Sivopixant

Names

[ Name ]:
Sivopixant

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor

Research Areas >> Neurological Disease

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₂ClN₅O₅

[ Molecular Weight ]:
507.93

Related Compounds

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