MolPharm xPharm- The Comprehensive Pharmacology Reference

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text (PDF)
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Pennefather, P.
Right arrow Articles by Quastel, D. M.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Pennefather, P.
Right arrow Articles by Quastel, D. M.

Modification of dose-response curves by effector blockade and uncompetitive antagonism

P Pennefather and DM Quastel

Kinetic equations were derived for simple models of agonist-antagonist- receptor interaction and used to predict theoretical dose-response curves for the situation where there exists "receptor reserve" and a simple rectangular hyperbolic relation between tissue response and receptor occupancy by agonist, generated by an "effector chain" that links final response to receptor activation. Drug action within this chain, or an "uncompetitive" antagonism exerted by a reversible agonist that combines primarily with the active agonist-receptor complex, may give the appearance of classical noncompetitive or competitive antagonism, depending upon the amount of receptor reserve and upon the rate constants involved in both agonist-receptor and antagonist- receptor interaction. The apparent potency and nature of antagonism by such an uncompetitive antagonist may depend upon the particular agonist against which it is tested. The phenomenon whereby true competitive antagonists reduce the maximal response to a partial agonist can be explained if the partial agonist, in addition to activating receptors, also acts as an uncompetitive antagonist.

Volume 22, Issue 2, pp. 369-380, 09/01/1982
Copyright © 1982 by American Society for Pharmacology and Experimental Therapeutics




This article has been cited by other articles:


Home page
 Mol. Pharmacol.Home page
J. Y. T. Yeung, K. J. Canning, G. Zhu, P. Pennefather, J. F. MacDonald, and B. A. Orser
Tonically Activated GABAA Receptors in Hippocampal Neurons Are High-Affinity, Low-Conductance Sensors for Extracellular GABA
Mol. Pharmacol., January 1, 2003; 63(1): 2 - 8.
[Abstract] [Full Text] [PDF]

Home page
 J. Neurosci.Home page
S. Mennerick, V. Jevtovic-Todorovic, S. M. Todorovic, W. Shen, J. W. Olney, and C. F. Zorumski
Effect of Nitrous Oxide on Excitatory and Inhibitory Synaptic Transmission in Hippocampal Cultures
J. Neurosci., December 1, 1998; 18(23): 9716 - 9726.
[Abstract] [Full Text] [PDF]


Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 1982 by the American Society for Pharmacology and Experimental Therapeutics