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PU02 (NMMP) is a potent and selective antagonist displaying IC50 values of ~1 μM at 5-HT(3)Rs and substantially lower activities at other Cys-loop receptors. PU02 is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively.
PU02 inhibits the proliferation of hepatocellular carcinoma (HepG2) cells associated with G2/M phase cell cycle arrest, and reduced cyclin-dependent kinase (CDK) 4 and cyclin B1/D1 levels. In an elaborate mutagenesis study of the 5-HT(3)A receptor guided by a homology model, PU02 is demonstrated to act through a transmembrane intersubunit site situated in the upper three helical turns of TM2 and TM3 in the (+)-subunit and TM1 and TM2 in the (-)-subunit.
| Molecular Weight | 292.36 |
| Formula | C16H12N4S |
| CAS Number | 313984-77-9 |
| Solubility (25°C) | DMSO >100 mg/mL |
| Storage | -20°C, sealed |
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