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Presynaptic antagonist-postsynaptic agonist at muscarinic cholinergic synapses. N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide

O Nordstrom, P Alberts, A Westlind, A Unden and T Bartfai

A muscarinic cholinergic ligand, N-methyl-N-(1-methyl-4-pyrrolidino-2- butynyl)-acetamide (Compound BM-5), was shown to act simultaneously as a presynaptic antagonist and as a postsynaptic agonist at peripheral and central muscarinic synapses. In the presence of eserine it enhanced release of [3H]acetylcholine evoked by electrical stimulation in the guinea pig ileum longitudinal muscle myenteric plexus preparation. It also enhanced the release of [3H]acetylcholine evoked by potassium (25 mM) from rat hippocampal slices. It contracted the ileum and stimulated the synthesis of cyclic guanosine 3',5'-monophosphate in rat hippocampal slices and in human lymphocytes in a manner similar to the muscarinic agonist oxotremorine. This effect of BM-5 could be blocked by atropine.

Volume 24, Issue 1, pp. 1-5, 07/01/1983
Copyright © 1983 by American Society for Pharmacology and Experimental Therapeutics






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