Puneet Varma (Editor)

Melatonin receptor 1B

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Species
  
Human

Entrez
  
4544

Human
  
Mouse

Ensembl
  
ENSG00000134640

Melatonin receptor 1B

Aliases
  
MTNR1B, FGQTL2, MEL-1B-R, MT2, Melatonin receptor 1B

External IDs
  
MGI: 2181726 HomoloGene: 4350 GeneCards: MTNR1B

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

Contents

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.

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. MTNR1B mRNA is expressed in human islets, and immunocytochemistry confirms that it is primarily localized in beta cells in islets.

Ligands

The following MT2R ligands have selectivity over MT1R:

  • Compound 3d: antagonist with sub-nM affinity
  • Compound 18f: antagonist and compound 18g partial agonist: sub-nM affinity, >100-fold selectivity over MT1
  • Compound 14: antagonist
  • Compound 13: agonist
  • References

    Melatonin receptor 1B Wikipedia