Source:http://linkedlifedata.com/resource/pubmed/id/20061148
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
2010-2-3
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pubmed:abstractText |
A series of novel dopamine D(1) antagonists derived from functionalization of the D-ring of SCH 39166 were prepared. A number of these compounds displayed subnanomolar D(1) activity and more than 1000-fold selectivity over D(2). We found C-3 derivatization afforded compounds with superior overall profile in comparison to the C-2 and C-4 derivatization. A number of highly potent D(1) antagonists were discovered which have excellent selectivity over other dopamine receptors and improved PK profile compared to SCH 39166.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BurgosRR,
pubmed-author:BurnettDuane ADA,
pubmed-author:FawziAhmadA,
pubmed-author:GreenleeWilliam JWJ,
pubmed-author:LachowiczJean EJE,
pubmed-author:LiQiangQ,
pubmed-author:McKittrickBrian ABA,
pubmed-author:SasikumarT KTK,
pubmed-author:SmithMichelleM,
pubmed-author:SuJingJ,
pubmed-author:TangHaiqunH,
pubmed-author:YeYuanzanY,
pubmed-author:ZhangHongtaoH,
pubmed-author:ZhuZhaoningZ
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pubmed:copyrightInfo |
Copyright (c) 2009 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
836-40
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pubmed:meshHeading | |
pubmed:year |
2010
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pubmed:articleTitle |
Discovery of new SCH 39166 analogs as potent and selective dopamine D1 receptor antagonists.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
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pubmed:publicationType |
Journal Article,
Comparative Study
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