Melatonin: Difference between revisions

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==Pharmacology==

melatonin is a full agonist of melatonin receptor 1 (picomolar binding affinity) and melatonin receptor 2 (nanomolar binding affinity), both of which belong to the class of G-protein coupled receptors (GPCRs).<ref name=":0">Jockers R, Delagrange P, Dubocovich ML, Markus RP, Renault N, Tosini G, et al. (September 2016). "Update on melatonin receptors: IUPHAR Review 20". ''British Journal of Pharmacology''. '''173''' (18): 2702–25. doi:10.1111/bph.13536. PMC 4995287. <nowiki>PMID 27314810</nowiki>.</ref> Melatonin receptors 1 and 2 are both Gi/o-coupled GPCRs, although melatonin receptor 1 is also Gq-coupled.<ref name=":0" /> Melatonin also acts as a high-capacity free radical scavenger within mitochondria which also promotes the expression of antioxidant enzymes such as superoxide dismutase, glutathione peroxidase, glutathione reductase, and catalase via signal transduction through melatonin receptors.<ref name=":0" /> Melatonin is metabolized in the liver by cytochrome P450 enzyme CYP1A2 to 6-hydroxymelatonin. Metabolites are conjugated with sulfuric acid or glucuronic acid for excretion in the urine. 5% of melatonin is excreted in the urine as the unchanged drug.<ref>Tordjman S, Chokron S, Delorme R, Charrier A, Bellissant E, Jaafari N, Fougerou C (April 2017). "Melatonin: Pharmacology, Functions and Therapeutic Benefits". ''Current Neuropharmacology''. '''15''' (3): 434–443. doi:10.2174/1570159X14666161228122115. PMC 5405617. <nowiki>PMID 28503116</nowiki>.</ref> Some of the metabolites formed via the reaction of melatonin with a free radical include cyclic 3-hydroxymelatonin, N1-acetyl-N2-formyl-5-methoxykynuramine (AFMK), and N1-acetyl-5-methoxykynuramine (AMK).<ref name=":0" />

==Subjective effects==

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 ==Pharmacology==
 {{pharmacology}}
-<br />
+melatonin is a full agonist of melatonin receptor 1 (picomolar binding affinity) and melatonin receptor 2 (nanomolar binding affinity), both of which belong to the class of G-protein coupled receptors (GPCRs).<ref name=":0">Jockers R, Delagrange P, Dubocovich ML, Markus RP, Renault N, Tosini G, et al. (September 2016). "Update on melatonin receptors: IUPHAR Review 20". ''British Journal of Pharmacology''. '''173''' (18): 2702–25. doi:10.1111/bph.13536. PMC 4995287. <nowiki>PMID 27314810</nowiki>.</ref> Melatonin receptors 1 and 2 are both G<sub>i/o</sub>-coupled GPCRs, although melatonin receptor 1 is also G<sub>q</sub>-coupled.<ref name=":0" /> Melatonin also acts as a high-capacity free radical scavenger within mitochondria which also promotes the expression of antioxidant enzymes such as superoxide dismutase, glutathione peroxidase, glutathione reductase, and catalase via signal transduction through melatonin receptors.<ref name=":0" /><br />Melatonin is metabolized in the liver by cytochrome P450 enzyme CYP1A2 to 6-hydroxymelatonin. Metabolites are conjugated with sulfuric acid or glucuronic acid for excretion in the urine. 5% of melatonin is excreted in the urine as the unchanged drug.<ref>Tordjman S, Chokron S, Delorme R, Charrier A, Bellissant E, Jaafari N, Fougerou C (April 2017). "Melatonin: Pharmacology, Functions and Therapeutic Benefits". ''Current Neuropharmacology''. '''15''' (3): 434–443. doi:10.2174/1570159X14666161228122115. PMC 5405617. <nowiki>PMID 28503116</nowiki>.</ref> Some of the metabolites formed via the reaction of melatonin with a free radical include cyclic 3-hydroxymelatonin, N1-acetyl-N2-formyl-5-methoxykynuramine (AFMK), and N1-acetyl-5-methoxykynuramine (AMK).<ref name=":0" />
 ==Subjective effects==
 {{Preamble/SubjectiveEffects}}