Int. J. Mol. Sci. 2013, 14(5), 8948-8962; doi:10.3390/ijms14058948
Article

New Radioligands for Describing the Molecular Pharmacology of MT1 and MT2 Melatonin Receptors

1 BPMC, Institut de Recherches SERVIER, 125 chemin de Ronde, Croissy-sur-Seine 78290, France 2 Celerion Switzerland AG Allmendstrasse 32, Fehraltorf CH-8320, Switzerland 3 Technologie SERVIER, 27 rue Vignat, Orléans 45000, France 4 ANAWA Trading SA, Unterdorfstrasse 21, Wangen CH-8602, Switzerland 5 Université Lille Nord de France, F-59000 Lille, France & UDSL, EA GRIIOT, UFR Pharmacie, Lille F-59000, France 6 DIVERCHIM, 6 Rue du Noyer, Roissy 95700, France 7 Institut de Chimie Organique et Analytique, UMR CNRS 7311, Université d'Orléans, rue de Chartres, Orléans 45067, France 8 Unité de Recherches et Découvertes en Neurosciences, Institut de Recherches SERVIER, 125 chemin de Ronde, Croissy-sur-Seine 78290, France
* Author to whom correspondence should be addressed.
Received: 16 March 2013; in revised form: 14 April 2013 / Accepted: 15 April 2013 / Published: 25 April 2013
(This article belongs to the Special Issue Advances in the Research of Melatonin)
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Abstract: Melatonin receptors have been studied for several decades. The low expression of the receptors in tissues led the scientific community to find a substitute for the natural hormone melatonin, the agonist 2-[125I]-iodomelatonin. Using the agonist, several hundreds of studies were conducted, including the discovery of agonists and antagonists for the receptors and minute details about their molecular behavior. Recently, we attempted to expand the panel of radioligands available for studying the melatonin receptors by using the newly discovered compounds SD6, DIV880, and S70254. These compounds were characterized for their affinities to the hMT1 and hMT2 recombinant receptors and their functionality in the classical GTPS system. SD6 is a full agonist, equilibrated between the receptor isoforms, whereas S70254 and DIV880 are only partial MT2 agonists, with Ki in the low nanomolar range while they have no affinity to MT1 receptors. These new tools will hopefully allow for additions to the current body of information on the native localization of the receptor isoforms in tissues.
Keywords: melatonin receptors; 2-iodomelatonin; alternative radioligands; synthesis; radiolabeling

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MDPI and ACS Style

Legros, C.; Matthey, U.; Grelak, T.; Pedragona-Moreau, S.; Hassler, W.; Yous, S.; Thomas, E.; Suzenet, F.; Folleas, B.; Lefoulon, F.; Berthelot, P.; Caignard, D.-H.; Guillaumet, G.; Delagrange, P.; Brayer, J.-L.; Nosjean, O.; Boutin, J.A. New Radioligands for Describing the Molecular Pharmacology of MT1 and MT2 Melatonin Receptors. Int. J. Mol. Sci. 2013, 14, 8948-8962.

AMA Style

Legros C, Matthey U, Grelak T, Pedragona-Moreau S, Hassler W, Yous S, Thomas E, Suzenet F, Folleas B, Lefoulon F, Berthelot P, Caignard D-H, Guillaumet G, Delagrange P, Brayer J-L, Nosjean O, Boutin JA. New Radioligands for Describing the Molecular Pharmacology of MT1 and MT2 Melatonin Receptors. International Journal of Molecular Sciences. 2013; 14(5):8948-8962.

Chicago/Turabian Style

Legros, Céline; Matthey, Ulrich; Grelak, Teresa; Pedragona-Moreau, Sandrine; Hassler, Werner; Yous, Saïd; Thomas, Emmanuel; Suzenet, Franck; Folleas, Benoît; Lefoulon, François; Berthelot, Pascal; Caignard, Daniel-Henri; Guillaumet, Gérald; Delagrange, Philippe; Brayer, Jean-Louis; Nosjean, Olivier; Boutin, Jean A. 2013. "New Radioligands for Describing the Molecular Pharmacology of MT1 and MT2 Melatonin Receptors." Int. J. Mol. Sci. 14, no. 5: 8948-8962.

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