Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 53, Issue 5, Pages 2324-2328Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm901827x
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Funding
- EPSRC [EP/E042139/1]
- Wellcome Trust [081925/Z/07/Z]
- Engineering and Physical Sciences Research Council [EP/E042139/1] Funding Source: researchfish
- EPSRC [EP/E042139/1] Funding Source: UKRI
- Wellcome Trust [081925/Z/07/Z] Funding Source: Wellcome Trust
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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.
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