Abstract
Optical isomers of YM-12617, a potent and selective alpha! -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.
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