, Volume 27, Issue 2, pp 101–110 | Cite as

Functional MT1 and MT2 melatonin receptors in mammals

  • Margarita L. DubocovichEmail author
  • Magdalena Markowska


Melatonin, dubbed the hormone of darkness, is known to regulate a wide variety of physiological processes in mammals. This review describes well-defined functional responses mediated through activation of high-affinity MT1 and MT2 proteinteoupled receptors viewed as potential targets for drug discovery. MT1 melatonin receptors modulate neuronal firing, arterial vasoconstriction, cell proliferation in cancer cells, and reproductive and metabolic functions. Ativation of MT2 melatonin receptors phase shift circadian rhythms of neuronal firing in the suprachiasmatic nucleus, inhibit dopamine release in retina, induce vasodilation and inhibition of leukocyte rolling in arterial beds, and enhance immune responses. The melatonin-mediated responses elicited by activation of MT1 and MT2 native melatonin receptors are dependent on circadian time, duration and mode of exposure to endogenous or exogenous melatonin, and functional receptor sensitivity. Together, these studies underscore the importance of carefully linking each melatonin receptor type to specific functional responses in target tissues to facilitate the design and development of novel therapeutic agent.

Key Words

MT1 and MT2 melatonin receptors MT3 site luzindole 4P-PDOT MT1 and MT2 knockout mice 


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Copyright information

© Humana Press Inc. 2005

Authors and Affiliations

  1. 1.Department of Molecular Pharmacology & Biological Chemistry, Department of Psychiatry & Behavioral SciencesNorthwestern University Feinberg School of Medicine Center for Drug Discovery and Chemical Biology Northwestern UniversityChicago

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