A series of ether derivatives of deoxamuscarine were synthesized and tested for muscarinic activity on guinea-pig hean, ileum, and bladder. The resulu show that: a) The innoduction of the benzyl group generates an agonist which is 5-fold more potent and IO-fold more selective than deoxamuscarine on ileum. Thii selectivity is ascrihed to an increase of efficacy. b) Affinity and efficacy are differently affected by the substituents studied. C) The so-called muscarinic subsite interacting with the hydroxy group of muscaxine-like compounds may accommodate bulky substituenis, and on the basis of this new functionalized congeners may be designed with a view to achieving more potent and more selective muscarinic ligands.
Effect of Deoxamuscarine Etherification on M2 and M3 Muscarinic Affinity and Efficacy
TAYEBATI, Seyed Khosrow
1992-01-01
Abstract
A series of ether derivatives of deoxamuscarine were synthesized and tested for muscarinic activity on guinea-pig hean, ileum, and bladder. The resulu show that: a) The innoduction of the benzyl group generates an agonist which is 5-fold more potent and IO-fold more selective than deoxamuscarine on ileum. Thii selectivity is ascrihed to an increase of efficacy. b) Affinity and efficacy are differently affected by the substituents studied. C) The so-called muscarinic subsite interacting with the hydroxy group of muscaxine-like compounds may accommodate bulky substituenis, and on the basis of this new functionalized congeners may be designed with a view to achieving more potent and more selective muscarinic ligands.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
