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Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor.
Austin, N E; Avenell, K Y; Boyfield, I; Branch, C L; Hadley, M S; Jeffrey, P; Johnson, C N; Macdonald, G J; Nash, D J; Riley, G J; Smith, A B; Stemp, G; Thewlis, K M; Vong, A K; Wood, M D.
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  • Austin NE; SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK.
Bioorg Med Chem Lett ; 11(5): 685-8, 2001 Mar 12.
Article en En | MEDLINE | ID: mdl-11266169
Starting from the tetrahydroisoquinoline SB-277011 1, a novel series of 5-substituted-2,3-dihydro-1H-isoindoles has been designed. Subsequent optimisation resulted in identification of 19, which has high affinity for the dopamine D3 receptor (pKi 8.3) and > or = 100-fold selectivity over other aminergic receptors. In rat studies 19 was brain penetrant with an excellent pharmacokinetic profile (oral bioavailability 77%, t1/2 5.2h).
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores de Dopamina D2 / Antagonistas de Dopamina / Indoles Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2001 Tipo del documento: Article Pais de publicación: Reino Unido
Buscar en Google
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores de Dopamina D2 / Antagonistas de Dopamina / Indoles Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2001 Tipo del documento: Article Pais de publicación: Reino Unido