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PU 02 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 with IC50 values ranging from 0.36 to 1.3 μM for human 5-HT3A, 5-HT3AB, 5-HT3AC, and 5-HT3AE in a FLIPR membrane potential assay using HEK293 cells expressing human recombinant receptors.1 It is selective for 5-HT3 over other Cys-loop containing receptors with IC50 values >100 μM for mouse, rat, and human nicotinic (nACh), human GABAA, and human glycine (Gly) receptors. PU 02 inhibits currents induced by 5-HT (Item No. 14332) in COS-7 cells expressing human 5-HT3A (IC50 = 0.49 μM). PU 02 also reduces growth of HepG2 cells in a dose-dependent manner via induction of cell cycle arrest at the G2/M phase and apoptosis.2
WARNING This product is not for human or veterinary use.
1. Discovery of a novel allosteric modulator of 5-
2. 6-