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rdf:type |
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lifeskim:mentions |
umls-concept:C0001128,
umls-concept:C0205177,
umls-concept:C0205464,
umls-concept:C0205531,
umls-concept:C0226896,
umls-concept:C0231491,
umls-concept:C0442027,
umls-concept:C0597357,
umls-concept:C1424685,
umls-concept:C1522240,
umls-concept:C1527415,
umls-concept:C1880022,
umls-concept:C1880355,
umls-concept:C2607417
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pubmed:issue |
10
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pubmed:dateCreated |
2009-5-22
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pubmed:abstractText |
In an effort to discover novel druglike NK(1) receptor antagonists a new series of suitably substituted C-phenylpiperazine derivatives was identified by an appropriate chemical exploration of related N-phenylpiperazine analogues, with the specific aim to maximize their in vitro affinity and optimize in parallel their pharmacokinetic profile. Among the compounds synthesized, 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) was identified as one of the most in vitro potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. On the basis of its preclinical profile, this compound was selected as a drug candidate.
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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 |
1520-4804
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pubmed:author |
pubmed-author:AlvaroGiuseppeG,
pubmed-author:CimarostiZadeoZ,
pubmed-author:CorsiMauroM,
pubmed-author:Di FabioRomanoR,
pubmed-author:DonatiDanieleD,
pubmed-author:GerrardPhilip APA,
pubmed-author:GriffanteCristianaC,
pubmed-author:GuercioGiuseppeG,
pubmed-author:MarchioroCarlaC,
pubmed-author:MattioliMarioM,
pubmed-author:MelottoSergioS,
pubmed-author:MontanariDinoD,
pubmed-author:PentassugliaGiorgioG,
pubmed-author:PizziDomenica ADA,
pubmed-author:ProveraStefanoS,
pubmed-author:RattiEmiliangeloE,
pubmed-author:RossiTinoT,
pubmed-author:TristDavid GDG,
pubmed-author:ZonziniLauraL
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pubmed:issnType |
Electronic
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pubmed:day |
28
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3238-47
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pubmed:meshHeading |
pubmed-meshheading:19388677-Administration, Oral,
pubmed-meshheading:19388677-Animals,
pubmed-meshheading:19388677-CHO Cells,
pubmed-meshheading:19388677-Cricetinae,
pubmed-meshheading:19388677-Cricetulus,
pubmed-meshheading:19388677-Drug Discovery,
pubmed-meshheading:19388677-Drug Evaluation, Preclinical,
pubmed-meshheading:19388677-Gerbillinae,
pubmed-meshheading:19388677-Pharmacokinetics,
pubmed-meshheading:19388677-Piperazines,
pubmed-meshheading:19388677-Piperidines,
pubmed-meshheading:19388677-Receptors, Neurokinin-1,
pubmed-meshheading:19388677-Structure-Activity Relationship
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pubmed:year |
2009
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pubmed:articleTitle |
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
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pubmed:affiliation |
Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline Medicines Research Centre, Via A. Fleming 4, 37135 Verona, Italy. rdf26781@gsk.com
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pubmed:publicationType |
Journal Article
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