Artículo
Structure–activity relationship of dopaminergic halogenated 1-benzyl-tetrahydroisoquinoline derivatives
El Aouad, Noureddine; Berenguer, Inmaculada; Romero, Vanessa; Marín, Paloma; Serrano, Ángel; Andujar, Sebastian Antonio
; Suvire, Fernando Daniel; Bermejo, Almudena; Ivorra, M. Dolores; Enriz, Ricardo Daniel
; Cabedo, Nuria; Cortes, Diego
Fecha de publicación:
11/2009
Editorial:
Elsevier France-editions Scientifiques Medicales Elsevier
Revista:
European Journal of Medical Chemistry
ISSN:
0223-5234
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
Two series of halogenated 1-benzyl-7-chloro-6-hydroxy-tetrahydroisoquinolines were prepared to explore the influence of each series on the affinity for dopamine receptors. All the compounds displayed a high affinity for D1-like and/or D2-like dopamine receptors in striatal membranes, although they were unable to inhibit [3H]-dopamine uptake in striatal synaptosomes. The halogen placed on the benzylic ring in 1-benzyl-THIQs, compounds of the series 1, 2′-bromobenzyl derivatives with Ki values into the nanomolar range, and the series 2, 2′,4′-dichlorobenzyl-THIQ homologues, proves to be an important factor to modulate affinity at dopamine receptor.
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Articulos(IMIBIO-SL)
Articulos de INST. MULTIDICIPLINARIO DE INV. BIO. DE SAN LUIS
Articulos de INST. MULTIDICIPLINARIO DE INV. BIO. DE SAN LUIS
Citación
El Aouad, Noureddine; Berenguer, Inmaculada; Romero, Vanessa; Marín, Paloma; Serrano, Ángel; et al.; Structure–activity relationship of dopaminergic halogenated 1-benzyl-tetrahydroisoquinoline derivatives; Elsevier France-editions Scientifiques Medicales Elsevier; European Journal of Medical Chemistry; 44; 11; 11-2009; 4616-4621
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