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URB937

CAS No. : 1357160-72-5

MCE 国际站：URB937

产品活性：URB937 是口服有效的、外周限制的 FAAH 抑制剂，IC₅₀ 值为 26.8 nM，可增加 anandamide 水平。URB937 不能影响脑内 FAAH 水平 (无法透过血脑屏障)。

研究领域：Metabolic Enzyme/Protease  |  Neuronal Signaling

作用靶点：FAAH

In Vitro: URB937 is actively extruded from the CNS by the ATP-binding cassette (ABC) membrane transporter, Abcg2.

In Vivo: URB937 (1 mg/kg, i.p.) administrated in mice increases anandamide levels in peripheral tissues, but not forebrain or hypothalamus.
URB937 (1 mg/kg, s.c.) suppresses pain responses elicited by i.p. injections of acetic acid.
URB937 in male rats (an oral dose 3 mg/kg, F = 36%) is absorbed at a moderate rate and displays a peak plasma concentration (C_max) of 159.47 ng/ml, which was achieved one hour after administration. URB937 exhibits T_1/2 of 60 min by an oral dose of 3 mg/kg.
URB937 produces a high degree of antinociception in female mice and rats in models of visceral and inflammatory pain. Moreover, the compound displayed a restricted access to placental and fetal tissues in pregnant mice and rats.
URB937 (1 mg/kg, every 2 days for 30 days) attenuates radiation-induced lung injury and increased endocannabinoid concentration in lung tissue.

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