Melatonin receptor 1B

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Melatonin receptor 1B
Identifiers
SymbolsMTNR1B; MT2; MEL-1B-R
External IDsOMIM600804 MGI2181726 HomoloGene4350 IUPHAR: MT2 GeneCards: MTNR1B Gene
RNA expression pattern
250px
More reference expression data
Orthologs
SpeciesHumanMouse
Entrez4544244701
EnsemblENSG00000134640ENSMUSG00000050901
UniProtP49286P70329
RefSeq (mRNA)NM_005959NM_145712
RefSeq (protein)NP_005950NP_663758
Location (UCSC)Chr 11:
92.34 - 92.36 Mb
Chr 9:
15.61 - 15.62 Mb
PubMed search[1][2]

Melatonin receptor 1B, also known as MTNR1B, is a protein that in humans is encoded by the MTNR1B gene.[1][2]

Function

This gene encodes the MT2 protein, one of two high-affinity forms of a receptor for melatonin, the primary hormone secreted by the pineal gland. This gene product is an integral membrane protein that is a G-protein coupled, 7-transmembrane receptor. It is found primarily in the retina and brain; however, this detection requires RT-PCR. It is thought to participate in light-dependent functions in the retina and may be involved in the neurobiological effects of melatonin.[1]

Clinical significance

Several studies have identified MTNR1B receptor mutations that are associated with increased average blood sugar level and around a 20 percent elevated risk of developing type 2 diabetes.[3][4][5] MTNR1B mRNA is expressed in human islets, and immunocytochemistry confirms that it is primarily localized in beta cells in islets.[4]

MT2R Ligands

The following MT2R ligands have selectivity over MT1R:

  • Compound 3d: antagonist with sub-nM affinity[6]
  • Compound 18f: antagonist and compound 18g partial agonist: sub-nM affinity, >100-fold selectivity over MT1[7]
  • Compound 14: antagonist[8]
  • Compound 13: agonist[9]

See also

References

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External links

  • "Melatonin Receptors: MT2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

Further reading

This article incorporates text from the United States National Library of Medicine, which is in the public domain.


es:Receptor de melatonina 1B
  1. 1.0 1.1 "Entrez Gene: MTNR1B melatonin receptor 1B". 
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  3. "Gene That Regulates Glucose Levels And Increases Risk For Diabetes Identified". ScienceDaily. 2008-06-28. Retrieved 2009-01-18. ; "Body Clock Linked To Diabetes And High Blood Sugar In New Genome-wide Study". ScienceDaily. 2008-12-08. Retrieved 2009-01-18. ; "Is There A Relationship Between Sleep-wake Rhythm And Diabetes? A New Gene Variant Influences Fasting Glucose Levels Via The Melatonin Metabolism". ScienceDaily. 2009-01-16. Retrieved 2009-01-18. 
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  5. Staiger H, Machicao F, Schäfer SA; et al. (2008). "Polymorphisms within the novel type 2 diabetes risk locus MTNR1B determine beta-cell function". PLoS ONE. 3 (12): e3962. doi:10.1371/journal.pone.0003962. PMC 2597741Freely accessible. PMID 19088850. 
  6. Rivara S, Lodola A, Mor M; et al. (2007). "N-(substituted-anilinoethyl)amides: design, synthesis, and pharmacological characterization of a new class of melatonin receptor ligands". J. Med. Chem. 50 (26): 6618–26. doi:10.1021/jm700957j. PMID 18052314. 
  7. Bedini A, Spadoni G, Gatti G; et al. (2006). "Design and synthesis of N-(3,3-diphenylpropenyl)alkanamides as a novel class of high-affinity MT2-selective melatonin receptor ligands". J. Med. Chem. 49 (25): 7393–403. doi:10.1021/jm060850a. PMID 17149869. 
  8. Yous S, Durieux-Poissonnier S, Lipka-Belloli E; et al. (2003). "Design and synthesis of 3-phenyl tetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands". Bioorg. Med. Chem. 11 (5): 753–9. doi:10.1016/S0968-0896(02)00473-X. PMID 12538005. 
  9. Mattson RJ, Catt JD, Keavy D; et al. (2003). "Indanyl piperazines as melatonergic MT2 selective agents". Bioorg. Med. Chem. Lett. 13 (6): 1199–202. doi:10.1016/S0960-894X(03)00090-8. PMID 12643943.