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 Mel1A or MTNR1A) and MT2 (or Mel1B or MTNR1B) receptor subtypes are present in humans and other mammals,[2] while an additional melatonin receptor subtype MT3 (or Mel1C or MTNR1C) has been identified in amphibia and birds.[3]
Contents
Expression patterns[edit]
In mammals, melatonin receptors are found in the brain and some peripheral organs. However, there is considerable variation in the density and location of MT receptor expression between species.[4]
MT1[edit]
In humans, The MT1 subtype is expressed in the pars tuberalis of the pituitary gland and the suprachiasmatic nuclei of the hypothalamus.
MT2[edit]
The MT2 subtype is expressed in the retina. MT2 receptor mRNA has not been detected by in situ hybridization in the rat suprachiasmatic nucleus or pars tuberalis.[5]
MT3[edit]
The MT3 subtype of many non-mammalian vertebrates is expressed in various brain areas.[3]
MT Receptor function[edit]
MT1[edit]
In humans, The MT1 subtype's expression in the pars tuberalis of the pituitary gland and suprachiasmatic nuclei of the hypothalamus is indicative of melatonin's circadian and reproductive functional involvement.
MT2[edit]
In humans, the MT2 subtype's expression in the retina is suggestive of melatonin's effect on the mammalian retina occurring through this receptor. Research suggests that melatonin acts to inhibit the Ca2+-dependent release of dopamine.[5] Melatonin's action in the retina is believed to affect several light-dependent functions, including phagocytosis and photopigment disc shedding.[6]
MT3[edit]
Selective Ligands[edit]
Agonists[edit]
- 6-Hydroxymelatonin
- Agomelatine
- GR-196,429
- Melatonin
- N-Acetylserotonin
- Piromelatine
- Ramelteon
- Tasimelteon
- TIK-301 (LY-156,735)[7]
Antagonists[edit]
See also[edit]
References[edit]
- ^ 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.
- ^ Reppert SM, Weaver DR, Godson C (1996). "Melatonin receptors step into the light: cloning and classification of subtypes". Trends Pharmacol. Sci. 17 (3): 100–02. doi:10.1016/0165-6147(96)10005-5. PMID 8936344.
- ^ 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.
- ^ 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.
- ^ a b Reppert SM, Godson C, Mahle CD, Weaver DR, Slaugenhaupt SA, Gusella JF (September 1995). "Molecular characterization of a second melatonin receptor expressed in human retina and brain: the Mel1b melatonin receptor". Proc. Natl. Acad. Sci. U.S.A. 92 (19): 8734–38. Bibcode:1995PNAS...92.8734R. doi:10.1073/pnas.92.19.8734. PMC 41041
. PMID 7568007. - ^ Besharse JC, Dunis DA (March 1983). "Methoxyindoles and photoreceptor metabolism: activation of rod shedding". Science. 219 (4590): 1341–43. Bibcode:1983Sci...219.1341B. doi:10.1126/science.6828862. PMID 6828862.
- ^ Nickelsen T, Samel A, Vejvoda M, Wenzel J, Smith B, Gerzer R (September 2002). "Chronobiotic effects of the melatonin agonist LY 156735 following a simulated 9h time shift: results of a placebo-controlled trial". Chronobiol. Int. 19 (5): 915–36. doi:10.1081/cbi-120014108. PMID 12405554.
External links[edit]
- "Melatonin Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
- Melatonin Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)
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