URB937

URB937 is a **potent, orally active, peripherally restricted inhibitor of fatty acid amide hydrolase** (FAAH), the enzyme responsible for degrading endocannabinoids such as anandamide and related fatty acid amides. Unlike other FAAH inhibitors, URB937 is actively excluded from the central nervous system (CNS) by the membrane transporter ABCG2, resulting in selective action in peripheral tissues. URB937 markedly **increases anandamide and oleoylethanolamide levels in peripheral tissues**, resulting in strong **analgesic effects in animal models** of acute, chronic, inflammatory, neuropathic, and migraine pain, as well as disease states characterized by bladder overactivity and radiation-induced lung injury. Preclinical safety studies show a high degree of target selectivity, lack of genotoxicity, and good oral tolerability, with no significant toxicity at supramaximal doses. URB937 is under continued preclinical development for the treatment of pain and possibly other peripheral disorders[1][3][7][9][10].

Other names

EX-937EX937EX 937URB937URB-937URB 937