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dc.creatorPenjišević, Jelena
dc.creatorŠukalović, Vladimir
dc.creatorAndrić, Deana
dc.creatorKostić Rajačić, Slađana
dc.creatorŠoškić, Vukić
dc.creatorRoglić, Goran
dc.date.accessioned2019-01-30T17:16:33Z
dc.date.available2019-01-30T17:16:33Z
dc.date.issued2007
dc.identifier.issn0365-6233
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/360
dc.description.abstractClinical properties of atypical antipsychotics are based on their interaction with D2 dopamine receptor and serotonin 5-HT1A and 5-HT2A receptors. As a part of our research program on new antipsychotics, we synthesized various derivatives of 1-cinnamyl-4-(2- methoxyphenyl)piperazines, and evaluated their affinities for D2, 5-HT1A, 5-HT2A, and adrenergic (α1) receptors using radioligand-binding assays. In addition, we performed docking analysis using models for the D2 and 5-HT1A receptors. All compounds exhibited low to moderate affinity to 5-HT1A and 5-HT 2A receptors, high affinity to the D2 receptor and large variability in affinities for the α1 receptor. Docking analysis indicated that the binding to D2 and 5-HT1A receptors is based on (i) interaction between protonated N1 of the piperazine ring and various aspartate residues, (ii) hydrogen bonds between various moieties of the ligand and the residues of threonine, serine, histidine or tryptophane, and (iii) edge-to-face interactions of the aromatic ring of the arylpiperazine moiety with phenylalanine or tyrosine residues. Docking data for the D 2 receptor can account for the binding properties obtained in binding assays, suggesting that the model is reliable and robust. However, docking data for the 5-HT1A receptor cannot account for actual binding properties, suggesting that further refinement of the model is required.en
dc.publisherWiley-V C H Verlag Gmbh, Weinheim
dc.relationinfo:eu-repo/grantAgreement/MESTD/MPN2006-2010/142009/RS//
dc.rightsrestrictedAccess
dc.sourceArchiv der Pharmazie
dc.subject5-HT2A receptoren
dc.subjectDopamine D2 receptoren
dc.subjectPiperazinesen
dc.subjectSerotonin 5-HT1Aen
dc.title1-Cinnamyl-4-(2-methoxyphenyl)piperazines: Synthesis, binding properties, and docking to dopamine (D2) and serotonin (5-HT1A) receptorsen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractAндрић, Д.; Роглић, Г.; Шукаловић, Владимир; Костић Рајачић, Слађана; Пењишевић, Јелена; Шошкић, В.;
dc.citation.volume340
dc.citation.issue9
dc.citation.spage456
dc.citation.epage465
dc.citation.other340(9): 456-465
dc.citation.rankM22
dc.identifier.pmid17763374
dc.identifier.doi10.1002/ardp.200700062
dc.identifier.rcubConv_4079
dc.identifier.scopus2-s2.0-34748901387
dc.identifier.wos000249747700002
dc.type.versionpublishedVersion


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