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dc.creatorDukic, S
dc.creatorKostić Rajačić, Slađana
dc.creatorŠoškic, V
dc.creatorJoksimovic, J
dc.date.accessioned2019-05-02T10:37:48Z
dc.date.available2019-05-02T10:37:48Z
dc.date.issued1997
dc.identifier.issn0365-6233
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/2830
dc.description.abstractWith 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.
dc.publisherWiley
dc.relationMinistry for Science and Technology of Serbi
dc.rightsrestrictedAccess
dc.sourceArchiv der Pharmazie
dc.subjectDopamine D2
dc.subjectpiperidine derivative
dc.titleSynthesis and dopaminergic properteis of 3- and 4-substituted 1-{-[5-(1H-benzimidazole-2-thione)]ethyl}piperidines and related compounds
dc.typearticleen
dc.rights.licenseARR
dcterms.abstractЈоксимовиц, Ј; Шошкиц, В; Костић-Рајачић, Слађана; Дукиц, С;
dc.rights.holderWiley
dc.citation.volume330
dc.citation.issue1-2
dc.citation.spage25
dc.citation.epage28
dc.identifier.doi10.1002/ardp.19973300107
dc.identifier.scopus2-s2.0-0030610512
dc.type.versionpublishedVersion


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