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Mixed dopaminergic/serotonergic properties of several 2-substituted 4-[2-(5-benzimidazole)ethyl]-1-arylpiperazines
dc.creator | Kostić Rajačić, Slađana | |
dc.creator | Šoškić, Vukić | |
dc.creator | Joksimovic, J | |
dc.date.accessioned | 2019-05-02T10:32:08Z | |
dc.date.available | 2019-05-02T10:32:08Z | |
dc.date.issued | 1998 | |
dc.identifier.issn | 0365-6233 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/2829 | |
dc.description.abstract | A series of substituted 4-[2-(5-benzimidazole)ethyl]-arylpiperazines was synthesized by introducing different substituents into position 2 of benzimidazole ring of 4-[2-(N,N-di-n-propylamino)ethyl]-1,2-diaminobenzenes. They were evaluated for in vitro binding affinity at the D 1 and D 2 dopamine and 5-HT(1A) serotonin receptors using synaptosomal membranes of the bovine caudate nuclei and hippocampi, respectively. Tritiated SCH 23390 (D 1 receptor-selective), spiperone (D 2 receptor selective),and 8-OH-DPAT (5-HT(1A) receptor selective) were employed as the radioligands. Only compound 6 expressed a moderate binding affinity at the dopamine D 1 receptor, while the remaining ligands were inefficient or weak competitors of [ 3 H]SCH 23390. Compound 12 was an absolutely inactive competitor of all three radioligands. Also, compound 7 was an inefficient displacer of [ 3 H]-8-OH-DPAT. Compound 19 with a K(i) value of 3.5 nM was the most potent competitor of [ 3 H]spiperone and compound 13 (K(i) = 3.3 nM) was the most efficient in displacing [ 3 H]-8-OH-DPAT from the 5-HT(1A) serotonin receptor. Ligands 5, 6, 8-11, and 13-20 expressed mixed dopaminergic/serotonergic activity in nanomolar range of concentrations with varying affinity ratios which strongly depended on the properties of the substituents introduced into position 2 of benzimidazole ring of the parent compounds. | en |
dc.publisher | Wiley-VCH Verlag | |
dc.relation | Ministry for Science and Technology of Serbia | |
dc.rights | restrictedAccess | |
dc.source | Archiv der Pharmazie | |
dc.title | Mixed dopaminergic/serotonergic properties of several 2-substituted 4-[2-(5-benzimidazole)ethyl]-1-arylpiperazines | en |
dc.type | article | en |
dc.rights.license | ARR | |
dcterms.abstract | Шошкиц, В; Костић-Рајачић, Слађана; Јоксимовиц, Ј; | |
dc.rights.holder | Wiley-VCH Verlag | |
dc.citation.volume | 331 | |
dc.citation.issue | 1 | |
dc.citation.spage | 22 | |
dc.citation.epage | 26 | |
dc.identifier.pmid | 9507698 | |
dc.identifier.doi | 10.1002/(SICI)1521-4184(199801)331:1<22::AID-ARDP22>3.0.CO;2-Q | |
dc.identifier.scopus | 2-s2.0-0345698656 | |
dc.type.version | publishedVersion |