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Toward biophysical probes for the 5-HT3 receptor : structure-activity relationship study of granisetron derivatives
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Vernekar, Sanjeev Kumar V., Hallaq, Hasan Y., Clarkson, Guy J., Thompson, Andrew J., Silvestri, Linda, Lummis, Sarah C. R. and Lochner, Martin (2010) Toward biophysical probes for the 5-HT3 receptor : structure-activity relationship study of granisetron derivatives. Journal of Medicinal Chemistry, Vol.53 (No.5). pp. 2324-2328. doi:10.1021/jm901827x ISSN 0022-2623.
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Official URL: http://dx.doi.org/10.1021/jm901827x
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.
| Item Type: | Journal Article | ||||
|---|---|---|---|---|---|
| Subjects: | Q Science > QD Chemistry | ||||
| Divisions: | Faculty of Science, Engineering and Medicine > Science > Chemistry | ||||
| Journal or Publication Title: | Journal of Medicinal Chemistry | ||||
| Publisher: | American Chemical Society | ||||
| ISSN: | 0022-2623 | ||||
| Official Date: | 11 March 2010 | ||||
| Dates: |
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| Volume: | Vol.53 | ||||
| Number: | No.5 | ||||
| Number of Pages: | 5 | ||||
| Page Range: | pp. 2324-2328 | ||||
| DOI: | 10.1021/jm901827x | ||||
| Status: | Peer Reviewed | ||||
| Publication Status: | Published | ||||
| Access rights to Published version: | Restricted or Subscription Access | ||||
| Funder: | Engineering and Physical Sciences Research Council (EPSRC), Wellcome Trust | ||||
| Grant number: | EP/E042139/1 (EPSRC), 081925/Z/07/Z |
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