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