SYNTHESIS, BIOLOGICAL IN-VITRO EVALUATION AND STEREOSELECTIVITY OF ONDANSETRON ANALOGS - NOVEL 5-HT2A RECEPTOR ANTAGONISTS

The tetrahydrocarbazolone moiety of the 5-HT3 receptor antagonist onda nsetron has been combined with molecular fragments of typical 5-HT2A r eceptor ligands. Several of the resulting compounds are potent 5-HT2A antagonists. The antipodes of the most potent compound, a N-substitute d 4-(4-fluorobenzoyl)piperidine, are analogues of ketanserin which dis play a high degree of stereoselectivity at 5-HT2A receptors (148:1).