Cat. No. 4532
Chemical Name: 2-Chloro-3-(4-methyl-1-piperazinyl)
Biological ActivityHigh affinity 5-HT3 receptor antagonist (IC50 values are 0.04 and 22 nM for human 5HT3A and 5-HT3AB receptors respectively). Exhibits partial agonist activity at 5-HT3A receptors at higher concentrations (EC50 = 5.2 μM). Also histamine H4 receptor antagonist (pKi = 6.64 in HEK cells).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Thompson et al (2012) VUF10166, a novel compound with differing activities at 5-HT3A and 5-HT3AB receptors. J.Pharmacol.Exp.Ther. 341 350. PMID: 22306960.
Smits et al (2008) Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo. J.Med.Chem. 51 2457. PMID: 18357976.
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Keywords: VUF 10166, supplier, 5-ht, serotonin, receptors, antagonists, high, affinity, partial, agonists, 5-ht3a, 5-ht3ab, 5-ht3, 5ht, VUF10166, Tocris Bioscience, 5-HT3 Receptor Antagonist products