Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site.
Article Details
- CitationCopy to clipboard
Hibert MF, Hoffmann R, Miller RC, Carr AA
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.
- PubMed ID
- 2342053 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Granisetron 5-hydroxytryptamine receptor 3A Kd (nM) 7.94 N/A N/A Details Granisetron 5-hydroxytryptamine receptor 3A Kd (nM) 0.126 N/A N/A Details Granisetron 5-hydroxytryptamine receptor 3A Kd (nM) 0.02 N/A N/A Details Metoclopramide 5-hydroxytryptamine receptor 3A Kd (nM) 50.12 N/A N/A Details Ondansetron 5-hydroxytryptamine receptor 3A Kd (nM) 0.0794 N/A N/A Details Ondansetron 5-hydroxytryptamine receptor 3A Kd (nM) 50.12 N/A N/A Details Ondansetron 5-hydroxytryptamine receptor 3A Kd (nM) 0.398 N/A N/A Details