RT Journal Article
SR Electronic
T1 Presynaptic antagonist-postsynaptic agonist at muscarinic cholinergic synapses. N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.
JF Molecular Pharmacology
JO Mol Pharmacol
FD American Society for Pharmacology and Experimental Therapeutics
SP 1
OP 5
VO 24
IS 1
A1 Nordström, O
A1 Alberts, P
A1 Westlind, A
A1 Undén, A
A1 Bartfai, T
YR 1983
UL http://molpharm.aspetjournals.org/content/24/1/1.abstract
AB 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.