Agonists of the peripheral cannabinoid (CB) receptor CB may have antinociceptive and anti-inflammatory effects, as well as prevent osteoporosis. 4-Quinolone-3-carboxamide Furan CB Agonist is a high-affinity ligand of CB (K = 8.5 nM) with little affinity for CB (K >10,000 nM). This compound demonstrates antinociceptive efficacy in the mouse formalin test at 1 mg/kg, an action which is blocked by a CB-selective antagonist, AM630 .
4-Quinolone-3-Carboxamide Furan CB2 Agonist is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a Ki of 8.5 nM. 4-Quinolone-3-Carboxamide Furan CB2 Agonist has high affinity and selectivity for CB2.
体外研究
4-Quinolone-3-Carboxamide Furan CB2 Agonist (1 μM; 72 hours) has very low or no cytotoxicity to Hep-G2 cells.
Cell Proliferation Assay
Cell Line:
Hep-G2 (Human hepatoblastoma) cells
Concentration:
1 μM
Incubation Time:
72 hours
Result:
Exhibited very low or no cytotoxicity to Hep-G2 cells.
体内研究
4-Quinolone-3-Carboxamide Furan CB2 Agonist (1 and 3 mg/kg; 1 hour) is very potent (with maximal effect being reached already at the 1 mg/kg dose) and has antihyperalgesic effects, efficacious also on the first phase of the nocifensive response and strongly reduced by AM630 (CB2-selective antagonist/inverse agonist) .
Animal Model:
Formalin injection induces a biphasic stereotypical nocifensive behavior in mice
Dosage:
Formalin (1.25% in saline, 30 μL), 1 and 3 mg/kg CB2 receptor agonist 2, 1 mg/kg AM630, monitor every 5 minutes for 1 hour
Administration:
Injection in the dorsal surface of one side of the hindpaw (Formalin), i.p. (CB2 receptor agonist, AM630)
Result:
Elicited antihyperalgesic effects and potent (with maximal effect being reached already at the 1 mg/kg dose) and efficacious, strongly reduced by AM630.
分子式
C30H36N2O4
分子量
488.62
CAS号
1314230-75-5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
Ethanol : 30 mg/mL (61.40 mM; Need ultrasonic and warming)