IC50: 25 nM (hP2X3), >24000 nM (hP2X2/3), 92 nM (rP2X3), 1820 nM (rP2X2/3), 126 nM (gpP2X3), 3450 nM (gpP2X2/3)[1]
Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough[1].
Camlipixant (BLU-5937; 500 nM) 阻断 ATP 介导的背根神经节 (DRG) 神经元敏化[1]。
Camlipixant (BLU-5937; 3-30 mg/kg; oral) 减少组胺和 ATP 诱导的豚鼠咳嗽过敏[1]。
Camlipixant (BLU-5937; 10-20 mg/kg; i.p.) 与对照动物相比，不会改变味觉知觉[1]。
Camlipixant (BLU-5937) 表现出优异的类药物特性，包括良好的口服生物利用度，在人体内预测清除率低，无血脑屏障渗透性，安全性高[1]。
| Animal Model: | Male Dunkin Hartley guinea pigs[1] |
| Dosage: | 0.3, 3, 30 mg/kg |
| Administration: | PO, approximately 2 h prior to tussive agent exposure |
| Result: | Significantly reduced the histamine-induced enhancement in the number of citric acid-induced coughs. Reduced significantly and dose-dependently the ATP-induced enhancement of citric acid-induced coughs. |
[1]. Garceau D, Chauret N. BLU-5937: A selective P2X3 antagonist with potent anti-tussive effect and no taste alteration. Pulm Pharmacol Ther. 2019 Jun;56:56-62.