ChemInform Abstract: Effect of Deoxamuscarine Etherification on M2 and M3 Muscarinic Affinity and Efficacy.
Abstract
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ChemInform Abstract
In view of the interest in structure-activity relationship of different receptor subtypes, a series of known and newly synthesized ( e.g. (Ic)) ether derivatives of deoxamuscarine (Ia) are tested for muscarinic activity on guinea-pig heart, ileum, and bladder. The results show that introduction of the benzyl group generates an agonist which is 5-fold more potent and 10-fold more selective than ( Ia) on ileum. However, replacement of the hydrogen atom of the hydroxy group by a larger group effects affinity and efficacy differently. The results are used as basis for designing new functionalized congeners for preparing more potent and selective muscarinic ligands.
