SSR411298 是一种具有口服活性、选择性和可逆的脂肪酸酰胺水解酶 (FAAH) 抑制剂。SSR411298 具有用于创伤后应激障碍研究的潜力。
SSR411298 is an orally active, selective and reversible fatty acid amide hydrolase (FAAH) inhibitor. SSR411298 has the potential for post-traumatic stress disorder research[1].
SSR411298 (0.1, 1, 10, 100, 1000, 10000 nM) inhibits mouse brain FAAH in a concentration-dependent manner[1]. SSR411298 produces maximal inhibition of FAAH between 0.3 and 30 mg/kg in the ex-vivo experiment[1].
SSR411298 (0.3, 1, 3 mg/kg; p.o.; twice a day during 2 days; 60 minutes before pretest, immediately after, and 60 minutes before the second session of testing) produces robust antidepressant-like activity in the rat forced-swimming test and in the mouse chronic mild stress model, restoring notably the development of inadequate coping responses to chronic stress in male Wistar rats weighing 235-290 g[1]. SSR411298 (0.3, 1, 3, 10 mg/kg; po; single dose; two hours prior to sacrifice) produces a significant global increase of tissular AEA, PEA and OEA levels in the hippocampus, but not of 2-AG levels[1].
[1]. Guy Griebel, et al. The selective reversible FAAH inhibitor, SSR411298, restores the development of maladaptive behaviors to acute and chronic stress in rodents. Sci Rep. 2018 Feb 5;8(1):2416.
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