Приказ основних података о документу
The Novel Phenylpropiophenone Derivates Induced Relaxation of Isolated Rat Aorta
dc.creator | Ivković, B. | |
dc.creator | Vladimirov, Sote | |
dc.creator | Novaković, Radmila | |
dc.creator | Ćupić, Vitomir | |
dc.creator | Heinle, H. | |
dc.creator | Gojković-Bukarica, Ljiljana | |
dc.date.accessioned | 2020-06-03T13:32:04Z | |
dc.date.available | 2020-06-03T13:32:04Z | |
dc.date.issued | 2012 | |
dc.identifier.issn | 0004-4172 | |
dc.identifier.uri | https://vet-erinar.vet.bg.ac.rs/handle/123456789/861 | |
dc.description.abstract | Our 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.publisher | Georg Thieme Verlag Kg, Stuttgart | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172041/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Technological Development (TD or TR)/31020/RS// | |
dc.rights | restrictedAccess | |
dc.source | Arzneimittelforschung-Drug Research | |
dc.subject | vasodilatation | en |
dc.subject | structure-properties relationship study | en |
dc.subject | ion channels | en |
dc.title | The Novel Phenylpropiophenone Derivates Induced Relaxation of Isolated Rat Aorta | en |
dc.type | article | |
dc.rights.license | ARR | |
dcterms.abstract | Ћупић, Витомир; Хеинле, Х.; Владимиров, Соте; Ивковић, Б.; Новаковић, Радмила; Гојковић-Букарица, Љиљана; | |
dc.citation.volume | 62 | |
dc.citation.issue | 7 | |
dc.citation.spage | 345 | |
dc.citation.epage | 350 | |
dc.citation.other | 62(7): 345-350 | |
dc.citation.rank | M23 | |
dc.identifier.wos | 000307038800008 | |
dc.identifier.doi | 10.1055/s-0032-1312617 | |
dc.identifier.pmid | 22628063 | |
dc.identifier.scopus | 2-s2.0-84864121581 | |
dc.type.version | publishedVersion |