A difference in mode of antagonism between optical isomers of a potent selective alpha1-adrenoceptor blocker (YM-12617) and norepinephrine in isolated rabbit iris dilator and aorta.

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概要

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• Optical isomers of YM-12617, a potent and selective alpha<SUB>1</SUB> -adrenoceptor blocker, were tested on the rabbit iris dilator and aorta. The order of potency was R(-)- isomer>racemate>S(+)-isomer. The R(-)-isomer and racemate behaved as an essentially irreversible antagonist to norepinephrine in the iris dilator where the efficacy of norepinephrine was small, although the S(+)-isomer was a competitive antagonist. These drugs behaved as a competitive antagonist of norepinephrine in the aorta where the efficacy of norepinephrine was large.

著者

• Takayanagi Issei

  Department Of Chemical Pharmacology Faculty Of Pharmaceutical Sciences University Of Tokyo:(correspo

• Furukawa Akira

  Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences

• Kameda Hiroyuki

  Department Of Transportation Engineering Kyoto University

• KONNO FUKIO

  Department of Biology, Faculty of Science, Kobe University

• KUBO Haruichi

  Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences

• TOYODA Toshie

  Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences

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