(±)-<wbr/>2-<wbr/>Methyl Arachidonoyl-<wbr/>2'-<wbr/>Fluoroethylamide

(±)-2-Methyl Arachidonoyl-2′-Fluoroethylamide

CAT N°: 90055
Price:

From €37.00 €31.45

(±)-2-Methyl arachidonoyl-2′-fluoroethylamide (2-Methyl-2′-fluoro AEA) is an analog of anandamide (AEA) in which the alcohol of the ethanolamide group has been removed and replaced with a fluorine atom. This substitution confers considerably increased binding affinity for the CB1 receptor (Ki = 5.7 nM in rat brain). It also confers additional selectivity, in that binding to CB2 is decreased relative to AEA.{7422} However, the in vivo activity of 2-fluoro AEA is enhanced much less than the binding affinity, because the analog remains a good substrate for FAAH and is rapidly hydrolyzed by this enzyme. 2-Methyl-2′-fluoro AEA is further modified by the addition of an ?-methyl group at the C-2 position of arachidonic acid. This substitution confers enhanced metabolic stability. 2-Methyl-2′-fluoro AEA can fully substitute for ?9-THC in animal self-administration tests, whereas AEA and 2-fluoro AEA cannot.{8152}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • (±)-N-(2-fluoroethyl)-2-methyl-5Z,8Z,11Z,14Z-eicosatetraenamide
  • Correlated keywords
    • anandamides ethanolamides AEA cannabinoids receptors CB1 binding affinity faah fatty acid hydrolases .DELTA.9-THC .DELTA.9THC DELTA9-THC DELTA9THC D9-THC D9THC tetrahydrocannabidiol selective analogs neurochemistry neuroscience fluoromethanandamide
  • Product Overview:
    (±)-2-Methyl arachidonoyl-2′-fluoroethylamide (2-Methyl-2′-fluoro AEA) is an analog of anandamide (AEA) in which the alcohol of the ethanolamide group has been removed and replaced with a fluorine atom. This substitution confers considerably increased binding affinity for the CB1 receptor (Ki = 5.7 nM in rat brain). It also confers additional selectivity, in that binding to CB2 is decreased relative to AEA.{7422} However, the in vivo activity of 2-fluoro AEA is enhanced much less than the binding affinity, because the analog remains a good substrate for FAAH and is rapidly hydrolyzed by this enzyme. 2-Methyl-2′-fluoro AEA is further modified by the addition of an ?-methyl group at the C-2 position of arachidonic acid. This substitution confers enhanced metabolic stability. 2-Methyl-2′-fluoro AEA can fully substitute for ?9-THC in animal self-administration tests, whereas AEA and 2-fluoro AEA cannot.{8152}

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