Melatonin Receptor 2 (MT2) Antibodies
The melatonin MT₂ receptor, formerly known as Mel1b and encoded by MTNR1B, is a class A G protein-coupled receptor activated by the endogenous hormone melatonin. It couples predominantly to Gi/o, inhibiting adenylyl cyclase and reducing intracellular cAMP. MT₂ expression has been reported in the retina, selected brain regions, and pancreatic islets. Its activation contributes to circadian phase shifting, retinal physiology, and the regulation of glucose homeostasis. Genetic variants in MTNR1B are associated with altered fasting glucose levels and an increased risk of type 2 diabetes. Melatonin stimulation can induce β-arrestin recruitment, receptor desensitization, and internalization, with responses depending on the cellular context and duration of exposure. The MT₂-preferring ligand 4P-PDOT is widely used experimentally as an antagonist, although agonist activity has been observed in some assays. Clinically used agonists that activate both MT₁ and MT₂ include ramelteon for insomnia and tasimelteon for non-24-hour sleep–wake disorder, with indications varying by country. No drug selectively targeting MT₂ over MT₁ is currently approved for therapeutic use. For more information on MT2 receptor pharmacology please refer to the IUPHAR database. For further reading refer to:
Dubocovich ML, Delagrange P, Krause DN, Sugden D, Cardinali DP, Olcese J. (2010) International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, classification, and pharmacology of G protein-coupled melatonin receptors. Pharmacol Rev, 62 (3): 343-80. [PMID:20605968]