Presynaptic antagonist-postsynaptic agonist at muscarinic cholinergic synapses. N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.
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.
D000109:Acetylcholine / Q000378:metabolism; D000818:Animals; D001667:Binding, Competitive; D006152:Cyclic GMP / Q000096:biosynthesis; D006168:Guinea Pigs; D006624:Hippocampus / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D008214:Lymphocytes / Q000187:drug effects / Q000378:metabolism; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D010276:Parasympatholytics; D010277:Parasympathomimetics; D011759:Pyrrolidines / Q000494:pharmacology*; D011813:Quinuclidinyl Benzilate / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D013569:Synapses
D010276:Parasympatholytics; D010277:Parasympathomimetics; D011759:Pyrrolidines; D011813:Quinuclidinyl Benzilate; C038672:N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide; D006152:Cyclic GMP; D000109:Acetylcholine