Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site.
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.
Hibert
M F
MF
Merrell Dow Research Institute, Strasbourg, France.
Hoffmann
R
R
Miller
R C
RC
Carr
A A
AA
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
D011985:Receptors, Serotonin; D012702:Serotonin Antagonists