| 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 | [Uses]
P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect[1]. | [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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