| 货号 | 10006731-10mg |
| 描述 | Numerous analogs of arachidonoyl ethanolamide (AEA) potentiate its biological activity. This potentiation is ascribed either to inhibition of AEA reuptake into neurons, or inhibition of fatty amide acyl hydrolase (FAAH) within the neurons.1,2 VDM11 is an AEA transport inhibitor with essentially no activity on either the central cannabinoid receptor (CB1), peripheral cannabinoid receptor (CB2), or the vanilloid receptor 1 (VR1).3 However, VDM11 inhibits FAAH and monoacylglycerol lipase (MAGL) and may act as an alternative FAAH substrate.4 At a concentration of 3 µM, VDM11, like AM404, inhibits glutamergic synaptic transmission between hippocampal neurons.5 The mechanism of this effect may be a direct action on sodium channels. Thus, the use of anandamide analogs as uptake inhibitors and interpretation of the results must be undertaken with care. |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Khanolkar, A.D., and Makriyannis, A. Structure-activity relationships of anandamide, an endogenous cannabinoid ligand. Life Sciences 65, 607-616 (1999). 2.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). 3.De Petrocellis, L.,Bisogno, T.,Davis, B.J., et al. Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: Inhibitors of anandamide uptake with negligible capsaicin-like activity. FEBS Letters 483, 52-56 (2000). 4.Vandervoorde, S., and Fowler, C.J. Inhibition of fatty acid amide hydrolase and monoacylglycerol lipase by the anandamide uptake inhibitor VDM11: Evidence that VDM11 acts as an FAAH substrate. British Journal of Pharmacology 145, 885-893 (2005). 5.Kelley, B.G., and Thayer, S.A. Anandamide transport inhibitor AM404 and structurally related compounds inhibit synaptic transmission between rat hippocampal neurons in culture independent of cannabinoid CB1 receptors. European Journal of Pharmacology 496, 33-39 (2004). | |
| 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 | 409.6 |
| 分子式 | C27H39NO2 |
| CAS号 | 313998-81-1 |
| 稳定性 | ≥ 1 year |
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