| Identification | Back Directory | [Name]
4-Quinolone-3-Carboxamide Furan CB2 Agonist | [CAS]
1314230-75-5 | [Synonyms]
4-Quinolone-3-Carboxamide Furan CB2 Agonist
N-(1-adamantyl)-6-(furan-2-yl)-8-methoxy-4-oxo-1-pentylquinoline-3-carboxamide
3-Quinolinecarboxamide, 6-(2-furanyl)-1,4-dihydro-8-methoxy-4-oxo-1-pentyl-N-tricyclo[3.3.1.13,7]dec-1-yl- | [Molecular Formula]
C30H36N2O4 | [MOL File]
1314230-75-5.mol | [Molecular Weight]
488.62 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
≤30mg/ml in ethanol;3mg/ml in DMSO;3mg/ml in dimethyl formamide | [form ]
crystalline solid | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Biological Activity]
ki: 8.5 nm4-quinolone-3-carboxamide furan cb2 agonist is a high-affinity ligand of cb2.the endocannabinoid system consists of endogenous cannabinoids (endocannabinoids), cannabinoid receptors (primarily cb1 and cb2), and the enzymes that synthesize and degrade endocannabinoids. | [in vitro]
previous study found that 4-quinolone-3-carboxamide furan cb2 agonist (4g) was devoid of any potential “indirect” agonist activity at cannabinoid receptors, exerted by prolonging the lifespan of endocannabinoids because 4g at up to a 10 μm concentration did not inhibit anandamide or 2-ag degradation by faah or magl, respectively. in cytotosicity study, 4g was tested at 1 μm and the results showed that it exhibited very low or no cytotoxicity, the cell viability being above 95% after a 72 h treatment [1]. | [in vivo]
in animal study, 4g was found to have antinociceptive activity in the formalin test in mice. moreover, 4g was very potent with maximal effect being reached at the 1 mg/kg dose and efficacious also on the first phase of the nocifensive response. the effect of 4g could be strongly reduced by the addition of am630, a cb2-selective antagonist/inverse agonist, therefore demonstrating that 4g might act as a potent and selective cb2 agonist [1]. | [References]
[1] s. pasquini, m. de rosa, v. pedani, et al. investigations on the 4-quinolone-3-carboxylic acid motif. 4. identification of new potent and selective ligands for the cannabinoid type 2 receptor with diverse substitution patterns and antihyperalgesic effects in mice. journal of medicinal chemistry 54, 5444-5453 (2011). |
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