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Updated: Mar 22, 2026
Simultaneous Electrophysiological Recording and Calcium Imaging of Suprachiasmatic Nucleus Neurons
Published on: December 8, 2013
Melatonin receptors as therapeutic targets in the suprachiasmatic nucleus
1a Institut des neurosciences cellulaires et Integratives, INCI UPR 3212 , CNRS and the University of Strasbourg , Strasbourg , France.
Introduction:
Disorders of rhythmicity can cause a variety of pathologies and are known to impair processes involved in metabolism, as well as in cardiovascular disease and cancer. Developing strategies to treat or prevent such diseases is a new challenge for medicine. Rhythms depend on a complex multi-oscillatory circadian network which, in mammals, is hierarchically organized with the suprachiasmatic nuclei (SCN) as master clock. The SCN, thus form an ideal structure for target discovery in circadian pathologies.
Areas Covered:
The development of strategies to treat or prevent disorders of rhythmicity is a new challenge for medicine. Several pharmacological approaches have been suggested, but until now, it has been mostly melatonin (MTL) or MTL-agonists which have demonstrated usefulness in modulating clock activities in vivo. A great number of structurally different MTL receptor ligands have been developed, some of which are already approved and marketed as drugs. The MTL receptor involved in phase-shifting circadian rhythms (chronobiotic effect) is the MT1 subtype.
Expert Opinion:
As the two receptor subtypes for MTL may have divergent functions, the development of highly selective MT1 and MT2 agonists (and antagonists) is key for the discovery of novel therapeutic agents in specifically defined circadian pathologies. The identification of cells expressing the different MTL receptor subtypes should also permit a better understanding of MLT physiology/pharmacology.
Insights
Disorders of rhythmicity impact metabolism, cardiovascular disease, and cancer. Targeting the master clock, the suprachiasmatic nuclei (SCN), and melatonin (MTL) receptors offers new therapeutic strategies for circadian pathologies.
Area of Science:
- Chronobiology
- Pharmacology
- Molecular Medicine
Background:
- Disorders of rhythmicity are linked to various pathologies, including metabolic dysfunction, cardiovascular disease, and cancer.
- Circadian rhythms are regulated by a complex network, with the suprachiasmatic nuclei (SCN) acting as the master clock in mammals.
- The SCN presents an ideal target for developing interventions against circadian rhythm disorders.
Purpose of the Study:
- To review current strategies for treating disorders of rhythmicity.
- To highlight the role of melatonin (MTL) and its receptor ligands in modulating circadian clock activity.
- To emphasize the importance of targeting specific melatonin receptor subtypes for therapeutic development.
Main Methods:
- Review of pharmacological approaches for circadian rhythm modulation.
- Analysis of melatonin (MTL) and its receptor agonists' efficacy in vivo.
- Examination of structurally diverse MTL receptor ligands and their therapeutic applications.
Main Results:
- Melatonin (MTL) and MTL-agonists are currently the primary agents for modulating circadian clock activities.
- Numerous structurally distinct MTL receptor ligands have been developed, with some already approved as drugs.
- The MT1 receptor subtype is identified as the key mediator of the chronobiotic effect in phase-shifting circadian rhythms.
Conclusions:
- Developing highly selective agonists and antagonists for MT1 and MT2 melatonin receptors is crucial for novel therapeutic discovery in specific circadian pathologies.
- Understanding the divergent functions of MTL receptor subtypes may lead to more targeted treatments.
- Identifying cells expressing different MTL receptor subtypes will enhance comprehension of melatonin physiology and pharmacology.
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