Affinity and efficacy correlate with chemical structure more than potency does in a series of pentatomic cyclic muscarinic agonists
Open Access
- 1 August 1985
- journal article
- research article
- Published by Wiley in British Journal of Pharmacology
- Vol. 85 (4) , 783-786
- https://doi.org/10.1111/j.1476-5381.1985.tb11076.x
Abstract
1 The efficacy and affinity of nine pentatomic cyclic muscarinic agonists were determined on the guinea-pig ileum, according to the method of Furchgott & Bursztyn (1967). 2 The efficacy and affinity of these agonists are affected differently by structural modifications. 3 Our results suggest that a strong dipole oriented in the same direction as that of the hydroxy group of muscarine, or the presence of a polarizable atom in the same position, are important for efficacy.This publication has 11 references indexed in Scilit:
- DETERMINATION OF DISSOCIATION-CONSTANTS AND RELATIVE EFFICACIES OF OXOTREMORINE ANALOGS AT MUSCARINIC RECEPTORS IN THE GUINEA-PIG ILEUM BY PHARMACOLOGICAL PROCEDURES1984
- The relative contribution of affinity and efficacy to agonist activity: organ selectivity of noradrenaline and oxymetazoline with reference to the classification of drug receptorsBritish Journal of Pharmacology, 1984
- AFFINITY, EFFICACY, AND STEREOSELECTIVITY OF OXOTREMORINE ANALOGS FOR MUSCARINIC RECEPTORS IN THE ISOLATED GUINEA-PIG ILEUM1983
- Benzilycholine mustard and spare receptors in guinea pig ileumLife Sciences, 1982
- Relation between structure and cholinergic activity. II. Synthesis and muscarinic activity of some sulfur analogs of 2-methyl-4-trimethylammoniomethyl-1,3-dioxolane-iodide.1975
- 1 Stereochemical Aspects of Parasympathomimetics and their Antagonists: Recent DevelopmentsProgress in Medicinal Chemistry, 1975
- STEREOSPECIFICITY IN THE REACTIONS OF CHOLINESTERASE AND THE CHOLINERGIC RECEPTORAnnals of the New York Academy of Sciences, 1967
- COMPARISON OF DISSOCIATION CONSTANTS AND OF RELATIVE EFFICACIES OF SELECTED AGONISTS ACTING ON PARASYMPATHETIC RECEPTORS*Annals of the New York Academy of Sciences, 1967
- A MODIFICATION OF RECEPTOR THEORYBritish Journal of Pharmacology and Chemotherapy, 1956