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dc.creatorTomic, Mirko
dc.creatorVaskovic, Djurdjica
dc.creatorTovilović, Gordana
dc.creatorAndrić, Deana
dc.creatorPenjišević, Jelena
dc.creatorKostić-Rajačić, Slađana
dc.date.accessioned2018-11-22T00:19:32Z
dc.date.available2018-11-22T00:19:32Z
dc.date.issued2011
dc.identifier.issn0365-6233
dc.identifier.urihttp://cherry.chem.bg.ac.rs/handle/123456789/1337
dc.description.abstractFive groups of previously synthesized and initially screened non-substituted and 4-halogenated arylpiperazin-1-yl-ethyl-benzimidazoles were estimated for their in-vitro binding affinities at the rat D-2, 5-HT2A, and alpha(1)-adrenergic receptors. Among all these compounds, 2-methoxyphenyl and 2-chlorophenyl piperazines demonstrate the highest affinities for the tested receptors. The effects of 4-halogenation of benzimidazoles reveal that substitution with brominemay greatly increase the affinity of the compounds for the studied receptors, while the effect of substitution with chlorine is less remarkable. Most of the tested components show 5-HT2A/D-2 pK(i) binding ratios slightly above or less than 1, while only 4-chloro-6-(2-{4-[3-(trifluoromethyl) phenyl]piperazin-1-yl}ethyl)-1H-benzimidazole expresses an appropriate higher binding ratio (1.14), which was indicated for atypical neuroleptics. This compound exhibits a non-cataleptic action in rats and prevents d-amphetamine-induced hyperlocomotion in mice, which suggest its atypical antipsychotic potency.en
dc.publisherWiley-Blackwell, Malden
dc.relationinfo:eu-repo/grantAgreement/MESTD/MPN2006-2010/143032/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/MPN2006-2010/142009/RS//
dc.rightsrestrictedAccess
dc.sourceArchiv der Pharmazie
dc.subjectArylpiperazinesen
dc.subjectAtypical antipsychoticsen
dc.subjectD-2 receptorsen
dc.subject5-HT2A receptorsen
dc.subjectPharmacological screeningen
dc.titlePharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D-2 and 5-HT2A Receptor Ligandsen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractТовиловиц, Гордана; Костиц-Рајациц, Сладјана; Пењисевиц, Јелена; Aндрић, Деана; Томиц, Мирко; Васковиц, Дјурдјица;
dc.citation.volume344
dc.citation.issue5
dc.citation.spage287
dc.citation.epage291
dc.identifier.wos000290441500002
dc.identifier.doi10.1002/ardp.200900168
dc.citation.other344(5): 287-291
dc.citation.rankM22
dc.identifier.pmid21509803
dc.type.versionpublishedVersionen
dc.identifier.scopus2-s2.0-79955416905
dc.identifier.rcubKon_2175


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