Irreversible α adrenoceptor blocking effects and reversible muscarinic blocking and nicotinic blocking effects of tetramine disulfides on the heart

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Abstract
Inotropic effects of phenylephrine, carbachol and butyrylcholine were used in the rabbit left atrium to evaluate, respectively, .alpha.-adrenoceptor blocking, muscarinic blocking and nicotinic blocking effects of tetramine disulfides ((RNH(CH2)nNH(CH2)2S-)2 .cntdot. 4HX). The .alpha.-adrenoceptor blocking potencies of newly synthesized derivatives R = 3'',4''-(OH)2-benzyl, n = 5-9, were similar to those of compounds R = 2''-OCH3-benzyl, n = 5-7. Muscarinic blocking and nicotinic blocking potencies of tetramine disulfides were correlated with .alpha. adrenoceptor blocking potency. Compounds R = 3'',4''-(OH)2-benzyl had relatively low muscarinic blocking potencies and compounds R = 2''-OCH3-benzyl had relatively low nicotinic blocking potencies.