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dc.creatorIvković, B.
dc.creatorVladimirov, Sote
dc.creatorNovaković, Radmila
dc.creatorĆupić, Vitomir
dc.creatorHeinle, H.
dc.creatorGojković-Bukarica, Ljiljana
dc.date.accessioned2020-06-03T13:32:04Z
dc.date.available2020-06-03T13:32:04Z
dc.date.issued2012
dc.identifier.issn0004-4172
dc.identifier.urihttp://vet-erinar.vet.bg.ac.rs/handle/123456789/861
dc.description.abstractOur aim was to define how different chemical properties of newly developed phenylpropiophenone derivates (PhPds) influenced their potency and efficacy to relax rat aorta. A contribution of ion channels in the PhPds and propafenone mechanism of vasodilatation was tested. PhPds were syntethysed by substitution in the benzyl moiety with -F, -CH3 or -CF3 groups on the ortho or para position. The vasodilatation by PhPds was examined on the rings of rat aorta precontracted with phenylephrine. In order to test involvement of voltage-gated Na+ and K+ channels and L-type Ca2+ channels in a mechanism of action of PhPds, we used their blockers: lidocaine, nifedipine and 4-aminopiridine, respectively. Aorta was more sensitive to 5-ortho-trifluoromethyl derivate than to propafenone and other PhPds. The 5-para-methyl derivate had lower potency and efficacy than propafenone and other PhPds. Lidocaine did not influenced relaxation induced by PhPds, but slightly inhibited the effect of propafenone. The 4-aminopiridine only inhibited relaxation induced by 5-para-methyl derivate. Nifedipine inhibited relaxation of the rat aorta induced by 5-ortho-trifluoromethyl derivate and by propafenone. Introduction of 5-ortho-trifluoromethyl and 5-para-methyl group in the benzyl moiety of propafenone molecule changed its potency, efficacy and mechanism of action in the rat aorta. The 4-aminopiridine- and nifedipine sensitive ion channels are involved in mechanism of action of 5-para-methyl and 5-ortho-trifluoromethyl derivate. The introduction of other tested groups in the benzyl moiety does not affect pharmacological properties of the PhPds in relation to propafenone.en
dc.publisherGeorg Thieme Verlag Kg, Stuttgart
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172041/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Technological Development (TD or TR)/31020/RS//
dc.rightsrestrictedAccess
dc.sourceArzneimittelforschung-Drug Research
dc.subjectvasodilatationen
dc.subjectstructure-properties relationship studyen
dc.subjection channelsen
dc.titleThe Novel Phenylpropiophenone Derivates Induced Relaxation of Isolated Rat Aortaen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractЋупић, Витомир; Хеинле, Х.; Владимиров, Соте; Ивковић, Б.; Новаковић, Радмила; Гојковић-Букарица, Љиљана;
dc.citation.volume62
dc.citation.issue7
dc.citation.spage345
dc.citation.epage350
dc.citation.other62(7): 345-350
dc.citation.rankM23
dc.identifier.wos000307038800008
dc.identifier.doi10.1055/s-0032-1312617
dc.identifier.pmid22628063
dc.identifier.scopus2-s2.0-84864121581
dc.identifier.rcubconv_1849
dc.type.versionpublishedVersion


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