URB 937 is a potent inhibitor of fatty-acid amide hydrolase (FAAH), an intracellular serine hydrolase responsible for the deactivation of the endocannabinoid anandamide. It is actively extruded from the central nervous system (CNS), and therefore increases anandamide levels exclusively in peripheral tissues.
URB937 is a fatty acid amide hydrolase (FAAH) inhibitor th at is actively excluded from the CNS by the membrane transporter ABCG2. The ED50 for inhibition of FAAH activity in the brain is 200 times higher than inhibition of renal FAAH activity. In vivo administration of URB937 elevates anandamide levels in peripheral tissues, and attenuates acetic acid-induced writhing, hyperalgesia in a sciatic nerve ligation model, and pain and edema in carrageenan injected paws.
