Abstract
A series of new derivatives, related to diphenidol and to its 2-carbonyl analogue, were designed as antimuscarinic agents. The synthesized compounds were evaluated both as hydrochlorides and as methiodides by functional tests at guinea-pig heart (M(2)), guinea-pig ileum (M(3)) and rabbit vas deferens (putative M(4)). Two derivatives (3a and 5a) showed an M(3)-selective profile similar to that of the reference compounds, though they resulted less potent.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Guinea Pigs
-
Heart / drug effects
-
Heart / physiology
-
Ileum / drug effects
-
Ileum / physiology
-
In Vitro Techniques
-
Male
-
Muscarinic Antagonists / chemical synthesis*
-
Muscarinic Antagonists / pharmacology*
-
Muscle Contraction / drug effects
-
Muscle, Smooth / drug effects
-
Muscle, Smooth / physiology
-
Piperidines / chemical synthesis*
-
Piperidines / pharmacology*
-
Receptor, Muscarinic M2 / antagonists & inhibitors
-
Receptor, Muscarinic M3 / antagonists & inhibitors
-
Receptor, Muscarinic M4 / antagonists & inhibitors
-
Structure-Activity Relationship
-
Vas Deferens / drug effects
-
Vas Deferens / physiology
Substances
-
Muscarinic Antagonists
-
Piperidines
-
Receptor, Muscarinic M2
-
Receptor, Muscarinic M3
-
Receptor, Muscarinic M4
-
diphenidol