omitir hasta el contenido
Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.
CerrarVer este material de antemano
Chequeando…

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

Autor: M Froimowitz Afiliación: Massachusetts College of Pharmacy and Health Sciences, Boston, Massachusetts 02115, USA. mfroimowitz@mcphs.eduY GuLA DakinPM NagafujiCJ KelleyTodos autores
Edición/Formato: Artículo Artículo : Inglés (eng)
Publicación:Journal of medicinal chemistry, 2007 Jan 25; 50(2): 219-32
Base de datos:De MEDLINE®/PubMed®, una base de datos de la Biblioteca Nacional de Medicina de los Estados Unidos.
Otras bases de datos: British Library SerialsArticleFirst
Resumen:
Methylphenidate analogues, in which the carbomethoxy has been replaced by an alkyl group and with different phenyl substituents, have been synthesized and tested in monoamine transporter assays.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  Leer más
Calificación:

(todavía no calificado) 0 con reseñas - Ser el primero.

Más materiales como éste

 

&AllPage.SpinnerRetrieving;

Encontrar un ejemplar en la biblioteca

&AllPage.SpinnerRetrieving; Encontrando bibliotecas que tienen este material…

Detalles

Tipo de documento: Artículo
Todos autores / colaboradores: M Froimowitz Afiliación: 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
Nota del idioma: English
Identificador único: 110081487
Premios:

Resumen:

Methylphenidate analogues, in which the carbomethoxy has been replaced by an alkyl group and with different phenyl substituents, have been synthesized and tested in monoamine transporter assays.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.

Reseñas

Reseñas contribuidas por usuarios
Recuperando reseñas de GoodReads…
Recuperando reseñas de DOGObooks…

Etiquetas

Todas las etiquetas de usuarios (1)

Ver etiquetas más populares como: lista de etiquetas | nube de etiquetas

  • good  (por 1 persona)

Materiales similares

Listas de usuarios con este material (1)

Confirmar este pedido

Ya ha pedido este material. Escoja OK si desea procesar el pedido de todos modos.

Datos enlazados


<http://www.worldcat.org/oclc/110081487>
library:oclcnum"110081487"
owl:sameAs<info:oclcnum/110081487>
rdf:typeschema:Article
schema:contributor
schema:contributor
schema:contributor
schema:contributor
schema:contributor
schema:contributor
schema:contributor
schema:creator
schema:datePublished"2007-01-25"
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
schema:isPartOf
schema:name"Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter."
schema:pageStart"219"
schema:url

Content-negotiable representations

Cerrar ventana

Inicie una sesión con WorldCat 

¿No tienes una cuenta? Puede fácilmente crear una cuenta gratuita.