Abstract
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, Parkinsons and Huntingtons 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, Serotonin receptors, Structure-activity relationships, Molecular modelling
Current Medicinal Chemistry
Title: An Overview on Benzylisoquinoline Derivatives with Dopaminergic and Serotonergic Activities
Volume: 16 Issue: 19
Author(s): N. Cabedo, I. Berenguer, B. Figadere and D. Cortes
Affiliation:
- Centro de Ecologia Quimica Agricola, Universidad Politecnica de Valencia (UPV), 46022 Valencia, Spain.,Spain
Keywords: Benzylisoquinoline derivatives, Dopamine receptors, Serotonin receptors, Structure-activity relationships, Molecular modelling
Abstract: 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, Parkinsons and Huntingtons 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.
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Cite this article as:
Cabedo N., Berenguer I., Figadere B. and Cortes D., An Overview on Benzylisoquinoline Derivatives with Dopaminergic and Serotonergic Activities, Current Medicinal Chemistry 2009; 16(19) . https://dx.doi.org/10.2174/092986709788682100
DOI https://dx.doi.org/10.2174/092986709788682100 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |

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