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Affinity and efficacy correlate with chemical structure more than potency does in a series of pentatomic cyclic muscarinic agonists
Author(s) -
Angeli P.,
Brasili L.,
Giannella M.,
Gualtieri F.,
Pigini M.
Publication year - 1985
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1985.tb11076.x
Subject(s) - potency , muscarinic acetylcholine receptor , chemistry , endocrinology , agonist , medicine , muscarinic agonist , guinea pig , pharmacology , stereochemistry , biochemistry , receptor , in vitro
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.