Synthesis and pharmacological evaluation of a new class of 2-oxo-8-azaspiro (4,5)decan-1-ones as analogues of the muscarinic agonist RS-86.
A new series of 8-substituted-2-oxo-8-azaspiro (4,5)decan-1-ones has been synthesized and compounds tested for their cholinergic properties in comparison with the muscarinic agonist RS-86. Preliminary in vitro and in vivo pharmacological data indicate that none of them is provided with significant cholinergic effects either at central or peripheral level. A possible explanation for the lack of activity is given on the basis of conformational studies.
Cignarella
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Istituto di Chimica Farmaceutica e Tossicologica, Università di Milano, Italy.
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D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D002415:Cats; D006168:Guinea Pigs; D007651:Keto Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D051379:Mice; D008958:Models, Molecular; D010277:Parasympathomimetics / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D013388:Succinimides / Q000138:chemical synthesis / Q000494:pharmacology*
D007651:Keto Acids; D010277:Parasympathomimetics; D013141:Spiro Compounds; D013388:Succinimides; C001886:2-ethyl-8-methyl-2,8-diazaspiro(4,5)decane-1,3-dione