Structure–activity relationship of dopaminergic halogenated 1-benzyl-tetrahydroisoquinoline derivatives
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 w...
| Autores: | , , , , , , , , , , , |
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| Tipo de recurso: | artículo |
| Estado: | Versión publicada |
| Fecha de publicación: | 2009 |
| País: | Argentina |
| Institución: | Consejo Nacional de Investigaciones Científicas y Técnicas |
| Repositorio: | CONICET Digital (CONICET) |
| Idioma: | inglés |
| OAI Identifier: | oai:ri.conicet.gov.ar:11336/113647 |
| Acceso en línea: | http://hdl.handle.net/11336/113647 |
| Access Level: | acceso abierto |
| Palabra clave: | 1-Halogenated benzyl-7-chloro-6-hydroxy-tetrahydroisoquinolines BINDING DOPAMINE RECEPTORS DOPAMINE UPTAKE STRUCTURE-ACTIVITY RELATIONSHIPS https://purl.org/becyt/ford/1.4 https://purl.org/becyt/ford/1 |
| Sumario: | 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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