Specificity in the Pharmacological Actions of Optical Isomers of cis-2,3-Dihydro-3-(4-methylpiperazinylmethyl)-2-phenyl-1,5-benzothiazepin-4(5H)-one (BTM)(Pharmacological)

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The pharmacological actions of the optical isomers of cis-2,3-dihydro-3-(4-methylpiperazinylmethyl)-2-phenyl-1,5-benzothiazepin-4(5H)-one (BTM) were studied and compared. Antiacetylcholine activity determined by the Magnus method was higher but antihistamine activity was lower with the (-)-compound than with the (+)-cornpound; the (±)-compound showed intermediate activities. The antiulcer action and antisecretory action in pylorus-ligated rats as well as the antistress ulcer action in mice were more potent with the (-)-compound than the (+)-compound. The optical isomers showed similar local anesthetic action, when tested by using the corneal reflex in guinea pigs. Analgesic action, tested by the acetic acid-induced writhing method, was observed with the (+)-compound, but not the (±)- or (-)-compound. The (+)-compound showed the strongest acute toxicity in mice, followed by the (±)- and the (-)-compounds in that order. These results suggest the presence of multiple targets for the various pharmacological activities. The (-)-compound appears to be more promising as an antiulcer agent, since the antiulcer effect was greater and the toxicity was milder as compared with (+)-compound.
公益社団法人日本薬学会の論文
1987-08-25