cas 133841-15-3, 7-Hydroxygranisetron | Articles data ｜lookchem

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133841-15-3

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High-affinity fluorescent ligands for the 5-HT3 receptor
The synthesis, photophysical and biological characterization of a small library of fluorescent 5-HT3 receptor ligands is described. Several of these novel granisetron conjugates have high quantum yields and show high affinity for the human 5-HT3AR.
Simonin, Jonathan,Vernekar, Sanjeev Kumar V.,Thompson, Andrew J.,Hothersall, J. Daniel,Connolly, Christopher N.,Lummis, Sarah C.R.,Lochner, Martin
p. 1151 - 1155
(2012/03/26)

Toward biophysical probes for the 5-HT3 receptor: Structure-activity relationship study of granisetron derivatives
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.
Vernekar, Sanjeev Kumar V.,Hallaq, Hasan Y.,Clarkson, Guy,Thompson, Andrew J.,Silvestr, Linda,Lummis, Sarah C. R.,Lochner, Martin
supporting information; experimental part
p. 2324 - 2328
(2010/07/17)

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Chemical Properties

Melting Point: 225-230 °C (decomp)
Boiling Point: 583.7±50.0 °C(Predicted)
Density: 1.41
PKA: 8.90±0.40(Predicted)
PSA: 70.39000
LogP: 2.35280

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