Dialkylaminoalkyl esters of 2,2-diphenyl-2-alkylthioacetic acids: a new class of potent and functionally selective muscarinic antagonists.

Abstract The synthesis and pharmacological activity as muscarinic antagonists of a number of 2-alkylthio-2,2-diphenylacetic acid esters are reported. The compounds studied are potent muscarinic antagonists and many of them show from moderate to high selectivity toward M 2 or toward M 1 and M 2 receptors when tested on tissues but lack selectivity on five muscarinic human receptors (m1–m5) cloned and expressed in CHO-K1 cells. As a consequence, the compounds behave as functionally selective antagonists. Those showing M 2 selectivity appear to be good drug candidates for the treatment of cognitive disorders connected with central cholinergic deficit.