Abstract:
The rat toxicant norbormide, was synthesized and six stereoisomers of norbormide were isolated and purified by chromatography in order to undertake structure-activity relationship studies with respect to vasorelaxant and vasoconstrictor properties. Isomers V, W and Y behave qualitatively like the isomeric mixture of norbormide isomers showing either vasoconstrictor or vasorelaxant activities. Isomers X and R exhibit vasorelaxant effects only. These results indicate that the selective vasoconstrictor effect is stereospecific thereby suggesting the existence of a norbormide-specific receptor.