URB-597 | FAAH inhibitor
URB-597 (546141-08-6) is a potent and selective fatty acid amide hydrolase (FAAH) inhibitor, IC50 = 3-5 nM.1 Produces cannabinoid CB1 and CB2 receptor-mediated analgesia in inflammatory pain states without causing side effects associated with cannabinoid receptor activation.2 Attenuates the anxiolytic-like effect of acetaminophen in a mouse model.3 Exerts anti-inflammatory effects in rat hippocampus and ameliorates age-related deficits.4 Off target effects of URB-597: Reduces tyrosine hydroxylase expression.5 Improves cognitive impairment caused by chronic cerebral hypoperfusion in a mouse model via inhibition of mTOR-dependent autophagy.6
References/Citations:
1) Piomelli et al. (2006), Pharmacological profile of the selective FAAH inhibitor KDS-4103 (URB597); CNS Drugs Rev., 12 21
2) Jayamanne et al. (2006), Actions of the FAAH inhibitor URB597 in neuropathic and inflammatory chronic pain models; Br. J. Pharmacol., 147 281
3) Zaitone et al. (2012), Inhibition of fatty acid amide hydrolase by URB597 attenuates the anxiolytic-like effect of acetaminophen in the mouse elevated plus-maze test; Behav. Pharmacol., 23 417
4) Murphy et al. (2012), The fatty acid amide hydrolase inhibitor URB597 exerts anti-inflammatory effects in hippocampus of aged rats and restores an age-related deficit in long-term potentiation; Neuroinflammation, 9 79
5) Bosier et al. (2013), The FAAH inhibitor URB597 efficiently reduces tyrosine hydroxylase expression through CB- and FAAH-independent mechanisms; Br. J. Pharmacol., 169 794
6) Wang et al. (2017), URB597 improves cognitive impairment induced by chronic cerebral hypoperfusion by inhibiting mTOR-dependent autophagy; Neuroscience, 344 293
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