| 体内研究: |
TRPV3 antagonist 74a (150 μg; intradermal injection; 30 minutes) decreases the number of scratches significantly. . TRPV3 antagonist 74a (10~100 mg/kg; p.o.) dose-dependently attenuates mechanical allodynia induced by von Frey hair stimulation to the ipsilateral (injured) hind paw. TRPV3 antagonist 74a exhibits anti-nociceptive activity in the reserpine model of central pain by increasing muscle pressure threshold. |
| 参考文献: |
1. Gomtsyan A, et al. Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists. J Med Chem. 2016;59(10):4926-4947. 2. Zhao J, et al. PAR2 Mediates Itch via TRPV3 Signaling in Keratinocytes. J Invest Dermatol. 2020;140(8):1524-1532. |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.956 ml |
14.779 ml |
29.558 ml |
| 5 mM |
0.591 ml |
2.956 ml |
5.912 ml |
| 10 mM |
0.296 ml |
1.478 ml |
2.956 ml |
| 50 mM |
0.059 ml |
0.296 ml |
0.591 ml |
|
| 注意: |
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