Next Article in Journal
Cell Signaling Experiments Driven by Optical Manipulation
Next Article in Special Issue
Role of Melatonin in Schizophrenia
Previous Article in Journal / Special Issue
Melatonin-Based Therapeutics for Neuroprotection in Stroke
Article Menu

Export Article

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

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 / Revised: 14 April 2013 / Accepted: 15 April 2013 / Published: 25 April 2013
(This article belongs to the Special Issue Advances in the Research of Melatonin)
View Full-Text   |   Download PDF [378 KB, uploaded 19 June 2014]   |  

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 melatonin receptors; 2-iodomelatonin; alternative radioligands; synthesis; radiolabeling
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

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.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Int. J. Mol. Sci. EISSN 1422-0067 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top