| CAS NO: | 1101854-58-3 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 520.49 |
| Cas No. | 1101854-58-3 |
| Formula | C27H24N2O9 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥20.35 mg/mL in DMSO |
| Chemical Name | (4-nitrophenyl) 4-[bis(1,3-benzodioxol-5-yl)-hydroxymethyl]piperidine-1-carboxylate |
| Canonical SMILES | C1CN(CCC1C(C2=CC3=C(C=C2)OCO3)(C4=CC5=C(C=C4)OCO5)O)C(=O)OC6=CC=C(C=C6)[N+](=O)[O-] |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
JZL184是一种有效的MAGL选择性抑制剂[1].
单酰基甘油脂肪酶(MAGL)是丝氨酸水解酶超家族的膜相关成员,可水解内源性大麻素2-花生四烯酸甘油酯(2-AG)和胞内甘油三酯贮存.
JZL184是一种有效的MAGL选择性抑制剂.在小脑Purkinje神经元中,JZL184(40-120 min)可以剂量依赖的方式延迟去极化诱导的激发抑制(DSE),该过程由CB1受体介导.在海马CA1区锥体神经元中,JZL184(100 nM)可显著延迟去极化诱导的抑制抑制(DSI),该过程由CB1受体激活介导.在小鼠小脑切片中,JZL184(100 nM)可显著增强Purkinje神经元中2-AG(10 μM)诱导的EPSC抑制.这些结果表明,MAGL是2-AG代谢的主要机制[1].
在小鼠中,JZL184可抑制2-AG水解,IC50值为8 nM,并能增加8倍的脑2-AG量.JZL184处理的小鼠具有CB1依赖的行为,包括镇痛\运动不足和体温过低[1].在大鼠中,在高水平环境厌恶下,JZL184(8 mg/kg)通过抑制MGL介导的2-AG水解,表现出抗焦虑样作用[3].在大鼠中,JZL184具有镇痛作用,在早期和晚期福尔马林疼痛下的ED50值分别为0.06和0.03 μM[4].
参考文献：
[1]. Pan B, Wang W, Long JZ, et al. Blockade of 2-arachidonoylglycerol hydrolysis by selective monoacylglycerol lipase inhibitor 4-nitrophenyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate (JZL184) Enhances retrograde endocannabinoid signaling. J Pharmacol Exp Ther, 2009, 331(2): 591-597.
[2]. Long JZ, Li W, Booker L, et al. Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects. Nat Chem Biol, 2009, 5(1): 37-44.
[3]. Sciolino NR, Zhou W, Hohmann AG. Enhancement of endocannabinoid signaling with JZL184, an inhibitor of the 2-arachidonoylglycerol hydrolyzing enzyme monoacylglycerol lipase, produces anxiolytic effects under conditions of high environmental aversiveness in rats. Pharmacol Res, 2011, 64(3): 226-234.
[4]. Guindon J, Guijarro A, Piomelli D, et al. Peripheral antinociceptive effects of inhibitors of monoacylglycerol lipase in a rat model of inflammatory pain. Br J Pharmacol, 2011, 163(7): 1464-1478.
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