Affinity and efficacy correlate with chemical structure more than potency does in a series of pentatomic cyclic muscarinic agonists.
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). The efficacy and affinity of these agonists are affected differently by structural modifications. 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.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D008297:Male; D008433:Mathematics; D009116:Muscarine / Q000031:analogs & derivatives / Q000494:pharmacology; D010277:Parasympathomimetics / Q000494:pharmacology*
D010277:Parasympathomimetics; C002394:muscarone; D009116:Muscarine