LEI-101 free base (LEI 101) is a potent, selective, orally available and peripherally restricted cannabinoid CB2 receptor agonist with binding pKi of 7.5 (hCB2R).
LEI-101 displays 100-fold selectivity for CB2 receptors over CB1 receptors in binding assays, does not interact with other proteins of the endocannabinoid system: human FAAH (hFAAH), MAGL, NAPE-PLD and DAGL.
LEI-101 behaves as a CB2 receptor partial agonist in the β-arrestin recruitment and GTPγS assays with pEC50 of 8.0 and 7.0, respectively.
LEI-101 (60 mg/kg, p.o.) does not induce cannabimimetic effects in vivo.
LEI-101 (3.0 or 10 mg/kg, p.o. and i.p.) attenuates biomarkers and histological damage of cisplatin-induced nephropathy in C57Bl6/J mice, prevents cisplatin-induced increases in serum creatinine and BUN levels.
LEI-101 attenuates cisplatin-induced renal 3-nitrotyrosine (3-NT) formation, attenuates cisplatin (Cis)-induced renal HNE adducts formation in wild type, but not in CB2R-/- mice.