| Identification | Back Directory | [Name]
1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)- | [CAS]
2417288-67-4 | [Synonyms]
1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)- | [Molecular Formula]
C24H26F2N4O3 | [MDL Number]
MFCD32857164 | [MOL File]
2417288-67-4.mol | [Molecular Weight]
456.48 |
| Hazard Information | Back Directory | [Biological Activity]
P2X3 antagonist 34 is a potent, selective, orally active P2X3 homotrimeric receptor antagonist with IC50 of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively . It is less active at human, rat and guinea pig P2X2/3 heterotrimeric receptors and has a strong antitussive effect. | [in vitro]
P2X3 antagonist 34 (BLU-5937; 500 nM) is able to block αβ-meATP-induced sensitization and firing activity of isolated primary nociceptors in rat dorsal root ganglions (DRGs), through P2X3 homotrimeric receptor antagonism. The sensitizing effect of αβ-meATP and the inhibition of P2X3 antagonist 34 are reversible after washout. | [in vivo]
P2X3 antagonist 34 (BLU-5937; 0.3-0 mg/kg, oral administration; male Dunkin Hartley guinea pigs) treatment significantly reduces the histamine-induced enhancement in the number of citric acid-induced coughs in a dose -dependent fashion in a guinea pig cough model.
It (BLU-5937; 3 and 30 mg/kg, oral) is also shown to reduce significantly and dose-dependently the ATP-induced enhancement of citric acid- induced coughs in the guinea pig. < table class="zh_use_1"> | Animal Model: | Male Dunkin Hartley guinea pigs | | Dosage: | 0.3 mg/kg, 3 mg/kg, 30 mg/kg | | Administration: | Oral administration | | Result: | < td class="col2"> Significantly reduced the histamine-induced enhancement in the n umber of citric acid-induced coughs in a dose-dependent fashion. |
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