Melatonin receptors (MTNRs) are a group of high-affinity Gi/G0 protein-coupled receptors, which bind the hormone melatonin to regulate a wide variety of physiological processes. Three types of melatonin receptors have been cloned, including MTNR1A, MTNR1B, and MTNR1C. In humans and other mammals, MTNR1A and MTNR1B are present, however, MTNR1C has been identified in amphibia and birds. MTNR1C seems to be the hamster homolog of human quinone reductase 2 and is therefore not considered within the GPCRs. MTNR1A and MTNR1B are widely distributed in the brain (especially in the suprachiasmatic nucleus) and in the retina with high concentrations, while these receptors are detected in the kidney, heart, lung and liver with lower levels. MTNR1A modulates the circadian, neuronal firing, arterial vasocon-striction, cell proliferation in cancer cells, and reproductive and metabolic functions. MTNR1B is mainly expressed in the retina, suggesting the effect on the circadian rhythms. Furthermore, activation of MTNR1B inhibits dopamine release in retina, induces vasodilation and inhibition of leukocyte rolling in arterial beds, enhances immune responses, regulates proliferation and differentiation of osteoblasts and involves in the pathogenesis of type 2 diabetes.
Here show partial members of MTNRs, including MTNR1A and MTNR1B. There are a lot of agonists and antagonists for MTNR1A and MTNR1B have been identified, which can enhance or reduce the melatonin-mediated responses to affect the physiologic processes. Further studies about the MTNRs mediated specific functional responses in target tissues are beneficial for the design and development of novel therapeutic agent.
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