Melatonin GPCR Assays
Background of Melatonin Receptors
Melatonin receptors (MTs) belong to the G-protein-coupled receptor (GPCR) family. They can bind melatonin specifically and participate in the regulation of the biological clock. There are three important members in this family: MT1, MT2, and MT3. MT1 and MT2 can be found in human bodies, while MT3 is mostly in amphibia. These receptors can do benefits in mood and memory disorders, sleep abnormalities, and others.
Fig.1. XFEL crystal structure of MT1 receptor in complex with ramelteon. (Stauch, 2019)
Distribution and Function of Melatonin Receptors
MT receptors inhabit the whole human body, they can be found in the retina, brain, kidneys, and many other vital organs. These receptors are essential in the signal pathways of a pineal gland secretion known as melatonin and contribute to the sleep-wake cycle regulation.
Subtypes and Mechanisms of Melatonin Receptors
There are two members of the MT receptors family in mammals, termed MT1 and MT2. They exert beneficial actions in anxiolytic, antinociceptive, antidepressant, and improve memory abilities.
| Receptor | Gene | Mechanism | Agonists | Antagonists |
| MT1 receptor | MTNR1A |
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| MT2 receptor | MTNR1B |
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| MT3 receptor | MTNR1C |
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Assay List of Melatonin Receptors
Creative Biolabs can provide a range of assays of melatonin receptors. You can choose the assay in the list or contact us for more information:
Published Data
| Paper Title | Melatonin receptor depletion suppressed hCG-induced testosterone expression in mouse Leydig cells |
| Journal | Cellular & Molecular Biology Letters |
| Published | 2019 |
| Abstract | Melatonin is a neurohormone secreted by the pineal gland. It is involved in many physiological activities, including reproductive regulation, sexual maturation, neuroendocrine, immune regulation, and anti-aging. Melatonin receptors MT1 and MT2 can act as homo- or heterodimers in different tissues, organs, or species to regulate cellular physiological activities and activate different signaling cascades. Leydig cells are the primary cells located between the seminiferous tubules of the testis and are responsible for the synthesis and secretion of testosterone. Leydig cells are responsible for promoting the development of male reproductive organs, and maintaining spermatogenesis and secondary sexual characteristics. Melatonin receptors are abundantly expressed on the surface of mesenchymal cells. In addition, more and more evidence shows that melatonin receptors are involved in reproductive regulation to a certain extent. In this study, the researchers explored whether the melatonin receptor plays a role in the synthesis of testosterone by Leydig cells in mice and whether it does so by regulating the expression of steroidogenic enzymes. |
| Result |
Through establishing siRNA-mediated melatonin receptor knockdown cell mLTC-1, researchers detect the expression of related factors and cellular processes including apoptosis and endoplasmic reticulum stress, and discover the potential role of melatonin receptor-mediated signaling pathways in reproductive regulation. Data showed that knockdown of the melatonin receptor significantly suppressed hCG-induced expression of genes related to testosterone synthesis and steroidogenesis, proving that the melatonin receptor plays different roles in the three pathways of endoplasmic reticulum stress (Perk, ATF6, IRE1). These results suggest that the melatonin receptors MTNR1A and MTNR1B are critical for suppressing hCG-induced ER stress and apoptosis. The study demonstrates that the mammalian melatonin receptors MT1 and MT2 participate in testosterone synthesis by mediating multiple cellular pathways.
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Fig.2. Effect of melatonin receptor knockdown on endoplasmic reticulum stress in Leydig cells. (Gao, 2019)
References
- Stauch, B.; et al. Structural basis of ligand recognition at the human MT1 melatonin receptor. Nature. 2019, 569(7755): 284-288.
- Gao, Y.; et al. Melatonin receptor depletion suppressed hCG-induced testosterone expression in mouse Leydig cells. Cellular & Molecular Biology Letters. 2019, 24: 21.
