货号 | 72620-5mg |
描述 | Anandamide (arachidonoyl ethanolamide; AEA) is an endogenous lipid with cannabinergic activity; along with 2-arachidonoyl glycerol, it forms part of the endocannabinoid system.1,2 AEA undergoes reuptake into neurons by a facilitated process.3 Controversy exists as to whether there is a specific AEA transporter, or instead the uptake process is simply driven by hydrolysis of AEA by intracellular fatty acyl amide hydrolase (FAAH).4,5 CAY10412 is an analog of AEA that has no intrinsic binding affinity for either CB1 or CB2receptors.6 It is a potent inhibitor of AEA reuptake in U937 lymphoma cells, with an IC50 of 3 µM.6 CAY10412 could be a useful tool for distinguishing the competing transporter theories. The pharmacology of CAY10412 is largely unexplored; it may enhance endocannabinoid signalling by augmenting endocannabinoid concentrations. |
供应商 | Cayman |
应用文献 | |
1.Devane, W.A.,Hanus, L.,Breuer, A., et al. Isolation and structure of a brain constituent that binds to the cannabinoid receptor. Science 258, 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 transduction. Proceedings of the National Academy of Sciences of the United States of America 90, 7656-7660 (1993). 3.Deutsch, D.G.,Glaser, S.T.,Howell, J.M., et al. The cellular uptake of anandamide is coupled to its breakdown by fatty-acid amide hydrolase. The Journal of Biological Chemisty 276(10), 6967-6973 (2001). 4.Beltramo, M.,Stella, N.,Calignano, A., et al. Functional role of high-affinity anandamide transport, as revealed by selective inhibition. Science 277, 1094-1097 (1997). 5.Glaser, S.T.,Abumrad, N.A.,Fatade, F., et al. Evidence against the presence of an anandamide transporter. Proceedings of the National Academy of Sciences of the United States of America 100(7), 4269-4274 (2003). 6.López-Rodriguez, M.L.,Viso, A.,Ortega-Gutiérrez, S., et al. Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors. Journal of Medicinal Chemistry 44, 4505-4508 (2001). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 400.6 |
分子式 | C25H36O2S |
CAS号 | 390824-17-6 |
稳定性 | ≥ 1 year |
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