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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.
訊號詞
Danger
危險聲明
危險分類
Acute Tox. 3 Oral
儲存類別代碼
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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