Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site

Abstract
A conformation-activity relationship study of 5-HT3 receptor antagonists was used to define a pharmacophore and receptor map to qualitatively account for their activity. The design and synthesis of specific keto-amino-indole derivatives that are potent 5-HT3 receptor antagonists gave some support to the model.

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