PU-02 is a potent and selective 5-HT3 receptor antagonist. PU02 exhibits IC(50) values of ~1 μM at 5-HT(3)Rs and substantially lower activities at other Cys-loop receptors. 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. References: Trattnig SM, Harpsoe K, Thygesen SB, Rahr LM, Ahring PK, Balle T, Jensen AA. Discovery of a novel allosteric modulator of 5-HT3 receptors: inhibition and potentiation of Cys-loop receptor signaling through a conserved transmembrane intersubunit site. J Biol Chem. 2012 Jul 20;287(30):25241-54. doi: 10.1074/jbc.M112.360370. Epub 2012 May 15. PubMed PMID: 22589534; PubMed Central PMCID: PMC3408183.

纯度：≥98%

CAS：313984-77-9