Functional MT1 and MT2 Melatonin Receptors in Mammals

Endocrine. 2005 Jul;27(2):101-10. doi: 10.1385/ENDO:27:2:101.


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 G protein-coupled receptors viewed as potential targets for drug discovery. MT1 melatonin receptors modulate neuronal firing, arterial vasocon-striction, cell proliferation in cancer cells, and reproductive and metabolic functions. Activation 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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Adrenal Glands / physiology
  • Animals
  • Cardiovascular Physiological Phenomena
  • Circadian Rhythm / physiology
  • Gonads / physiology
  • Humans
  • Hypothalamo-Hypophyseal System / physiology
  • Immune System / physiology
  • Mammals / physiology*
  • Neoplasms / physiopathology
  • Receptor, Melatonin, MT1 / metabolism
  • Receptor, Melatonin, MT1 / physiology*
  • Receptor, Melatonin, MT2 / metabolism
  • Receptor, Melatonin, MT2 / physiology*


  • Receptor, Melatonin, MT1
  • Receptor, Melatonin, MT2