The Annual Review of Pharmacology and Toxicology· 2015Q1· Review
MT1 and MT2 Melatonin Receptors: A Therapeutic Perspective
- 630citations
- Q1SCImago
- 2015year
Short summary
Melatonin's beneficial effects on sleep, mood, and neuroprotection are mediated through MT1 and MT2 receptors, leading to the development of novel agonists like agomelatine and ramelteon for treating insomnia, circadian disorders, and other conditions.
AI-generated from the title and abstract; the full text is not read.
Key points
- Melatonin acts via MT1 and MT2 G protein-coupled receptors.
- These receptors are involved in sleep, circadian rhythms, mood, learning, memory, neuroprotection, drug abuse, and cancer.
- Novel melatonin agonists (Circadin®, agomelatine, ramelteon, tasimelteon) have been developed for therapeutic use.
- Selective ligands for MT1 or MT2 receptors could lead to improved treatments.
AI-generated from the title and abstract; the full text is not read.
Abstract
Melatonin, or 5-methoxy-N-acetyltryptamine, is synthesized and released by the pineal gland and locally in the retina following a circadian rhythm, with low levels during the day and elevated levels at night. Melatonin activates two high-affinity G protein-coupled receptors, termed MT1 and MT2, to exert beneficial actions in sleep and circadian abnormality, mood disorders, learning and memory, neuroprotection, drug abuse, and cancer. Progress in understanding the role of melatonin receptors in the modulation of sleep and circadian rhythms has led to the discovery of a novel class of melatonin agonists for treating insomnia, circadian rhythms, mood disorders, and cancer. This review describes the pharmacological properties of a slow-release melatonin preparation (i.e., Circadin®) and synthetic ligands (i.e., agomelatine, ramelteon, tasimelteon), with emphasis on identifying specific therapeutic effects mediated through MT1 and MT2 receptor activation. Discovery of selective ligands targeting the MT1 or the MT2 melatonin receptors may promote the development of novel and more efficacious therapeutic agents.
The authors' abstract, as published at the source. The Annual Review of Pharmacology and Toxicology, 2015 · DOI ↗
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Field: Endocrine and Autonomic Systems
Endocrine and Autonomic SystemsNeuroscience