Rq 00203078, Potent And Selective Trpm8 Antagonist; Orally Active, Each

Details:

Rq 00203078 is a potent trpm8 antagonist (ic50 values are 5.3 And 8.3 Nm for rat and human channels respectively). Exhibits >350-fold selectivity for trpm8 over trpv4, trpv1 and trpa1. Reduces hsc3 and hsc4 oral squamous carcinoma cell migration and invasion in vitro. Also attenuates icilin -induced wet dog shakes in rats. Orally active.