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Synthesis and dopaminergic features of six novel 3-arylpiperidines
dc.creator | Kostić Rajačić, Slađana | |
dc.creator | Šoškić, Vukić | |
dc.creator | Joksimovic, J | |
dc.date.accessioned | 2019-05-02T10:14:56Z | |
dc.date.available | 2019-05-02T10:14:56Z | |
dc.date.issued | 1998 | |
dc.identifier.issn | 0006-6648 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/2826 | |
dc.description.abstract | Four substituted 3-aryl-1-{2-[5-(1H-benzimidazole)]ethyl}piperidines and two 3-aryl-1-{2-[6-(1,4-dihydroxyquinoxaline-2,3-dione)]ethyl} piperidines were synthesized, characterized and evaluated for in vitro binding affinity at the D1 and D2 dopamine and 5-HT1A serotonin receptors using synaptosomal membranes of fresh bovine caudate nuclei and hippocampi as a source of the dopamine and serotonin receptors, respectively, and the corresponding specific radioligands. All six novel compounds expressed no binding affinity at the D1 and 5-HT1A receptors. Derivatives of 1,4- dihydroxyquinoxaline-2,3-dione (compounds 8a and 8b) and of 2- dihalomethylbenzimidazole (ligands 9 and 10) were moderate competitors of [ 3 H]spiperone binding at the D2 dopamine receptors. However, benzimidazole- 2-thiones (compounds 7a and 7b) behaved as selective D2 receptor ligands with the binding affinity in the nanomolar range of concentrations. | en |
dc.rights | restrictedAccess | |
dc.source | Bollettino Chimico Farmaceutico | |
dc.subject | binding affinity | |
dc.subject | Dopamine Agents | |
dc.subject | Dopamine Receptors | |
dc.subject | Piperidines | |
dc.subject | serotoninergic system | |
dc.title | Synthesis and dopaminergic features of six novel 3-arylpiperidines | en |
dc.type | article | en |
dc.rights.license | ARR | |
dcterms.abstract | Јоксимовиц, Ј; Костић-Рајачић, Слађана; Соскиц, В; | |
dc.citation.volume | 137 | |
dc.citation.issue | 10 | |
dc.citation.spage | 417 | |
dc.citation.epage | 421 | |
dc.identifier.pmid | 10025971 | |
dc.identifier.rcub | https://hdl.handle.net/21.15107/rcub_cer_2826 | |
dc.identifier.scopus | 2-s2.0-0032406630 | |
dc.type.version | publishedVersion |
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