INVESTIGADORES
ENRIZENRIZ] ricardoricardo] danieldaniel]
artículos
Título:
Structure-Activity Relationship of dopaminergic halogenated 1-benzyl tetrahydroisoquinoline derivatives
Autor/es:
NOUREDDINE EL AOUAD ; INMACULADA BERENGUER ; VANESA , ROMERO ; PALOMA MARÍN ; ÁNGEL SERRANO ; SEBASTIÁN ANDUJAR ; FERNANDO SUVIRE ; ALMUDENA BERMEJO ; M. DOLORES IVORRA ; RICARDORICARDO] D. ENRIZENRIZ] ; NURIA CABEDO ; DIEGO CORTES.
Revista:
EUROPEAN JOURNAL OF MEDICAL CHEMISTRY
Editorial:
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Referencias:
Año: 2009 vol. 40 p. 4616 - 4616
ISSN:
0223-5234
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 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.1-like and/or D2-like dopamine receptors in striatal membranes, although 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 opamine receptor.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 opamine receptor.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 dpamine receptor.2, 2´,4´- dichlorobenzyl-THIQ homologues, proves to be an important factor to modulate affinity at dopamine receptor.1-like and/or D2-like dopamine receptors in striatal membranes, although 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 opamine receptor.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 opamine receptor.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 dpamine receptor.2, 2´,4´- dichlorobenzyl-THIQ homologues, proves to be an important factor to modulate affinity at dopamine receptor.
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