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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
10
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pubmed:dateCreated |
2010-5-12
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pubmed:abstractText |
Novel heterodimer analogues of melatonin were synthesized, when agomelatine (1) and various aryl units are linked via a linear alkyl chain through the methoxy group. The compounds were tested for their actions at melatonin receptors. Several of these ligands are MT(1)-selective with nanomolar or subnanomolar affinity. In addition, while most of the derivatives behave as partial agonists on one or both receptor subtypes, N-[2-(7-{4-[6-(1-methoxycarbonylethyl)naphthalen-2-yloxy]butoxy}naphthalen-1-yl)ethyl]acetamide (36), a subnanomolar MT(1) ligand with an 11-fold preference over MT(2) receptors, is a full antagonist on both receptors. Our results also confirm that the selectivity seen for the MT(1) receptor arises predominantly from steric factors and is not a consequence of the bridging of melatonin receptor dimers.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
1464-3391
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pubmed:author |
pubmed-author:AudinotValérieV,
pubmed-author:BennejeanCarolineC,
pubmed-author:BerthelotPascalP,
pubmed-author:BoutinJean AJA,
pubmed-author:CaignardDaniel HDH,
pubmed-author:ChavattePhilippeP,
pubmed-author:CoumailleauSophieS,
pubmed-author:DelagrangePhilippeP,
pubmed-author:Descamps-FrançoisCaroleC,
pubmed-author:MésangeauChristopheC,
pubmed-author:PérèsBasileB,
pubmed-author:RenardPierreP,
pubmed-author:YousSaïdS
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pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3426-36
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pubmed:meshHeading |
pubmed-meshheading:20444610-Acetamides,
pubmed-meshheading:20444610-Animals,
pubmed-meshheading:20444610-Binding, Competitive,
pubmed-meshheading:20444610-Binding Sites,
pubmed-meshheading:20444610-CHO Cells,
pubmed-meshheading:20444610-Cell Line,
pubmed-meshheading:20444610-Cricetinae,
pubmed-meshheading:20444610-Cricetulus,
pubmed-meshheading:20444610-Dose-Response Relationship, Drug,
pubmed-meshheading:20444610-Drug Design,
pubmed-meshheading:20444610-Melatonin,
pubmed-meshheading:20444610-Protein Binding,
pubmed-meshheading:20444610-Quantitative Structure-Activity Relationship,
pubmed-meshheading:20444610-Receptor, Melatonin, MT1,
pubmed-meshheading:20444610-Receptors, Melatonin
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pubmed:year |
2010
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pubmed:articleTitle |
Design, synthesis and pharmacological evaluation of novel naphthalenic derivatives as selective MT(1) melatoninergic ligands.
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pubmed:affiliation |
Univ Lille Nord de France, F-59000 Lille, France.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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