CAS:1020315-31-4PF-04457845

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PF-04457845 selectively inhibits FAAH with an IC50 of 7.2 nM. It has anti-inflammatory effects and is used as analgesic.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1020315-31-4

储存条件

分子式

C23H20F3N5O2

运输

蓝冰

分子量

455.43

别名

溶解度

动物实验配方

生物活性

描述Fatty acid amide hydrolase (FAAH) is an integral membrane serine hydrolase that degrades the fatty acid amide family of signaling lipids, including the endocannabinoid anandamide. PF-04457845 selectively inhibits FAAH with an IC₅₀ of 7.2 nM. Men aged 18–55 years with cannabis dependence were treated with PF-04457845 (4 mg per day), and they showed reduced symptoms of cannabis withdrawal, lower self-reported cannabis use and lower urinary THC-COOH concentrations, compared with placebo group. Osteoarthritis patients administrated with 4 mg q.d. PF-04457845 showed decreased FAAH activity by >96% and significantly increased 4 endogenous substrates (fatty acid amides). PF-04457845 was well tolerated in osteoarthritis patients, and there was no evidence of cannabinoid-type adverse events, but failed to induce effective analgesia.
作用机制PF-04457845 inhibits FAAH by a covalent, irreversible mechanism involving carbamylation of the active-site serine nucleophile of FAAH.