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Update on melatonin receptors: IUPHAR Review 20
Ralf Jockers1,2,3, Philippe Delagrange4, Margarita L Dubocovich5
1Inserm, U1016, Institut Cochin, Paris, France.
British Journal of Pharmacology
|June 18, 2016
Summary
This review updates knowledge on melatonin receptors (MT1 and MT2), their ligands, genetic variants, and roles in the central nervous system and immune system.
Area of Science:
- Pharmacology
- Molecular Biology
- Genetics
Background:
- Melatonin receptors (MT1 and MT2) are G protein-coupled receptors (GPCRs) crucial for melatonin signaling.
- These receptors, encoded by MTNR1A and MTNR1B genes, play significant roles in various physiological processes.
Purpose of the Study:
- To provide an updated overview of melatonin receptors, ligands, and their associated genetic variants.
- To summarize the structural aspects, dimerization, and physiological functions of melatonin receptors.
- To critically evaluate the antioxidant properties of melatonin and its receptor interactions.
Main Methods:
- Literature review of recent developments in melatonin receptor research.
- Analysis of phenotyping data from melatonin receptor knockout mice.
- Discussion of structural biology, genetic variants, and functional studies.
Main Results:
- Recent advances in melatonin receptor ligands and radioligands have been identified.
- Phenotyping of knockout mice reveals crucial roles in physiology and disease.
- Melatonin receptor dimers and type 2 diabetes-associated genetic variants are of significant interest.
Conclusions:
- Melatonin receptors are vital in the central nervous system and immune system.
- Understanding melatonin receptor structure, function, and genetics is essential for therapeutic development.
- The antioxidant properties of melatonin and its receptor interactions warrant further investigation.

