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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
23
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pubmed:dateCreated |
2007-11-6
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pubmed:abstractText |
A series of trans-4-phenylpyrrolidine-3-carboxamides were synthesized and characterized as potent ligands of the human melanocortin-4 receptor. Interestingly, a pair of diastereoisomers 20f-1 and 20f-2 displayed potent functional agonist and antagonist activity, respectively. Thus, the 3S,4R-compound 20f-1 possessed a K(i) of 11nM and an EC(50) of 24nM, while its 3R,4S-isomer 20f-2 exhibited a K(i) of 8.6 and an IC(50) of 65nM. Both compounds were highly selective over other melanocortin receptor subtypes. The MC4R agonist 20f-1 also demonstrated efficacy in diet-induced obese rats.
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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 |
Dec
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:ArellanoMelissaM,
pubmed-author:ChenCaroline WCW,
pubmed-author:FleckBeth ABA,
pubmed-author:FosterAlan CAC,
pubmed-author:HoareSam RSR,
pubmed-author:JiangWanlongW,
pubmed-author:MarinkovicDraganD,
pubmed-author:MarkisonStacyS,
pubmed-author:TranJoe AJA,
pubmed-author:TucciFabio CFC,
pubmed-author:WenJennyJ,
pubmed-author:XXX
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pubmed:issnType |
Electronic
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pubmed:day |
1
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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 |
6546-52
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pubmed:meshHeading |
pubmed-meshheading:17933528-Animals,
pubmed-meshheading:17933528-Biological Availability,
pubmed-meshheading:17933528-Humans,
pubmed-meshheading:17933528-Injections, Intravenous,
pubmed-meshheading:17933528-Protein Binding,
pubmed-meshheading:17933528-Pyrrolidines,
pubmed-meshheading:17933528-Rats,
pubmed-meshheading:17933528-Rats, Zucker,
pubmed-meshheading:17933528-Receptor, Melanocortin, Type 4
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pubmed:year |
2007
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pubmed:articleTitle |
Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human 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,
Comparative Study
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