Melatonin receptor 1B

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Melatonin receptor 1B
Symbols MTNR1B ; FGQTL2; MEL-1B-R; MT2
External IDs OMIM600804 MGI2181726 HomoloGene4350 IUPHAR: 288 ChEMBL: 1946 GeneCards: MTNR1B Gene
RNA expression pattern
PBB GE MTNR1B 208516 at tn.png
More reference expression data
Species Human Mouse
Entrez 4544 244701
Ensembl ENSG00000134640 ENSMUSG00000050901
UniProt P49286 Q3SXF8
RefSeq (mRNA) NM_005959 NM_145712
RefSeq (protein) NP_005950 NP_663758
Location (UCSC) Chr 11:
92.97 – 92.99 Mb
Chr 9:
15.82 – 15.87 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]


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[edit]

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[edit]

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[edit]


  1. ^ a b "Entrez Gene: MTNR1B melatonin receptor 1B". 
  2. ^ 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): 8734–8. doi:10.1073/pnas.92.19.8734. PMC 41041. PMID 7568007. 
  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. 
  4. ^ a b Prokopenko I, Langenberg C, Florez JC, et al. (January 2009). "Variants in MTNR1B influence fasting glucose levels". Nat. Genet. 41 (1): 77–81. doi:10.1038/ng.290. PMC 2682768. PMID 19060907. ; Lyssenko V, Nagorny CL, Erdos MR, et al. (January 2009). "Common variant in MTNR1B associated with increased risk of type 2 diabetes and impaired early insulin secretion". Nat. Genet. 41 (1): 82–8. doi:10.1038/ng.288. PMID 19060908. ; Bouatia-Naji N, Bonnefond A, Cavalcanti-Proença C, et al. (January 2009). "A variant near MTNR1B is associated with increased fasting plasma glucose levels and type 2 diabetes risk". Nat. Genet. 41 (1): 89–94. doi:10.1038/ng.277. PMID 19060909. 
  5. ^ Staiger H, Machicao F, Schäfer SA, et al. (2008). Maedler K, ed. "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 2597741. 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. 

External links[edit]

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

Further reading[edit]

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