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An Overview on Benzylisoquinoline Derivatives with Dopaminergic and Serotonergic Activities

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Dopamine and serotonin are important neurotransmitters in the mammalian central nervous system (CNS) involved in numerous physiological and behavioural disorders such as schizophrenia, major depression, anxiety, Parkinson's and Huntington's diseases, and attention deficit hyperactivity disorder. Several natural and synthetic benzylisoquinoline derivatives have displayed affinity for dopamine and serotonin receptors in nanomolar or micromolar ranges. This review covers the last three decades of dopaminergic and serotonergic activities, and especially focuses on structureactivity relationships of natural and synthetic benzylisoquinoline derivatives. We have included aporphines, 1- benzyltetrahydroisoquinolines, bis-benzylisoquinolines, protoberberines, cularines and other structural analogues. Further molecular modelling calculations have been considered as important tools to not only obtain structural information of both neurotransmitter receptors, but to also identify their pharmacophore features. The development of selective potential ligands like benzylisoquinoline derivatives may help in the therapy of diseases related to CNS dysfunction.

Keywords: Benzylisoquinoline derivatives; Dopamine receptors; Molecular modelling; Serotonin receptors; Structure-activity relationships

Document Type: Research Article


Affiliations: Centro de Ecologia Quimica Agricola, Universidad Politecnica de Valencia (UPV), 46022 Valencia, Spain.

Publication date: 2009-07-01

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