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À propos de : Design, Synthesis and BiologicalEvaluation of Novel Arachidonic AcidDerivatives as Highly Potent andSelective Endocannabinoid TransporterInhibitors        

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  • Design, Synthesis and BiologicalEvaluation of Novel Arachidonic AcidDerivatives as Highly Potent andSelective Endocannabinoid TransporterInhibitors
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  • In the present work, we have designed and synthesized a series of arachidonic acid derivatives of generalstructure I which have been characterized as highly potentand selective inhibitors of anandamide transporter (IC50 = 24−0.8 μM, Ki> 1000−5000 nM for CB1 and CB2 cannabinoidreceptors and vanilloid VR1 receptor). Among them, N-(3-furylmethyl)eicosa-5,8,11,14-tetraenamide deserves special attention as being the most potent endocannabinoid transporterinhibitor (IC50 = 0.8 μM) described to date.
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