LEI-101 (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.