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抑制剂描述: 产品名称:N-Arachidonyl maleimide 产品别名:见爱必信官网 英文别名:N-Arachidonyl maleimide 靶点:Others CAS:876305-42-9 纯度:≥98% 外观:见爱必信官网 保存方法:Store at -20°C 描述:
N-Arachidonyl Maleimide is a monoacylglycerol lipase (MGL) or MGL-like activity inhibitor.
2-Arachidonoyl glycerol (2-AG), an endogenous agonist of the central cannabinoid and peripheral cannabinoid receptors, is present with high levels in the central nervous system and is the most abundant molecular species of monoacylglycerol found brain. Monoacylglycerol lipase has been identified to hydrolyze 2-AG to arachidonic acid and glycerol, thereby terminating its biological actions.
溶解性:Soluble in DMSO (~30 mg/ml), 100% ethanol (20 mg/ml), DMF (~30 mg/ml), and aqueous buffers (sparingly). 体外研究: Previous study found that N-arachidonyl maleimide could increase the endogenous levels of 2-AG. Moreover, in agonist-stimulated guanosine 5'-O-(3-[(35)S]thio)triphosphate binding assay, N-arachidonyl maleimide was able to raise the potency of 2-AG, but not anandamide (AEA). In addition, unmasking of 2-AG effects of N-arachidonyl maleimide that were only partially reversed by SR141716A gave further support for the existence of non-CB(1), non-CB(2) cannabinoid receptors . 体内研究:Animal study showed that N-arachidonyl maleimide could unmask 2-AG activity in a tetrad of in vivo tests sensitive to the effects of cannabinoids in mice. The efficacy of 2-AG to produce hypothermia was reduced by the treatment of N-arachidonyl maleimide compared with Delta(9)-tetrahydrocannabinol. All tetrad effects were partially CB(1) receptor-mediated because they could be attenuated by CB(1) antagonist SR141716A and in CB(1)(-/-) mice .
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