info:eu-repo/semantics/article
Structure–activity relationship of dopaminergic halogenated 1-benzyl-tetrahydroisoquinoline derivatives
Fecha
2009-11Registro en:
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
0223-5234
CONICET Digital
CONICET
Autor
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
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.