Negative regulation of melatonin secretion by melatonin receptors in ovine pinealocytes.

Melatonin (MLT) is a biological modulator of circadian and seasonal rhythms and reproduction. The photoperiodic information is detected by retinal photoreceptors and transmitted through nerve transmissions to the pineal gland, where MLT is synthesized and secreted at night into the blood. MLT intera...

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Autores principales: Julie Lépinay, Catherine Taragnat, Jean-Philippe Dubois, Didier Chesneau, Ralf Jockers, Philippe Delagrange, Véronique Bozon
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Publicado: Public Library of Science (PLoS) 2021
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spelling oai:doaj.org-article:ec58cfd362ec4bc6a9bdb0ce84c51a872021-12-02T20:08:55ZNegative regulation of melatonin secretion by melatonin receptors in ovine pinealocytes.1932-620310.1371/journal.pone.0255249https://doaj.org/article/ec58cfd362ec4bc6a9bdb0ce84c51a872021-01-01T00:00:00Zhttps://doi.org/10.1371/journal.pone.0255249https://doaj.org/toc/1932-6203Melatonin (MLT) is a biological modulator of circadian and seasonal rhythms and reproduction. The photoperiodic information is detected by retinal photoreceptors and transmitted through nerve transmissions to the pineal gland, where MLT is synthesized and secreted at night into the blood. MLT interacts with two G protein-coupled receptors, MT1 and MT2. The aim of our work was to provide evidence for the presence of MLT receptors in the ovine pineal gland and define their involvement on melatonin secretion. For the first time, we identified the expression of MLT receptors with the specific 2-[125I]-MLT agonistic radioligand in ovin pinealocytes. The values of Kd and Bmax are 2.24 ± 1.1 nM and 20 ± 6.8 fmol/mg. MLT receptors are functional and inhibit cAMP production and activate ERK1/2 through pertussis toxin-sensitive Gi/o proteins. The MLT receptor antagonist/ inverse agonist luzindole increased cAMP production (189 ± 30%) and MLT secretion (866 ± 13%). The effect of luzindole on MLT secretion was additive with the effect of well-described activators of this pathway such as the β-adrenergic agonist isoproterenol and the α-adrenergic agonist phenylephrine. Co-incubation of all three compounds increased MLT secretion by 1236 ± 199%. These results suggest that MLT receptors are involved in the negative regulation of the synthesis of its own ligand in pinealocytes. While adrenergic receptors promote MLT secretion, MLT receptors mitigate this effect to limit the quantity of MLT secreted by the pineal gland.Julie LépinayCatherine TaragnatJean-Philippe DuboisDidier ChesneauRalf JockersPhilippe DelagrangeVéronique BozonPublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 16, Iss 7, p e0255249 (2021)
institution DOAJ
collection DOAJ
language EN
topic Medicine
R
Science
Q
spellingShingle Medicine
R
Science
Q
Julie Lépinay
Catherine Taragnat
Jean-Philippe Dubois
Didier Chesneau
Ralf Jockers
Philippe Delagrange
Véronique Bozon
Negative regulation of melatonin secretion by melatonin receptors in ovine pinealocytes.
description Melatonin (MLT) is a biological modulator of circadian and seasonal rhythms and reproduction. The photoperiodic information is detected by retinal photoreceptors and transmitted through nerve transmissions to the pineal gland, where MLT is synthesized and secreted at night into the blood. MLT interacts with two G protein-coupled receptors, MT1 and MT2. The aim of our work was to provide evidence for the presence of MLT receptors in the ovine pineal gland and define their involvement on melatonin secretion. For the first time, we identified the expression of MLT receptors with the specific 2-[125I]-MLT agonistic radioligand in ovin pinealocytes. The values of Kd and Bmax are 2.24 ± 1.1 nM and 20 ± 6.8 fmol/mg. MLT receptors are functional and inhibit cAMP production and activate ERK1/2 through pertussis toxin-sensitive Gi/o proteins. The MLT receptor antagonist/ inverse agonist luzindole increased cAMP production (189 ± 30%) and MLT secretion (866 ± 13%). The effect of luzindole on MLT secretion was additive with the effect of well-described activators of this pathway such as the β-adrenergic agonist isoproterenol and the α-adrenergic agonist phenylephrine. Co-incubation of all three compounds increased MLT secretion by 1236 ± 199%. These results suggest that MLT receptors are involved in the negative regulation of the synthesis of its own ligand in pinealocytes. While adrenergic receptors promote MLT secretion, MLT receptors mitigate this effect to limit the quantity of MLT secreted by the pineal gland.
format article
author Julie Lépinay
Catherine Taragnat
Jean-Philippe Dubois
Didier Chesneau
Ralf Jockers
Philippe Delagrange
Véronique Bozon
author_facet Julie Lépinay
Catherine Taragnat
Jean-Philippe Dubois
Didier Chesneau
Ralf Jockers
Philippe Delagrange
Véronique Bozon
author_sort Julie Lépinay
title Negative regulation of melatonin secretion by melatonin receptors in ovine pinealocytes.
title_short Negative regulation of melatonin secretion by melatonin receptors in ovine pinealocytes.
title_full Negative regulation of melatonin secretion by melatonin receptors in ovine pinealocytes.
title_fullStr Negative regulation of melatonin secretion by melatonin receptors in ovine pinealocytes.
title_full_unstemmed Negative regulation of melatonin secretion by melatonin receptors in ovine pinealocytes.
title_sort negative regulation of melatonin secretion by melatonin receptors in ovine pinealocytes.
publisher Public Library of Science (PLoS)
publishDate 2021
url https://doaj.org/article/ec58cfd362ec4bc6a9bdb0ce84c51a87
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AT catherinetaragnat negativeregulationofmelatoninsecretionbymelatoninreceptorsinovinepinealocytes
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