Melatonin receptor

melatonin receptor 1A
Identifiers
Symbol	MTNR1A
Entrez	4543
HUGO	7463
OMIM	600665
RefSeq	NM_005958
UniProt	P48039
Other data
Locus	Chr. 4 q35.1

melatonin receptor 1B
Identifiers
Symbol	MTNR1B
Entrez	4544
HUGO	7464
OMIM	600804
RefSeq	NM_005959
UniProt	P49286
Other data
Locus	Chr. 11 q21-q22

A melatonin receptor is a G protein-coupled receptor (GPCR) which binds melatonin.^[1]

Three types of melatonin receptor have been cloned. The MT₁ (or Mel_1A or MTNR1A) and MT₂ (or Mel_1B or MTNR1B) receptor subtypes are present in humans and other mammals^[2], while an additional melatonin receptor subtype MT₃ (or Mel_1C or MTNR1C) has been identified in amphibia and birds.^[3]

Expression patterns

In mammals, melatonin receptors are found in the brain and some peripheral organs. However, there is considerable variation in the density and location of the expression of melatonin receptors between species.^[4] The MT₁ subtype is present in the pars tuberalis of the pituitary gland and the suprachiasmatic nuclei of the hypothalamus. The MT₂ subtype is mainly present in the retina. The MT₃ subtype of many non-mammalian vertebrates is expressed in various brain areas.^[3]

Selective Ligands

Agonists

• Agomelatine
• Melatonin
• Ramelteon
• Tasimelteon
• LY-156,735^[5]

Antagonists

• Afobazole
• Luzindole - N-Acetyl-2-benzyltryptamine, CAS# 117946-91-5

See also

Discovery and development of melatonin receptor agonists

References

1. ^ Reppert SM (1997). "Melatonin receptors: molecular biology of a new family of G protein-coupled receptors". J. Biol. Rhythms 12 (6): 528–31. doi:10.1177/074873049701200606. PMID 9406026. 
2. ^ Reppert SM, Weaver DR, Godson C (1996). "Melatonin receptors step into the light: cloning and classification of subtypes". Trends Pharmacol. Sci. 17 (3): 100–2. doi:10.1016/0165-6147(96)10005-5. PMID 8936344. 
3. ^ ^{a b} Sugden D, Davidson K, Hough KA, Teh MT (2004). "Melatonin, melatonin receptors and melanophores: a moving story". Pigment Cell Res. 17 (5): 454–60. doi:10.1111/j.1600-0749.2004.00185.x. PMID 15357831. 
4. ^ Morgan PJ, Barrett P, Howell HE, Helliwell R (1994). "Melatonin receptors: localization, molecular pharmacology and physiological significance". Neurochem. Int. 24 (2): 101–46. doi:10.1016/0197-0186(94)90100-7. PMID 8161940. 
5. ^ Nickelsen T, Samel A, Vejvoda M, Wenzel J, Smith B, Gerzer R. Chronobiotic effects of the melatonin agonist LY 156735 following a simulated 9h time shift: results of a placebo-controlled trial. Chronobiology International. 2002 Sep;19(5):915-36. PMID 12405554

External links

• "Melatonin Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1291. 
• MeSH Melatonin+Receptors