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Brain-penetrant, orally active, potent and selective transient receptor potential cation channel TRPV1 antagonist with in vivo analgesia efficacy.
A-784168 is a brain-penetrant, orally active, potent and selective transient receptor potential (TRP) cation channel TRPV1 antagonist (IC50 = 25/14/33.7/35.1 nM against TRPV1 activation by 50 nM capsaicin/pH 5.5/3 µM NADA/10 µM anandamide in human TRPV1 tranfectants) with little activity or affinity toward other TRP channels and a panel of 74 neurotransmitter receptors. A-784168 reduces capsaicin-induced acute pain (ED50 = 10 µmol/kg p.o. 1h before capsaicin intraplantar injection) and CFA paw injection-induced chronic inflammatory thermal hyperalgesia (EC50 = 54 nmol) in rats in vivo.
A-784168 is a brain-penetrant, orally active, potent and selective transient receptor potential (TRP) cation channel TRPV1 antagonist (IC50 = 25/14/33.7/35.1 nM against TRPV1 activation by 50 nM capsaicin/pH 5.5/3 µM NADA/10 µM anandamide in human TRPV1 tranfectants) with little activity or affinity toward other TRP channels and a panel of 74 neurotransmitter receptors. A-784168 reduces capsaicin-induced acute pain (ED50 = 10 µmol/kg p.o. 1h before capsaicin intraplantar injection) and CFA paw injection-induced chronic inflammatory thermal hyperalgesia (EC50 = 54 nmol) in rats in vivo.
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Role of TRPV1 and ASIC3 in formalin-induced secondary allodynia and hyperalgesia
Pharmacological Reports, 66(6), 964-971 (2014)
TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists
The Journal of Neuroscience, 26(37), 9385-9393 (2006)
Characterization of nerve growth factor-induced mechanical and thermal hypersensitivity in rats
European Journal of Pain, 17(4), 469-479 (2013)
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