Orthosteric Drug Antagonism-6 (Article, 2006) [WorldCat.org]
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Orthosteric Drug Antagonism-6

Edition/Format: Chapter Chapter : English
Summary:
This chapter discusses the blockade of agonist-induced response through interaction with receptors. Antagonism can be classified operationally, in terms of the effects of antagonists on agonist dose-response curves, and mechanistically, in terms of the molecular effects of the antagonist on the receptor protein. When both the agonist and antagonist compete for a common binding site, the antagonism is termed  Read more...
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Details

ISBN: 978-0-12-370599-0
Publication:A Pharmacology Primer; 99-126; Elsevier Inc.
Language Note: English
Unique Identifier: 4934397076
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Abstract:

This chapter discusses the blockade of agonist-induced response through interaction with receptors. Antagonism can be classified operationally, in terms of the effects of antagonists on agonist dose-response curves, and mechanistically, in terms of the molecular effects of the antagonist on the receptor protein. When both the agonist and antagonist compete for a common binding site, the antagonism is termed competitive. The antagonism is quantified by measuring the ratio of equiactive concentrations of agonist measured in the presence of and absence of the antagonist. The model of simple competitive antagonism predicts that the slope of the Schild regression should be unity. It is found that if the slope of the regression is not unity or if the regression is not linear, then the complete data set cannot be used to estimate the antagonist potency. The model of simple competitive antagonism predicts parallel shifts of agonist dose-response curves with no diminution of maxima. It is found that the kinetics of offset of the antagonist from the receptor can dictate whether surmountable or insurmountable antagonism is observed.

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