Melatonin receptor 1B

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

Function
This gene encodes the MT2 is_associated_with::protein, one of two high-affinity forms of a receptor for is_associated_with::melatonin, the primary hormone secreted by the is_associated_with::pineal gland. This gene product is an is_associated_with::integral membrane protein that is a G-protein coupled, 7-is_associated_with::transmembrane receptor. It is found primarily in the retina and is_associated_with::brain; however, this detection requires RT-PCR. It is thought to participate in light-dependent functions in the is_associated_with::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 is_associated_with::blood sugar level and around a 20 percent elevated risk of developing is_associated_with::type 2 diabetes. MTNR1B mRNA is expressed in human islets, and is_associated_with::immunocytochemistry confirms that it is primarily localized in is_associated_with::beta cells in islets.

MT2R Ligands
The following MT2R ligands have selectivity over MT1R:


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