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Functional MT1 and MT2 melatonin receptors in mammals

Functional MT1 and MT2 melatonin receptors in mammals 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. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Endocrine Springer Journals

Functional MT1 and MT2 melatonin receptors in mammals

Dubocovich, Margarita; Markowska, Magdalena
Endocrine , Volume 27 (2) – May 24, 2007
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References (150)

Publisher
Springer Journals
Copyright
Copyright © 2005 by Humana Press Inc.
Subject
Medicine & Public Health; Endocrinology; Diabetes; Science, general; Internal Medicine
ISSN
1355-008X
eISSN
1559-0100
DOI
10.1385/ENDO:27:2:101
pmid
16217123
Publisher site
See Article on Publisher Site

Abstract

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.

Journal

Endocrine – Springer Journals

Published: May 24, 2007

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