Synthesis and evaluation of vasoconstrictor and vasorelaxant activity of norbormide isomers

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.