LY2828360

LY2828360 is a small molecule investigational drug that acts as a slowly signaling, G protein–biased agonist of the cannabinoid CB2 receptor. It selectively activates CB2 over CB1 receptors and inhibits cAMP accumulation while activating ERK1/2 signaling pathways without recruiting β-arrestin or internalizing the receptor[1][4][5][6]. Preclinical studies have shown that LY2828360 suppresses neuropathic nociception and attenuates the development of tolerance to opioid analgesics such as morphine in animal models of chemotherapy-induced neuropathic pain[5][6][7]. The compound has demonstrated good central nervous system penetration and oral activity in preclinical models. In clinical trials for osteoarthritic knee pain (NCT01319929), it was found to lack both toxicity and efficacy[3][5][6]. Developed by Eli Lilly, its primary investigated indication has been pain management—specifically osteoarthritic knee pain and chemotherapy-induced neuropathic pain.

Other names

8-(2-chlorophenyl)-2-methyl-6-(4-methylpiperazin-1-yl)-9-(tetrahydro-2H-pyran-4-yl)-9H-purineCB2 receptor agonist LY2828360CB-2 receptor agonist LY2828360CB 2 receptor agonist LY28283601231220-79-3UNII-O12H7VFU6PUNII-O-12H7VFU6PUNII-O 12H7VFU6P