Gefapixant

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Gefapixant

CAS No. : 1015787-98-0

MCE 国际站：Gefapixant

产品活性：Gefapixant (MK-7264) 是一个口服的、P2X3 受体活性拮抗剂，其对人同源重组 hP2X3 和 hP2X2/3 的 IC₅₀ 值分别是 ~30 nM 和 100-250 nM。

研究领域：Membrane Transporter/Ion Channel

作用靶点：P2X Receptor

In Vitro: The aryloxy-pyrimidinediamine, Gefapixant (AF-219) is an orally active small molecule antagonist at human P2X3-containing receptors. The IC₅₀ of Gefapixant has been reported as ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors, potencies very similar to those reported for recombinant rat receptors, and it displays no inhibitory impact on any non-P2X3 subunit containing receptors (IC₅₀ values>>10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5 and hP2X7 channels).

In Vivo: In an adjuvant-induced rthritis model in rat (7d following intraplantar administration of complete Freund's adjuvant), AF-353 produces dose-dependent antihyperalgesia in weight-bearing asymmetry and von Frey filament mechanical tests; magnitude of effect is compared with that of the NSAID naproxen. In a rat model of knee osteoarthritis (14d following intra-articular administration of monoiodoacetate), Gefapixant (7d bid, orally; right) attenuates the weight bearing laterality with complete reversal of apparent hyperalgesia at the two higher doses.

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