4-Quinolone-3-Carboxamide CB2 Ligand

Cannabinoids (CBs) and their synthetic analogs produce biochemical and pharmacological effects by interacting with the central CB1 and peripheral CB2 receptors. The CB2 receptor has emerged as a pharmacotherapeutic target for treating osteoporosis, as well as for eliciting antinociceptive effects in various models of pain. 4-Quinolone-3-carboxamide CB2 ligand is a selective, high-affinity ligand of the CB2 receptor, displaying a Ki value of 0.6 nM (Ki >10,000 nM for CB1) in vitro. At a dose of 6 mg/kg, 4-quinolone-3-carboxamide CB2 ligand exhibits antinociceptive activity in a formalin test of nocifensive response in mice. This analgesic affect is not significantly reversed by the CB2 antagonist AM630 (Cay-10006974), which suggests 4-quinolone-3-carboxamide CB2 ligand may behave as an inverse agonist.Formal Name: 1,4-dihydro-8-methoxy-4-oxo-1-pentyl-N-tricyclo[3.3.1.13,7]dec-1-yl-3-quinolinecarboxamide. CAS Number: 1314230-69-7. Synonyms: 4Q3C CB2 Ligand. Molecular Formula: C26H34N2O3. Formula Weight: 422.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMSO: 3 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:4): 0.2 mg/ml. lambdamax: 230, 323 nm. SMILES: O=C(C1=CN(CCCCC)C2=C(C=CC=C2OC)C1=O)N[C@@]34CC5C[C@H](C4)C[C@H](C3)C5. InChi Code: InChI=1S/C26H34N2O3/c1-3-4-5-9-28-16-21(24(29)20-7-6-8-22(31-2)23(20)28)25(30)27-26-13-17-10-18(14-26)12-19(11-17)15-26/h6-8,16-19H,3-5,9-15H2,1-2H3,(H,27,30)/t17-,18+,19?,26?. InChi Key: YGNQQLUXHGNAEG-SJCABOPASA-N.