EFFECTS OF A NEW CHOLINOLYTIC DRUG OF TROPANES AND ITS OPTICAL ISOMERS ON CENTRAL MUSCARINIC AND NICOTINIC RECEPTORS

2 pha-(2',2'-disubstituted-2'-hydroxy-ethoxy)tropane (2 alpha-DHET), a new cholinolytic, is a racemic tertiary amine with two chiral carboni c atoms. It has four optical isomers whose absolute configurations are 1R-2 alpha-2'S, 1R-2 alpha-2'R, 1S-2 alpha-2'R and 1S-2 alpha-2'S. Th ese compounds showed both antimuscarinic and antinicotinic activity, b locking both muscarinic and nicotinic receptors. Central muscarinic re ceptors, rather than nicotinic receptors, have a stereoselective speci ficity to these compounds. The 2'R configurations are more suitable to the stereostructure of the binding site of muscarinic receptors than the 2'S configuration. (C) 1995 The Italian Pharmacological Society