Melatonin GPCR Family Subtypes and Products

What Are Melatonin Receptors?

Melatonin receptors are a family of G protein-coupled receptors (GPCRs) comprised of MT1 and MT2 receptors. Melatonin receptors bind the endogenous ligand melatonin, a chemical produced within the pineal gland. Melatonin is responsible for regulating a variety of biological processes, such as reproductive and circadian rhythms, sleep, and hormone production. The MT1 receptor is primarily responsible for the sleep promoting effects of melatonin, while the MT2 receptor’s primary role is in the regulation of circadian rhythm following the natural day-night cycle. MT2 receptors also regulate the function of osteoblasts, and have been found to play a role in type 2 diabetes. Research is being done on the potential application of melatonin in the treatment of neuro-disorders like Alzheimer’s, Parkinson’s, addiction, and depression. Melatonin is already commonly used as remedies for jet lag and insomnia.

Melatonin Receptor Information

Clickable Text Interaction

MT1

MT2

MT1 (Melatonin receptor 1A, previously Mel 1A or ML 1A) is a receptor for melatonin. Melatonin is synthesized mainly in the pineal gland but is also made by other organs, such as the retina and the stomach. It is essential to the regulation of the mammalian circadian system and reproductive function. Melatonin receptor agonists may also be useful as a supplement to classical antidepressant treatments.

MT2 receptor, also known as MTNR1B (Melatonin receptor type 1B), is a high affinity receptor for melatonin. It is known to mediate the reproductive and circadian actions of melatonin and is considered as a novel therapeutic target for the development of subtype-selective analogs for the treatment of circadian sleep and mood-related disorders. MT2 receptor is also likely to mediate the interfering with the apoptotic pathway activated by heat shock in HL-60 cells.

Melatonin Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
MelatoninMT1humanCHO-K1C1223-1DC1223-1MC1223-1
MT2humanHEK293T Gαqi5C1224DC1224MC1224
MT2mouseHEK293TCm1224DCm1224MCm1224
MT2ratHEK293TCr1224DCr1224MCr1224