产品描述: | A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux |
靶点: |
P2X3 Receptor |
体内研究: |
A-317491 (0.1-30 mg/kg; a single s.c.) dose-dependently reverses inflammatory mechanical hyperalgesia in rats. A-317491 (3-30 mg/kg; a single .v.) exhibits the plasma half-life (7.38 h), clearance rate (1.83 L/h/kg), and volume of distribution (0.17 L/kg) Animal Model: Male adult Sprague-Dawley rats received an intraplantar injection of Freund's complete adjuvant Dosage: 0.1, 1, 3, 10, 30 mg/kg Administration: A single s.c. Result: Produced a dose-dependent reduction in mechanical hyperalgesia 1 h, 3 h and 5 h post-administration. |
参考文献: |
1. Jarvis MF, et, al. A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat. Proc Natl Acad Sci U S A. 2002 Dec 24;99(26):17179-84. 2. Wu G, et, al. A-317491, a selective P2X3/P2X2/3 receptor antagonist, reverses inflammatory mechanical hyperalgesia through action at peripheral receptors in rats. Eur J Pharmacol. 2004 Nov 3;504(1-2):45-53. |
溶解性: |
Soluble in DMSO、H2O |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.768 ml |
8.841 ml |
17.681 ml |
5 mM |
0.354 ml |
1.768 ml |
3.536 ml |
10 mM |
0.177 ml |
0.884 ml |
1.768 ml |
50 mM |
0.035 ml |
0.177 ml |
0.354 ml |
|
注意: |
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