Eliapixant (BAY 1817080) is a potent, selective P2X3 receptor antagonist with IC50 of 8 nM (hP2X3).
Eliapixant inhibits agonist-mediated hP2X2/3 receptor response, show no inhibition on recombinant cell lines expressing hP2X1 receptors, and the homotrimeric hP2X2, hP2X4, and hP2X7 receptors.
Eliapixant reduces inflammatory pain in relevant animal models, and reduces vaginal hyperalgesia in an animal model of endometriosis-associated dyspareunia, even beyond treatment cessation.
