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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
Indoloquinolizidine-peptide hybrids as multiple agonists for D1 and D2 dopamine receptors
ChemMedChem, Volume 4, No. 9, Year 2009
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Description
Multiple-specificity ligands are considered promising pharmacological tools that may show higher efficacy in the treatment of diseases for which the modulation of a single target is therapeutically inadequate. We prepared a set of novel ligands for D1 and D2 dopamine receptors by combining two indolo[2,3-α]quinolizidine scaffolds with various tripeptide moieties. The binding and functional properties of these molecules were determined by radioligand binding studies in brain striatuma membranes and by intracellular cAMP production assays in cells expressing different dopamine receptor subtypes. Some indoloquinolizidine - peptide hybrids, mainly with the trans configuration, showed dual agonist activity at both D1 and D2 dopamine receptors and may therefore be useful for testing the therapeutic potential of multivalent drugs on these targets. © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.
Authors & Co-Authors
Vendrell, Marc Martínez
Spain, Barcelona
Universitat de Barcelona
Singapore, Singapore City
A-star, Singapore Bioimaging Consortium
Lavilla, Rodolfo
Spain, Barcelona
Irb Barcelona - Institute for Research in Biomedicine
Alberício, Fernando
Spain, Barcelona
Irb Barcelona - Institute for Research in Biomedicine
Spain, Madrid
Centro de Investigación Biomédica en Red de Bioingeniería, Biomateriales y Nanomedicina
Spain, Barcelona
Universitat de Barcelona
Royo, Míriam
Spain, Barcelona
Universitat de Barcelona
Spain, Madrid
Centro de Investigación Biomédica en Red de Bioingeniería, Biomateriales y Nanomedicina
Statistics
Citations: 18
Authors: 4
Affiliations: 5
Identifiers
Doi:
10.1002/cmdc.200900149
ISSN:
18607187