跳到内容
Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.
关闭预览资料
正在查...

Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.

著者: M Froimowitz 附属: Massachusetts College of Pharmacy and Health Sciences, Boston, Massachusetts 02115, USA. mfroimowitz@mcphs.eduY GuLA DakinPM NagafujiCJ Kelley所有著者
版本/格式: 文章 文章 : 英语
刊登在:Journal of medicinal chemistry, 2007 Jan 25; 50(2): 219-32
数据库:取自MEDLINE®/PubMed®,这是美国医学图书馆的一个数据库。
其它数据库: British Library SerialsArticleFirst
提要:
Methylphenidate analogues, in which the carbomethoxy has been replaced by an alkyl group and with different phenyl substituents, have been synthesized and tested in monoamine transporter assays. As predicted from a pharmacophore model, most of the RR/SS diastereomers showed high potency as dopamine reuptake inhibitors. Analogues with a 4-chlorophenyl group and an unbranched initial alkyl atom had consistently  再读一些...
评估:

(尚未评估) 0 附有评论 - 争取成为第一个。

更多类似这样的

 

&AllPage.SpinnerRetrieving;

在图书馆查找

&AllPage.SpinnerRetrieving; 正在查找有这资料的图书馆...

详细书目

文件类型: 文章
所有的著者/提供者: M Froimowitz 附属: Massachusetts College of Pharmacy and Health Sciences, Boston, Massachusetts 02115, USA. mfroimowitz@mcphs.edu; Y Gu; LA Dakin; PM Nagafuji; CJ Kelley; D Parrish; JR Deschamps; A Janowsky
ISSN:0022-2623
语言注释: English
专有的标识符 110081487
奖励:

摘要:

Methylphenidate analogues, in which the carbomethoxy has been replaced by an alkyl group and with different phenyl substituents, have been synthesized and tested in monoamine transporter assays. As predicted from a pharmacophore model, most of the RR/SS diastereomers showed high potency as dopamine reuptake inhibitors. Analogues with a 4-chlorophenyl group and an unbranched initial alkyl atom had consistently enhanced selectivity for the dopamine transporter. The most potent compounds were those with a three- or four-carbon chain. The "inactive" RS/SR diastereomers showed substantial activity when the phenyl substituent was 3,4-dichloro. On a locomotor assay, one compound was found to have a slow onset and a long duration of action. The activity of these compounds provides additional evidence for a conformational/superposition model of methylphenidate with cocaine-like structures. A ketone analogue, obtained by hydrogenating a previously described vinylogous amide, had activity similar to that of methylphenidate.

评论

用户提供的评论
正在获取GoodReads评论...
正在检索DOGObooks的评论

标签

所有的用户标签 (1)

查看最热门的标签,展示的形式是: 标签列表 | 标签云(tag cloud)

  • good  (由 1 个人)

相似资料

这资料的用户列表 (1)

确认申请

你可能已经申请过这份资料。如果还是想申请,请选确认。

链接数据


Primary Entity

<http://www.worldcat.org/oclc/110081487> # Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.
    a schema:Article, schema:CreativeWork ;
    library:oclcnum "110081487" ;
    rdfs:comment "949 $l Research Support, Non-U.S. Gov't" ;
    rdfs:comment "949 $l Journal Article" ;
    rdfs:comment "949 $l Research Support, N.I.H., Extramural" ;
    schema:contributor <http://experiment.worldcat.org/entity/work/data/86047151#Person/parrish_d> ; # Parrish D
    schema:contributor <http://experiment.worldcat.org/entity/work/data/86047151#Person/deschamps_jr> ; # Deschamps JR
    schema:contributor <http://experiment.worldcat.org/entity/work/data/86047151#Person/nagafuji_pm> ; # Nagafuji PM
    schema:contributor <http://experiment.worldcat.org/entity/work/data/86047151#Person/gu_y> ; # Gu Y
    schema:contributor <http://experiment.worldcat.org/entity/work/data/86047151#Person/dakin_la> ; # Dakin LA
    schema:contributor <http://experiment.worldcat.org/entity/work/data/86047151#Person/kelley_cj> ; # Kelley CJ
    schema:contributor <http://experiment.worldcat.org/entity/work/data/86047151#Person/janowsky_a> ; # Janowsky A
    schema:creator <http://experiment.worldcat.org/entity/work/data/86047151#Person/froimowitz_m> ; # Froimowitz M
    schema:description "Methylphenidate analogues, in which the carbomethoxy has been replaced by an alkyl group and with different phenyl substituents, have been synthesized and tested in monoamine transporter assays. As predicted from a pharmacophore model, most of the RR/SS diastereomers showed high potency as dopamine reuptake inhibitors. Analogues with a 4-chlorophenyl group and an unbranched initial alkyl atom had consistently enhanced selectivity for the dopamine transporter. The most potent compounds were those with a three- or four-carbon chain. The "inactive" RS/SR diastereomers showed substantial activity when the phenyl substituent was 3,4-dichloro. On a locomotor assay, one compound was found to have a slow onset and a long duration of action. The activity of these compounds provides additional evidence for a conformational/superposition model of methylphenidate with cocaine-like structures. A ketone analogue, obtained by hydrogenating a previously described vinylogous amide, had activity similar to that of methylphenidate." ;
    schema:exampleOfWork <http://worldcat.org/entity/work/id/86047151> ;
    schema:isPartOf <http://worldcat.org/issn/0022-2623#50_2> ;
    schema:name "Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter." ;
    schema:pageStart "219" ;
    schema:productID "110081487" ;
    wdrs:describedby <http://www.worldcat.org/title/-/oclc/110081487> ;
    .


Related Entities

<http://worldcat.org/issn/0022-2623>
    a schema:Periodical ;
    rdfs:label "Journal of medicinal chemistry" ;
    schema:issn "0022-2623" ;
    .

<http://www.worldcat.org/title/-/oclc/110081487>
    a genont:InformationResource, genont:ContentTypeGenericResource ;
    schema:about <http://www.worldcat.org/oclc/110081487> ; # Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.
    schema:dateModified "2016-06-14" ;
    void:inDataset <http://purl.oclc.org/dataset/medline> ;
    .


Content-negotiable representations

关闭窗口

请登入WorldCat 

没有张号吗?很容易就可以 建立免费的账号.