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dc.creatorRoglić, Goran
dc.creatorDukić-Stefanovic, S
dc.creatorAndrić, Deana
dc.creatorKostić Rajačić, Slađana
dc.creatorŠoškić, Vukić
dc.date.accessioned2019-05-02T10:09:30Z
dc.date.available2019-05-02T10:09:30Z
dc.date.issued2001
dc.identifier.issn0031-7144
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/2825
dc.description.abstractEight novel N-heteroarylalkyl-N-phenylpiperazines have been synthesized, chemically characterized and evaluated for in vitro binding affinity at the dopamine and serotonin receptors. Synaptosomal membranes of fresh bovine caudate nuclei (D(1) and D(2)), the membranes of COS-7 cells (D(4.4)) and those prepared from fresh bovine hippocampi (5-HT(1A)) were used as a source of the corresponding receptor subtypes. [(3)H]SCH 23390 (D(1)-selective), [(3)H]spiperone (D(2)- and D(4.4)- selective) and [(3)H]-8-OH-DPAT (5-HT(1A)-selective) served as radioligands. None of the compounds expressed the affinity for the binding at the D(1) subtype receptor. Compounds 7-9 containing a single methylene group serving as a bridge between heteroaryl and N-phenylpiperazine part of the molecule were inactive [(3)H]spiperone and [(3)H]-8-OH-DPAT competitors. Ligands 15-19 (three methylene groups connecting heteroaryl- and N-phenylpiperazine part of the molecule) acted as moderate competitors of [(3)H]spiperone binding at the D(2) receptor subtype, with the exception of 15 (a thione) which expressed a high binding affinity at the D(2) receptor subtype. Compounds 15-19 behaved as moderate displacers of 8-OH-[(3)H]DPAT. Among all eight novel ligands only compound 15 expressed a moderate binding affinity at the D(4.4) receptor subtype.en
dc.publisherGovi-Verlag Pharmazeutischer Verlag Gmbh, Eschborn
dc.rightsrestrictedAccess
dc.sourcePharmazie
dc.titleInvestigation of mixed D(2)/5-HT(1A) activity of N-heteroarylmethyl-N-phenylpiperazines, N-heteroarylethyl-N-phenylpiperazines and N-heteroarylpropyl-N-phenylpiperazinesen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractДукиц-Стефановиц, С; Соскиц, В; Роглић, Горан; Костић-Рајачић, Слађана; Aндрић, Деана;
dc.citation.volume56
dc.citation.issue10
dc.citation.spage803
dc.citation.epage807
dc.citation.other56(10): 803-807
dc.citation.rankM23
dc.identifier.pmid11683128
dc.identifier.rcubKon_1449
dc.identifier.scopus2-s2.0-0034740857
dc.identifier.wos000172074800012


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