URB937

URB937 is an orally active and peripherally restricted FAAH inhibitor (IC₅₀=26.8 nM) and increases anandamide levels. URB937 fails to affect FAAH activity in the brain (not penetrate the blood-brain barrier)^[1]. IC50 & Target: IC50: 26.8 nM (FAAH)^[1]. In Vitro: URB937 is actively extruded from the CNS by the ATP-binding cassette (ABC) membrane transporter, Abcg2^[3]. In Vivo: URB937 (1 mg/kg, i.p.) administrated in mice increases anandamide levels in peripheral tissues, but not forebrain or hypothalamus^[1].
URB937 (1 mg/kg, s.c.) suppresses pain responses elicited by i.p. injections of acetic acid^[1].
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^[2].
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^[3].
URB937 (1 mg/kg, every 2 days for 30 days) attenuates radiation-induced lung injury and increased endocannabinoid concentration in lung tissue^[4].