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

Sanjeev Kumar V. Vernekar, Hasan Y. Hallaq, Guy Clarkson, Andrew J. Thompson, Linda Silvestr, Sarah C.R. Lummis, Martin Lochner

Research output: Contribution to journalArticlepeer-review

43 Scopus citations


This report describes the synthesis and biological characterization of novel granisetron derivatives that are antagonists of the human serotonin (5-HT3A) 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-HT3A receptors in mammalian cells.

Original languageEnglish (US)
Pages (from-to)2324-2328
Number of pages5
JournalJournal of medicinal chemistry
Issue number5
StatePublished - Mar 11 2010

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