Приказ основних података о документу
Synthesis and dopaminergic properteis of 3- and 4-substituted 1-{-[5-(1H-benzimidazole-2-thione)]ethyl}piperidines and related compounds
dc.creator | Dukić, Slađana | |
dc.creator | Kostić Rajačić, Slađana | |
dc.creator | Šoškić, Vukić | |
dc.creator | Joksimovic, J | |
dc.date.accessioned | 2019-05-02T10:37:48Z | |
dc.date.available | 2019-05-02T10:37:48Z | |
dc.date.issued | 1997 | |
dc.identifier.issn | 0365-6233 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/2830 | |
dc.description.abstract | With an aim of creating new, high affinity dopaminergic ligands, six different 3- and 4-substituted 1-{2-[5-(1H-benzimidazole-2-thione)]ethyl}piperidines and nine related heterocyclic congeners were synthesized and evaluated for in vitro binding affinity at D 1 and D 2 dopamine receptors. Synaptosomal membranes prepared from fresh bovine caudate nuclei were used as a source of the dopamine receptors. Only 4-[bis-(4-fluorophenyl)methylene]-piperidines, compounds 9e, 10d, and 11d, expressed moderate affinity for the D 1 receptors, while all other compounds were inactive competitors of [ 3H]SCH 23390. Compounds 9c, 9d, 10c, 11a, and 11c were inactive in the D 2 receptor binding assay, as well. Derivatives of 4-phenylpiperidine (9-11b) and 3-phenyl-piperidine (10a) expressed a moderate to low affinity for the D 2 receptors. However, racemic (±)-1-{2-[5-(1H-benzimidazole-2-thione)]ethyl}-3-phenylpiperidine 9a and its enantiomer (+)-9a behaved as selective, high affinity D 2 receptor ligands, the latter being some four times more active than the racemate. | en |
dc.publisher | Wiley | |
dc.relation | Ministry for Science and Technology of Serbi | |
dc.rights | restrictedAccess | |
dc.source | Archiv der Pharmazie | |
dc.subject | Dopamine D2 | |
dc.subject | piperidine derivative | |
dc.title | Synthesis and dopaminergic properteis of 3- and 4-substituted 1-{-[5-(1H-benzimidazole-2-thione)]ethyl}piperidines and related compounds | en |
dc.type | article | en |
dc.rights.license | ARR | |
dcterms.abstract | Јоксимовиц, Ј; Шошкиц, В; Костић-Рајачић, Слађана; Дукиц, С; | |
dc.rights.holder | Wiley | |
dc.citation.volume | 330 | |
dc.citation.issue | 1-2 | |
dc.citation.spage | 25 | |
dc.citation.epage | 28 | |
dc.identifier.doi | 10.1002/ardp.19973300107 | |
dc.identifier.scopus | 2-s2.0-0030610512 | |
dc.identifier.wos | A1997WR36900006 | |
dc.type.version | publishedVersion |