cis(-)-2,3-Dihydro-3-(4-methylpiperazinylmethyl)-2-phenyl-1,5- benzothiazepin-4(5H)-one monohydrochloride and its butylbromide as M1-receptor antagonists.
Selectivity of cis(-)-2,3-dihydro-3-(4-methylpiperazinylmethyl)-2-phenyl-1,5-b enzothiazepin-4 (5H)-one monohydrochloride (BTM-1086) and its butylbromide (BTM-1073) to subtypes of muscarinic receptor, M1-and M2-receptors were tested, using pirenzepine, a M1-selective antagonist and atropine, a nonselective antagonist as reference drugs. Like pirenzepine, BTM-1086 and BTM-1073 were M1-selective antagonists. BTM-1086 was most selective among the test drugs. BTM-1073, a butylbromide of BTM-1086 was more potent than BTM-1086 in antimuscarinic activity tested on the isolated ileal longitudinal muscle, suggesting that quarternarization increased selectivity to M2-receptor but not to M1-receptor.
D000109:Acetylcholine / Q000037:antagonists & inhibitors; D000818:Animals; D001285:Atropine / Q000494:pharmacology; D001667:Binding, Competitive; D002540:Cerebral Cortex / Q000378:metabolism; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects / Q000378:metabolism; D010276:Parasympatholytics; D010890:Pirenzepine / Q000494:pharmacology; D011813:Quinuclidinyl Benzilate / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D011976:Receptors, Muscarinic / Q000145:classification / Q000187:drug effects*; D013841:Thiazepines / Q000494:pharmacology*
D010276:Parasympatholytics; D011976:Receptors, Muscarinic; D013841:Thiazepines; C051759:BTM 1073; D010890:Pirenzepine; D011813:Quinuclidinyl Benzilate; C029165:BTM 1042; D001285:Atropine; D000109:Acetylcholine