Melatonin receptor 1B
Lua error in Module:Infobox_gene at line 33: attempt to index field 'wikibase' (a nil value). Melatonin receptor 1B, also known as MTNR1B, is a protein that in humans is encoded by the MTNR1B gene.[1][2]
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.[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]
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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Further reading
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External links
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This article incorporates text from the United States National Library of Medicine, which is in the public domain.
