Effect of BM-5, a presynaptic antagonist-postsynaptic agonist, on cortical acetylcholine release.
The effect of N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl) acetamide (BM-5) on acetylcholine release from the cerebral cortex was investigated in unanaesthetized and urethane-anaesthetized rats. BM-5 at doses ranging from 0.3 to 5 mg/kg i.p. enhanced acetylcholine output in both groups of rats. The maximum increase occurred with 0.5 mg/kg in the unanaesthetized and 2 mg/kg in the anaesthetized rats. The effect lasted approximately 60 min. At the largest doses peripheral muscarinic effects including salivation, chromodachryorrhea and rhinorrhea were also seen. These results demonstrate that BM-5 exerts presynaptic antagonistic and postsynaptic agonistic effects on muscarine receptors in vivo also.
D000109:Acetylcholine / Q000378:metabolism*; D000758:Anesthesia; D000818:Animals; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism*; D008297:Male; D010277:Parasympathomimetics / Q000494:pharmacology*; D011759:Pyrrolidines / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D017981:Receptors, Neurotransmitter / Q000187:drug effects* / Q000378:metabolism; D012472:Salivation / Q000187:drug effects
D010277:Parasympathomimetics; D011759:Pyrrolidines; D017981:Receptors, Neurotransmitter; C038672:N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide; D000109:Acetylcholine