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Design, Synthesis and Biological Evaluation of Novel Arachidonic Acid Derivatives as Highly Potent and Selective Endocannabinoid Transporter Inhibitors

In the present work, we have designed and synthesized a series of arachidonic acid derivatives of general structure I which have been characterized as highly potent and selective inhibitors of anandamide transporter (IC50 = 24−0.8 μM, K i > 1000−5000 nM for CB1 and CB2 cannabinoid receptors and v...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2001-12, Vol.44 (26), p.4505-4508
Main Authors: López-Rodríguez, María L, Viso, Alma, Ortega-Gutiérrez, Silvia, Lastres-Becker, Isabel, González, Sara, Fernández-Ruiz, Javier, Ramos, José A
Format: Article
Language:English
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Summary:In the present work, we have designed and synthesized a series of arachidonic acid derivatives of general structure I which have been characterized as highly potent and selective inhibitors of anandamide transporter (IC50 = 24−0.8 μM, K i > 1000−5000 nM for CB1 and CB2 cannabinoid receptors and vanilloid VR1 receptor). Among them, N-(3-furylmethyl)eicosa-5,8,11,14-tetraenamide deserves special attention as being the most potent endocannabinoid transporter inhibitor (IC50 = 0.8 μM) described to date.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm015545y