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Science 4 August 1989:
Vol. 245. no. 4917, pp. 486 - 493
DOI: 10.1126/science.2569237
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Articles

Science, Vol 245, Issue 4917, 486-493
Copyright © 1989 by American Association for the Advancement of Science

articles

Drugs from emasculated hormones: the principle of syntopic antagonism

J Black

Department of Analytical Pharmacology, Rayne Institute, King's College Hospital School of Medicine and Dentistry, London, United Kingdom.

This lecture illustrates the early stages in the planning and discovery of propranolol, an adrenaline beta-adrenergic receptor antagonist, and cimetidine, a histamine H2-receptor antagonist--the first examples of clinically useful drugs from each of these classes. The significance of selective agonists, partial agonists, and syntopic antagonists and the importance of the bioassay and the use of molar models in the drug discovery process are discussed. For the future, an outline of potential developments in hormone-receptor concepts is offered leading to the conclusion that progress may depend on improvements in bioassays and related molar modeling.


THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
A Novel Mechanism of G Protein-coupled Receptor Functional Selectivity: MUSCARINIC PARTIAL AGONIST McN-A-343 AS A BITOPIC ORTHOSTERIC/ALLOSTERIC LIGAND.
C. Valant, K. J. Gregory, N. E. Hall, P. J. Scammells, M. J. Lew, P. M. Sexton, and A. Christopoulos (2008)
J. Biol. Chem. 283, 29312-29321
   Abstract »    Full Text »    PDF »
ACCELERATED COMMUNICATION: Influence of G Protein Type on Agonist Efficacy.
Q. Yang and S. M. Lanier (1999)
Mol. Pharmacol. 56, 651-656
   Abstract »    Full Text »


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