rdf:type |
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lifeskim:mentions |
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pubmed:issue |
24
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pubmed:dateCreated |
2007-11-16
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pubmed:abstractText |
A series of trans-N-alkyl-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanemethylamines was synthesized and characterized for binding and function at the melanocortin-4 receptor (MC4R), and several potent benzylamine derivatives were identified. Compound 18 v was found to bind MC4R with potent affinity (K(i)=0.5 nM) and high selectivity over the other melanocortin subtypes and behaved as a functional antagonist (IC(50)=48 nM).
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Amides,
http://linkedlifedata.com/resource/pubmed/chemical/Carboxylic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Chlorine Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclohexanes,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrrolidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Melanocortin, Type 4,
http://linkedlifedata.com/resource/pubmed/chemical/piperazine,
http://linkedlifedata.com/resource/pubmed/chemical/pyrrolidine
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6825-31
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pubmed:meshHeading |
pubmed-meshheading:17964151-Amides,
pubmed-meshheading:17964151-Carboxylic Acids,
pubmed-meshheading:17964151-Chlorine Compounds,
pubmed-meshheading:17964151-Cyclohexanes,
pubmed-meshheading:17964151-Ligands,
pubmed-meshheading:17964151-Molecular Structure,
pubmed-meshheading:17964151-Piperazines,
pubmed-meshheading:17964151-Pyrrolidines,
pubmed-meshheading:17964151-Receptor, Melanocortin, Type 4,
pubmed-meshheading:17964151-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 receptor.
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pubmed:affiliation |
Department of Medicinal Chemistry, Neurocrine Biosciences Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
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pubmed:publicationType |
Journal Article
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