N-Arachidonyl Maleimide

- Overview
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    Background
    
    IC50: 140 nMN-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.In vitro: 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 [1].In vivo: 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 [1]. Clinical trial: So far, no clinical study has been conducted.
- Properties
  - Alternative Name
    
    NAM; eicosa-5Z,8Z,11Z,14Z-tetraenyl-1-pyrrole-2,5-dione
    
    CAS Number
    
    876305-42-9
    
    Molecular Formula
    
    C24H35NO2
    
    Molecular Weight
    
    369.5
    
    Appearance
    
    A solution in ethanol. To change the solvent, simply evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide
    
    Storage
    
    Store at -80°C
    
    * For Research Use Only

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N-Arachidonyl Maleimide

Background

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