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Identification of a Tool Compound to Study the Mechanisms of Functional Selectivity between D2 and D3 Dopamine Receptors

AuthorsReyes-Resina, I.; Samadi, Abdelouahid ; Navarro, Gemma; Saadeh, H. A.; Khasawneh, M. A.; Mestres, J.; Marco-Contelles, José ; Franco, Rafael
Issue Date2018
PublisherAmerican Chemical Society
CitationACS Omega 3: 17368-17375 (2018)
AbstractThe search for synthetic selective compounds for G-protein-coupled receptors has provided a myriad of molecules with high selectivity and therapeutic potential. In some cases, however, selectivity is difficult to obtain. For instance, the selectivity ratio is relatively low for compounds acting on D and D dopamine receptors, which are targets of neurodegenerative diseases such as Parkinson's and Huntington's. From a therapeutic point of view, it is of interest the relative recent discovery of biased agonism, which is characterized by different signaling pathways engaged by different compounds acting on a given receptor. The aim of this paper was to investigate whether new piribedil-derived compounds could display higher selectivity for D or D receptor and/or provide biased signaling. The results show that selectivity was not different, but that one of the molecules described here, 5-((4-(pyrimidin-2-yl)piperazin-1-yl)methyl)quinolin-8-ol (10), does engage Gi-mediated signaling via D or D receptors, whereas it does not activate the mitogen-activated-protein kinase pathway, which is usually activated by dopamine receptor agonists.
Publisher version (URL)http://dx.doi.org/10.1021/acsomega.8b02509
Identifiersdoi: 10.1021/acsomega.8b02509
issn: 2470-1343
Appears in Collections:(IQOG) Artículos
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