An endogenous cannabinoid
Arachidonoyl ethanolamide (AEA) is the ethanolamine amide of arachidonic acid, originally isolated from porcine brain.1 AEA is an endogenous cannabinoid neurotransmitter that binds to both cannabinoid 1 (CB1) and CB2 receptors.2 AEA has Ki values ranging from 61 to 543 nM for CB1 receptors and from 279 to 1,940 nM for CB2 receptors.3
1.Devane, W.A., Hanus, L., Breuer, A., et al.Isolation and structure of a brain constituent that binds to the cannabinoid receptorScience258(5090)1946-1949(1992) 2.Felder, C.C., Briley, E.M., Axelrod, J., et al.Anandamide, an endogenous cannabimimetic eicosanoid, binds to the cloned human cannabinoid receptor and stimulates receptor-mediated signal transductionProc. Natl. Acad. Sci. USA90(16)7656-7660(1993) 3.Pertwee, R.G.Pharmacology of cannabinoid receptor ligandsCurr. Med. Chem.6(8)635-664(1999)
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Animal experiment: |
Mice[2]Eleven-week-old C57BL/6J male mice and global CB1R-/- mice are housed individually on a 12/12-h light/dark schedule at 22-23°C with ad libitum access to water and food. A group of mice is subject to a high-fat diet (30% lard). After 16 weeks of diet, animals with a weight gain less than +10 g compared with controls are excluded from the study. Diet-induced obesity (DIO) mice (39.1±1.1 vs. 27.3±0.9 g, DIO vs. control) are glucose intolerant and insulin resistant. On the day of each experiment, food is removed from the cages for 6 h (from 8:00 A.M. to 2:00 P.M.). Anandamide is administered intraperitoneally at 10 mg/kg. In control experiments, animals are injected with vehicle (4% DMSO/1% Tween 80)[2]. |
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参考文献: [1]. Malek N, et al. Anandamide, Acting via CB2 Receptors, Alleviates LPS-Induced Neuroinflammation in Rat Primary Microglial Cultures. Neural Plast. 2015;2015:130639. |
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