Sivopixant (S-600918) is a potent and selective P2X3 receptor antagonist (P2X3 IC50 =4.2 nM; P2X2/3 IC50 =1100 nM). Sivopixant shows strong analgesic effect [1].
In Vivo, Sivopixant (S-600918) (i.v.;1 mg/kg) shows a longer half-life (T1/2= 10.1 hours) and a strong analgesic effect in the rat Seltzer model of allodynia (ED50=0.4 mg/kg)[1].
References:
[1]. Kai H, et al. Discovery of clinical candidate Sivopixant (S-600918): Lead optimization of dioxotriazine derivatives as selective P2X3 receptor antagonists [published online ahead of print, 2021 Sep 26]. Bioorg Med Chem Lett. 2021;52:128384.
In Vivo, Sivopixant (S-600918) (i.v.;1 mg/kg) shows a longer half-life (T1/2= 10.1 hours) and a strong analgesic effect in the rat Seltzer model of allodynia (ED50=0.4 mg/kg)[1].
References:
[1]. Kai H, et al. Discovery of clinical candidate Sivopixant (S-600918): Lead optimization of dioxotriazine derivatives as selective P2X3 receptor antagonists [published online ahead of print, 2021 Sep 26]. Bioorg Med Chem Lett. 2021;52:128384.