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Novel 5-[2-(N,N-di-n-propylamino)-ethyl]benzimidazole-derived high affinity dopaminergic ligands
dc.creator | Dragović, D | |
dc.creator | Kostić Rajačić, Slađana | |
dc.creator | Šoškić, Vukić | |
dc.creator | Joksimović, J | |
dc.date.accessioned | 2019-05-02T10:46:35Z | |
dc.date.available | 2019-05-02T10:46:35Z | |
dc.date.issued | 1996 | |
dc.identifier.issn | 0031-7144 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/2832 | |
dc.description.abstract | Derivatives of a noncatechol dopamine (DA) bioisostere 5-[2-(N,N-di-n-propylamino)ethyl]-benzimidazole (15) were synthesized and checked for affinity towards D-1 and D-2 DA receptors (DAR). Ten compounds were obtained by introducing groups of different inductive effects into position 2 of the parent compound 15, while two other compounds were synthesized by introducing a 1-naphthyl group into the side chain of dichloromethyl (9) and dibromomethyl (10) derivatives of 15. The affinity and selectivity of these novel compounds for the D-1 and D-2 class of the DAR were estimated by in vitro competition binding assays using synaptosomal membranes of the bovine caudate nuclei and [ 3 H]SCH 23390 (D-1 selective) and [ 3 H]spiperone (D-2 selective) as radioligands. None of the synthesized compounds expressed the affinity for the binding to D-1 receptors, while compounds 13, 14, 10, 9, 7 and 8, in this rank order of potencies competed with [ 3 H]spiperone binding to D-2 receptors under conditions of prevented radioligand binding to serotonin 5HT 2 receptors. Their affinities for this class of the DAR were about 2- to 555-fold higher in comparison to the parent compound 15, thus suggesting that some of them could be successfully used as dopaminergic ligands. | en |
dc.publisher | Govi-Verlag Pharmazeutischer Verlag GmbH | |
dc.rights | restrictedAccess | |
dc.source | Pharmazie | |
dc.title | Novel 5-[2-(N,N-di-n-propylamino)-ethyl]benzimidazole-derived high affinity dopaminergic ligands | en |
dc.type | article | en |
dc.rights.license | ARR | |
dcterms.abstract | Шошкић, В; Јоксимовић, Ј; Драговић, Д; Костић-Рајачић, Слађана; | |
dc.citation.volume | 51 | |
dc.citation.issue | 10 | |
dc.citation.spage | 694 | |
dc.citation.epage | 697 | |
dc.identifier.rcub | https://hdl.handle.net/21.15107/rcub_cer_2832 | |
dc.identifier.scopus | 2-s2.0-0029856314 | |
dc.type.version | publishedVersion |
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