Toward biophysical probes for the 5-HT3 receptor: structure-activity relationship study of granisetron derivatives.

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Vernekar SK, Hallaq HY, Clarkson G, Thompson AJ, Silvestri L, Lummis SC, Lochner M

Toward biophysical probes for the 5-HT3 receptor: structure-activity relationship study of granisetron derivatives.

J Med Chem. 2010 Mar 11;53(5):2324-8. doi: 10.1021/jm901827x.

PubMed ID

20146481 [ View in PubMed

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Abstract

This report describes the synthesis and biological characterization of novel granisetron derivatives that are antagonists of the human serotonin (5-HT(3)A) receptor. Some of these substituted granisetron derivatives showed low nanomolar binding affinity and allowed the identification of positions on the granisetron core that might be used as attachment points for biophysical tags. A BODIPY fluorophore was appended to one such position and specifically bound to 5-HT(3)A receptors in mammalian cells.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Granisetron	5-hydroxytryptamine receptor 3A	Ki (nM)	1.45	N/A	N/A	Details