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

M F Hibert; R Hoffmann; R C Miller; A A Carr

doi:10.1021/jm00168a011

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

J Med Chem. 1990 Jun;33(6):1594-600. doi: 10.1021/jm00168a011.

Authors

M F Hibert¹, R Hoffmann, R C Miller, A A Carr

Affiliation

¹ Merrell Dow Research Institute, Strasbourg, France.

PMID: 2342053
DOI: 10.1021/jm00168a011

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.

MeSH terms

Animals
Binding Sites
Guinea Pigs
Mice
Protein Conformation
Rabbits
Rats
Receptors, Serotonin / drug effects
Receptors, Serotonin / metabolism*
Serotonin Antagonists / pharmacology*
Structure-Activity Relationship

Substances

Receptors, Serotonin
Serotonin Antagonists