Synthesis and muscarinic activity of some muscarone analogs.
The synthesis of some muscarone analogs has been accomplished and their muscarinic activity has been assayed in three in vitro functional tests. The results of such an investigation put in evidence the active role played by the methylene moiety, placed exocyclic to the pentaatomic ring, on the interaction of the ligands with the different muscarinic receptor subtypes. Worth noting is the ileum-atria selectivity displayed by methylene derivative 7.
De Micheli
C
C
Dipartimento di Scienze Farmaceutiche dell'Università, Piazzale Europa, Trieste.
De Amici
M
M
Grana
E
E
Zonta
F
F
Giannella
M
M
Piergentili
A
A
D000818:Animals; D006168:Guinea Pigs; D006325:Heart Atria; D007082:Ileum; D007583:Jejunum; D008297:Male; D009116:Muscarine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects; D010277:Parasympathomimetics / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D011976:Receptors, Muscarinic / Q000187:drug effects
D010277:Parasympathomimetics; D011976:Receptors, Muscarinic; C002394:muscarone; D009116:Muscarine