GP 2a

GP 2a is a cannabinoid 2 (CB2) receptor agonist (Ki = 7.6 nM for the mouse receptor). It is selective for CB2 receptors over CB1 receptors (Ki = 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). GP 2a inhibits SNI-induced increases in the number of activated spinal microglia and spinal astrocytes in the same mice.Formal Name: N-cyclohexyl-1-(2,4-dichlorophenyl)-1,4-dihydro-6-methyl-indeno[1,2-c]pyrazole-3-carboxamide. CAS Number: 919077-81-9. Synonyms: NESS 400. Molecular Formula: C24H23Cl2N3O. Formula Weight: 440.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly Soluble: 0.1-1 mg/ml, DMSO: Sparingly Soluble: 1-10 mg/ml. SMILES: O=C(C1=NN(C2=C(Cl)C=C(Cl)C=C2)C3=C1CC4=C3C=CC(C)=C4)NC5CCCCC5. InChi Code: InChI=1S/C24H23Cl2N3O/c1-14-7-9-18-15(11-14)12-19-22(24(30)27-17-5-3-2-4-6-17)28-29(23(18)19)21-10-8-16(25)13-20(21)26/h7-11,13,17H,2-6,12H2,1H3,(H,27,30). InChi Key: SPEFJYZGXZENAF-UHFFFAOYSA-N.