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|Section2= |Section3= }} ''N''-Arachidonoyl dopamine (NADA) is an endocannabinoid that acts as an agonist of the CB1 receptor and the transient receptor potential V1 (TRPV1) ion channel. Its discovery was described in 2002 by an academic research group from Italy and the USA. It was found in the brain of rats, with especially high concentrations in the hippocampus, cerebellum, and striatum. It activates the TRPV1 channel with an EC50 of approximately of 50nM. The high potency makes it the putative endogenous TRPV1 agonist. Several cytochrome P450 endoplasmic reticulum-bound enzymes, i.e. CYP4A11, CYP4F2, CYP4F3, CYP4Z1, and CYP2U1 in humans,〔Curr Top Med Chem. 2013;13(12):1429-40.〕〔Cardiol Rev. 2014 Jan-Feb;22(1):1-12. doi: 10.1097/CRD.0b013e3182961659. Review〕〔Toxicol Appl Pharmacol. 2012 Oct 1;264(1):73-83. doi: 10.1016/j.taap.2012.07.019〕〔Prostaglandins Leukot Essent Fatty Acids. 2010 Aug;83(2):105-10. doi: 10.1016/j.plefa.2010.06.005〕〔Alcohol Clin Exp Res. 2015 May;39(5):790-7. doi: 10.1111/acer.12697〕 Cyp4a12a and Cyp4a12b ins mice,〔Prostaglandins Other Lipid Mediat. 2015 Jul;120:40-9. 〕 and Cyp4a1, Cyp4a2, Cyp4a3, and Cyp4a8 in rats〔 ω-hydroxylate arachidonic acid to form 20-hydroxyeicosatetraenoic acid (20-HETE) and lesser amounts of 19-hydroxyeicosatetraenoate (19-HETE) (see 20-Hydroxyeicosatetraenoic acid). Rat liver endoplasmic reticulum (i.e. microsome) preparations hydroxylated MADA to 20-hydroxy and lesser amounts of 19-hydroxy arachidonoyl dopamine products; both metabolites as well as 18-hydroxy arachidonoyl dopamine stimulated recombinant human TRPV(1) receptors, being about 10-fold less potent than NADA in doing so.〔Prostaglandins Other Lipid Mediat. 2009 Jan;88(1-2):10-7. doi: 10.1016/j.prostaglandins.2008.08.004〕 These results identify a variety of metabolically modified NADA's as potential TRPV1 agonists and suggest that one or more of the cited cytochrome P450 enzymes may be involved in inactivating NADA. == See also == * Endocannabinoid 抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)』 ■ウィキペディアで「N-Arachidonoyl dopamine」の詳細全文を読む スポンサード リンク
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