International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, Classification, and Pharmacology of G Protein-Coupled Melatonin Receptors

Jul 8, 2010Pharmacological reviews

Naming, types, and drug effects of melatonin receptors that work through G proteins

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Abstract

Melatonin concentrations in circulation follow a circadian rhythm, peaking at night.

  • Melatonin is synthesized mainly in the pineal gland and retina, with additional production in various tissues.
  • High nighttime levels of melatonin provide timing cues to target tissues that have melatonin receptors.
  • Melatonin receptors, specifically MT(1) and MT(2), may influence daily and seasonal rhythms of physiology and behavior.
  • These receptors are potential therapeutic targets for conditions such as insomnia, depression, cardiovascular diseases, and cancer.
  • Current research focuses on characterizing these receptors and developing ligands for treating multiple illnesses.

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