Melatonin receptor

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

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

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



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