Warburg (; 8 October 1883 – 1 August 1970) In 1931 was awarded the Nobel Prize in Physiology for his "discovery of the nature and mode of action of the respiratory enzyme.
WARNBURG EFFECT : cancer cells under aerobic (well-oxygenated) conditions to metabolize glucose to lactate (aerobic glycolysis) is known as the Warburg effect. Warburg made the observation that tumor slices consume glucose and secrete lactate at a higher rate than normal tissues.
Cancer cell metabolism: special Reference to Lactate Pathway
Morphine presentation
1.
2. Opioid drugs, typified by morphine, produce
their pharmacological actions, including
analgesia, by acting on receptors located on
neuronal cell membranes.
3. Morphine (1804):
Named after the Greek God, Morpheus (God of dreams)
Good for treating dull, constant pain rather than sharp, periodic pain.
Side effects:
-Excitation, Euphoria
-Nausea, Pupil constriction
-Constipation,
-Tolerance and Dependence,
-Depression of breathing.
4. Why it gives feelings of Euphoria and causes addiction?
There are different types of Opioid Receptors,
Its action depends on the type of receptor morphine binds to…
7. Now, Let’s see together the effect of masking or removing functional groups on
activity…
1- The Phenol Moiety:
Masking the phenol group resulted in decreased activity, thus it is crucial for
activity.
R=H Morphine
R=Me Codeine
Codeine 20% active (injected
peripherally)
0.1% active (injected into brain)
NMe
O
RO
HO
H
H
8. 2- The 6-alcohol:
•Activity increases due to reduced polarity
•Compounds cross the blood brain barrier more easily
•6-OH is not important for binding
NMe
O
HO
HO
NMe
O
HO
O
NMe
O
HO
9. R=Ac 6-Acetylmorphine
Increased activity (4x)
•Acetyl masks a polar alcohol group making it easier to cross BBB
•Phenol group is free and molecule can bind immediately
•Dependence is very high
•6-Acetylmorphine is banned in many countries
NMe
O
HO
RO
H
H
10. 3- The Double Bond at 7,8:
Dihydromorphine
Increased activity
The alkene group is not important to binding.
NMe
O
HO
HO
H
H
11. 4- The 3o
Amine:
No activity
Nitrogen is essential to binding.
CHMe
O
HO
HO
H
H
12. NR= NH Normorphine
Reduced activity (25%)
NR= N+Me2
No activity
•Normorphine is more polar and crosses the BBB slowly
•Note: R affects whether the analogue is an agonist (axial and reaching to agonist site) or an
antagonist (equatorial and reaching to antagonist site), rigidification could be applied to
stabilize such conformations.
•Optimum distance between 3
o
amine and phenyl ring is essential for activity.
NR
O
HO
HO
H
H
14. Morphine analogsavailable as drugs:
1- Codeine (1832):
How it’s related: Methyl ether of morphine.
Activity: 20% that of morphine.
Treats: Moderate pain, Coughs, diarrhea.
15. 2- Heroin (1874):
How it’s related: 3,6-diacetyl ester of morphine.
Activity: 2x that of morphine as it is easier to cross BBB.
Treats: Pain in terminally ill patients.
Side effects: Euphoria, addiction, tolerance.
16. 5- Methadone(1937):
How its related: Rings B,C,D,E opened.
Activity: Less than Morphine.
Used to: Treat addiction.
Advantages: Can be given orally, Less side effects.
17. 3- Levorphanol (1948):
How it’s related: Ether bridge removed.
Activity: 5x that of morphine.
Advantage: It can be taken orally, Lasts longer, Easier to synthesize.
Side effects: High toxicity, comparable dependence.
18. 4- Fentanyl (1960):
How it’s related: Rings B,C,D removed.
Activity: 100x that of morphine.
Advantages: Cross BBB efficiently, Really easy to make, Rapid onset, short
duration, Can be administered any route (IV, oral, transdermal, buccal).
Used for: Anesthesia and Chronic pain management
Side effects: Sudden respiratory depression, More addictive than heroin, Less
euphoria, more sedation.
19. 8- Dipipanone (1970):
How it’s related: Rings B,C,D opened.
Activity: Similar to morphine.
Used for: Patients allergic to morphine.
Side effects: Sudden respiratory depression, risk of abuse.
20. 6- Sufentanil (1974):
How it’s related: Rings B,C,D removed.
Activity: 500x that of morphine
Advantages: Strongest Pain killer available for humans.
Used for: in surgery and post-operative pain management for patients that are
heavily Opioid tolerant because of long term opiate use.
Side effects: Sudden respiratory depression, anaphylaxis in rare cases.
21. 7-Tapentadol (2008):
How it’s related: Rings B,C,D removed.
Activity: Weak μ agonist and inhibit the reuptake of norepinephrine (similar to
Tramadol).
Advantages: Less side effects.
Used for: Indicated for controlling the pain of diabetic neuropathy.
Side effects: Dependence and addiction.
22. References:
1-The Annals of Pharmacotherapy: Overview of Oral Modified-Release Opioid Products for the Management of
Chronic Pain, by: Celene M. Amabile, Bill J. Bowman.
2- Bioorganic & Medicinal Chemistry: Design, synthesis, and structure–activity relationship of novel opioid κ-
agonists, by: Koji Kawai et al.
3- Indian J Anaesth.: Sufentanil Vs Fentanyl for Fast-Track Cardiac Anaesthesia, by: C M Deshpande et al.
4- Expert Opinion on Pharmacotherapy: Mechanistic and functional differentiation of tapentadol and tramadol, by:
Robert B Raffa, Helmut Buschmann.