LY2828360

LY2828360 is a cannabinoid (CB) receptor 2 agonist (K_i = 40.3 nM).¹ It selectively activates CB₂ over CB₁ in a GTPγS binding assay (EC₅₀s = 20.1 and >100,000 nM, respectively). It reduces differences in hind paw weight bearing between monoiodoacetic acid- and saline-injected knees in a rat model of knee joint-related chronic pain induced by monoiodoacetic acid (MIA) when administered at doses greater than or equal to 0.1 mg/kg. LY2828360 dose-dependently reduces mechanical and cold allodynia induced by paclitaxel (Item No. 10461) in mice and prevents development of morphine tolerance when administered at dose of 3 mg/kg per day for 12 days.² It also reduces paclitaxel-induced allodynia in morphine-tolerant mice.

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1. Hollinshead, S.P., Tidwell, M.W., Palmer, J., et al. Selective cannabinoid receptor type 2 (CB₂) agonists: Optimization of a series of purines leading to the identification of a clinical candidate for the treatment of osteoarthritic pain. J. Med. Chem. 56(14), 5722-5733 (2013).

2. Lin, X., Dhopeshwarkar, A.S., Huibregtse, M., et al. Slowly signaling G protein-biased CB₂ cannabinoid receptor agonist LY2828360 suppresses neuropathic pain with sustained efficacy and attenuates morphine tolerance and dependence. Mol. Pharmacol. 93(2), 49-62 (2018).