PSB-1011 is a competitive inhibitor of the rat P2X2 receptor with a Ki of 79 nM. PSB-1011 exhibited a competitive mechanism of action (pA(2) 7.49). It was >100-fold selective versus P2X4, P2X7, and several investigated P2Y receptor subtypes (P2Y(2,4,6,12)); selectivity versus P2X1 and P2X3 receptors was moderate (>5-fold). PSB-1011 was >13-fold more potent at the homomeric P2X2 than at the heteromeric P2X2/3 receptor. References: Hausmann R, Schmalzing G. P2X1 and P2X2 receptors in the central nervous system as possible drug targets. CNS Neurol Disord Drug Targets. 2012 Sep;11(6):675-86. Review. PubMed PMID: 22963438.

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CAS：4499-01-8