产品
编 号:F066401
分子式:C24H23F3N4O2
分子量:456.46
产品类型
结构图
CAS No: 1196109-52-0
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产品详情
生物活性:
PF-3845 is a potent, selective, irreversible and orally active inhibitor of fatty acid amide hydrolase (FAAH), with a Ki of 0.23 μM. PF-3845 is a covalent inhibitor that carbamylates FAAH's serine nucleophile. PF-3845 can reduce pain sensation, inflammation, and anxiety/depression without substantial effects on motility or cognition.
体内研究:
PF-3845 (1-30 mg/kg; p.o.) produces cannabinoid receptor-dependent reductions in inflammatory pain in rat.PF-3845 (10 mg/kg; a single i.p.) selectively inhibits FAAH in mice for up to 24 hours.PF-3845 (10 mg/kg; a single i.p.) causes a dramatic and sustained elevation in Anandamide (AEA) in mice.Animal Model:Male Sprague-Dawley rats (200g- 250g) are injected CFA
Dosage:1, 3, 10, 30 mg/kg
Administration:Oral administration
Result:Caused a dose-dependent inhibition of mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg.
体外研究:
PF-3845 (0.5 nM-10 μM; 40 min) inhibits human FAAH-1 (IC50=18 nM) in a concentration-dependent manner, and shows negligible activity against FAAH-2 (IC50>10 μM) in COS-7 cells.PF-3845 (0.1-1000 μM; 48 h) significantly decreases the Colo-205 cell viability.