Journal of Clinical Endocrinology & Metabolism, Vol 76, 295-301, Copyright © 1993 by Endocrine Society

ARTICLES

Melatonin receptors in human hypothalamus and pituitary: implications for circadian and reproductive responses to melatonin

DR Weaver, JH Stehle, EG Stopa and SM Reppert
Laboratory of Developmental Chronobiology, Massachusetts General Hospital, Boston 02114.

Two major physiological roles for the pineal hormone melatonin (MEL) have been identified in vertebrates: the hormone influences circadian rhythmicity and regulates seasonal responses to changes in day length. These effects of MEL are thought to be due to interaction with specific, high affinity MEL receptors in the suprachiasmatic nucleus (SCN) and hypophysial pars tuberalis (PT), respectively. Using the ligand 2-[125I]iodo-MEL ([125I]MEL), we examined putative MEL receptors in these regions in human and monkey tissue specimens by in vitro autoradiography. Specific, high affinity [125I]MEL-binding sites (Kd, 53.3 +/- 13.0 pM) were consistently observed in the human SCN. In contrast, specific [125I]MEL binding was detectable in the PT of only one of the eight human specimens examined. Specific [125I]MEL binding was also detected in the pars distalis of several subjects, but with an inconsistent distribution. In rhesus monkey tissue, MEL receptors were readily detected in the SCN and, as in all other seasonally breeding species examined to date, in the PT. The relative absence of MEL receptors from the human PT suggests that neuroendocrine responses to MEL in humans may occur by fundamentally different mechanisms than those that underlie the photoperiodic regulation of reproduction in seasonally breeding species.

This article has been cited by other articles:

				G BELLIPANNI, F DI MARZO, F BLASI, and A DI MARZO Effects of Melatonin in Perimenopausal and Menopausal Women: Our Personal Experience Ann. N.Y. Acad. Sci., December 1, 2005; 1057(1): 393 - 402. [Abstract] [Full Text] [PDF]

				K. P. Wright Jr, C. Gronfier, J. F. Duffy, and C. A. Czeisler Intrinsic Period and Light Intensity Determine the Phase Relationship between Melatonin and Sleep in Humans J Biol Rhythms, April 1, 2005; 20(2): 168 - 177. [Abstract] [PDF]

				C. Torres-Farfan, H. G. Richter, A. M. Germain, G. J. Valenzuela, C. Campino, P. Rojas-Garcia, M. L. Forcelledo, F. Torrealba, and M. Seron-Ferre Maternal melatonin selectively inhibits cortisol production in the primate fetal adrenal gland J. Physiol., February 1, 2004; 554(3): 841 - 856. [Abstract] [Full Text] [PDF]

				M. Naguib, P. G. Schmid III, and M. T. Baker The Electroencephalographic Effects of IV Anesthetic Doses of Melatonin: Comparative Studies with Thiopental and Propofol Anesth. Analg., July 1, 2003; 97(1): 238 - 243. [Abstract] [Full Text] [PDF]

				C. Torres-Farfan, H. G. Richter, P. Rojas-Garcia, M. Vergara, M. L. Forcelledo, L. E. Valladares, F. Torrealba, G. J. Valenzuela, and M. Seron-Ferre mt1 Melatonin Receptor in the Primate Adrenal Gland: Inhibition of Adrenocorticotropin-Stimulated Cortisol Production by Melatonin J. Clin. Endocrinol. Metab., January 1, 2003; 88(1): 450 - 458. [Abstract] [Full Text] [PDF]

				E. B. Klerman, J. M. Zeitzer, J. F. Duffy, S. B. S. Khalsa, and C. A. Czeisler Absence of an Increase in the Duration of the Circadian Melatonin Secretory Episode in Totally Blind Human Subjects J. Clin. Endocrinol. Metab., July 1, 2001; 86(7): 3166 - 3170. [Abstract] [Full Text] [PDF]

				S. Caglayan, M. Ozata, G. Ozisik, M. Turan, E. Bolu, C. Oktenli, N. Arslan, K. Erbil, D. Gul, and I. C. Ozdemir Plasma Melatonin Concentration before and during Testosterone Replacement in Klinefelter's Syndrome: Relation to Hepatic Indolamine Metabolism and Sympathoadrenal Activity J. Clin. Endocrinol. Metab., February 1, 2001; 86(2): 738 - 743. [Abstract] [Full Text]

				J. M. Zeitzer, N. T. Ayas, S. A. Shea, R. Brown, and C. A. Czeisler Absence of Detectable Melatonin and Preservation of Cortisol and Thyrotropin Rhythms in Tetraplegia J. Clin. Endocrinol. Metab., June 1, 2000; 85(6): 2189 - 2196. [Abstract] [Full Text]

				D. R. Weaver Reproductive Safety of Melatonin: A "Wonder Drug" to Wonder About J Biol Rhythms, December 1, 1997; 12(6): 682 - 689. [Abstract] [PDF]

				E. J. W. Van Someren, C. Lijzenga, M. Mirmiran, and D. F. Swaab Long-Term Fitness Training Improves the Circadian Rest-Activity Rhythm in Healthy Elderly Males J Biol Rhythms, April 1, 1997; 12(2): 146 - 156. [Abstract] [PDF]

				R. Luboshitzky, M. Dharan, D. Goldman, Y. Hiss, P. Herer, and P. Lavie Immunohistochemical Localization of Gonadotropin and Gonadal Steroid Receptors in Human Pineal Glands J. Clin. Endocrinol. Metab., March 1, 1997; 82(3): 977 - 981. [Abstract] [Full Text] [PDF]

				S. M. Yellon Daily Melatonin Treatments Regulate the Circadian Melatonin Rhythm in the Adult Djungarian Hamster J Biol Rhythms, March 1, 1996; 11(1): 4 - 13. [Abstract] [PDF]