GP 2a

GP 2a is a cannabinoid 2 (CB₂) receptor agonist (K_i = 7.6 nM for the mouse receptor).¹ It is selective for CB₂ receptors over CB₁ receptors (K_i = 900 nM for the mouse receptor). GP 2a (5 to 100 nM) induces the CB₂ receptor-dependent phosphorylation of ERK1/2 in HL-60 leukemia promyeloblasts. In vivo, GP 2a (4 mg/kg per day) increases the mechanical threshold force to paw withdrawal and the latency to paw withdrawal from a radiant heat stimulus in a mouse model of neuropathic pain induced by spared nerve injury (SNI).² GP 2a inhibits SNI-induced increases in the number of activated spinal microglia and spinal astrocytes in the same mice.

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1. Murineddu, G., Lazzari, P., Ruiu, S., et al. Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB₂ cannabinoid ligand 1-(2',4'-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide. J. Med. Chem. 49(25), 7502-7512 (2006).

2. Luongo, L., Palazzo, E., Tambaro, S., et al. 1-(2',4'-dichlorophenyl)-6-methyl-N-cyclohexylamine-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide, a novel CB₂ agonist, alleviates neuropathic pain through functional microglial changes in mice. Neurobiol. Dis. 37(1), 177-185 (2010).