title: 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.
authors.affiliation: Merrell Dow Research Institute, Strasbourg, France.
authors.forename: M F
authors.initials: MF
authors.lastname: Hibert
authors.forename: R
authors.initials: R
authors.lastname: Hoffmann
authors.forename: R C
authors.initials: RC
authors.lastname: Miller
authors.forename: A A
authors.initials: AA
authors.lastname: Carr
mesh_terms: D000818:Animals; D001665:Binding Sites; D006168:Guinea Pigs; D051379:Mice; D011487:Protein Conformation; D011817:Rabbits; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D011985:Receptors, Serotonin; D012702:Serotonin Antagonists