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Document
Document

... How do the different routes of administration affect plasma levels of cocaine? Cocaethylene How does cocaine work at the synapse (make sure to include NTs and relative affinities)? Cocaine psychosis Self administration of cocaine (generalization to other drugs)? Explain the significance of generaliz ...
Lecture 05 - binding quant - Cal State LA
Lecture 05 - binding quant - Cal State LA

... (theoretically, KD = EC50), it does not account for agonists that do not produce the maximum effect. Modified occupancy theory: modified to separate the binding affinity from the intrinsic activity () of the compound. That is, a compound can bind tightly, but cause a little or no effect. ...
Pharmacodynamics
Pharmacodynamics

... Pharmacodynamics relates to drugs binding to receptors and their effects. ...
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... Social Fund, within the framework of " Practice-oriented, student-friendly modernization of the biomedical education for strengthening the international competitiveness of the rural Hungarian universities " ...
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receptors

... influencing one another via the interplay of hundreds of neurotransmitters and their receptors, which in turn influence the passage of electrically charged particles across the nerve cell membrane.” ...
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... L-type Ca++ channel antagonists ACE inhibitors ATII-R antagonists Organic nitrates (NO) Nitroprusside… 18) Glitazones and sulfonylureas have been used for many years as oral antidiabetic drug. However, in recent years several novel concepts in the treatment of diabetes have emerged. Describe two dis ...
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... Ca2+ Diacylglycerol IP3 cAMP cGMP Protein kinases Third messengers ...
Pharmacology Ch 10 132-142 Adrenergic Pharmacology
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... and therefore preventing a second messenger being produced; or May interfere with gene expression as modulated by protein kinase C, regulating growth factors and ...
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... all three opiate receptors: mu, kappa and delta. These unique ligands have high binding affinity at all three opioid receptors and more balanced receptor activity than other opioids, with partial agonist / antagonist activity at mu, somewhat higher, but not full, kappa agonist activity, and moderate ...
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... the presence of angiotensin II and is reduced in the presence of non-selective AII receptor antagonists that block both AT1 and AT2 receptor subtypes (eg saralasin). AT1-selective antagonists have also been studied in this model, at pharmacologically relevant doses. The AT1 blocker eprosartan reduce ...
Cannabis (1)
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... Obesity is characterized by an abnormal accumulation of body fat, usually 20 percent or more over an individual's ideal body weight. Obesity results when the size or number of fat cells in a person's body increases. When a person gains weight, these fat cells first increase in size and later in num ...
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A1992HC31200002
A1992HC31200002

... effects. A unique regional distribution of the sttes was also described. Taken together, the data suggested that the unique anesthetic and psychotomimebc properties of PCP-like drugs are mediated at specific PCP receptors. The observation that a benzomorphan’o opiate, Kallyl normetazocine (SKF-10047 ...
Slide ()
Slide ()

... A: The percentage of receptor occupancy resulting from full agonist (present at a single concentration) binding to receptors in the presence of increasing concentrations of a partial agonist. Because the full agonist (filled squares) and the partial agonist (open squares) compete to bind to the same ...
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Cannabinoid receptor antagonist



The discovery of the endogenous cannabinoid system led to the development of CB1 receptor antagonists. The first cannabinoid receptor antagonist, rimonabant, was described in 1994. Rimonabant blocks the CB1 receptor selectively and it has been shown to decrease food intake and regulate body-weight gain. The prevalence of obesity worldwide is increasing dramatically and has a great impact on public health. The lack of efficient and well-tolerated drugs to cure obesity has led to an increased interest in research and development of cannabinoid antagonists. Cannabidiol, a naturally occurring cannabinoid, is a non-competitive CB1/2 antagonist.
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