The Novel Phenylpropiophenone Derivates Induced Relaxation of Isolated Rat Aorta
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2012
Authors
Ivković, B.Vladimirov, Sote
Novaković, Radmila
Ćupić, Vitomir
Heinle, H.
Gojković-Bukarica, Ljiljana
Article (Published version)
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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.
Keywords:
vasodilatation / structure-properties relationship study / ion channelsSource:
Arzneimittelforschung-Drug Research, 2012, 62, 7, 345-350Publisher:
- Georg Thieme Verlag Kg, Stuttgart
Funding / projects:
- Development of molecules with antiinflammatory and cardioprotective activity: structural modifications, modelling, physicochemical characterization and formulation investigations (RS-172041)
- Development of new technology for production of red wine and diatery supplements reach with polyphenols with cardioprotective effects (RS-31020)
DOI: 10.1055/s-0032-1312617
ISSN: 0004-4172
PubMed: 22628063
WoS: 000307038800008
Scopus: 2-s2.0-84864121581
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Fakultet veterinarske medicineTY - JOUR AU - Ivković, B. AU - Vladimirov, Sote AU - Novaković, Radmila AU - Ćupić, Vitomir AU - Heinle, H. AU - Gojković-Bukarica, Ljiljana PY - 2012 UR - https://vet-erinar.vet.bg.ac.rs/handle/123456789/861 AB - 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. PB - Georg Thieme Verlag Kg, Stuttgart T2 - Arzneimittelforschung-Drug Research T1 - The Novel Phenylpropiophenone Derivates Induced Relaxation of Isolated Rat Aorta VL - 62 IS - 7 SP - 345 EP - 350 DO - 10.1055/s-0032-1312617 ER -
@article{ author = "Ivković, B. and Vladimirov, Sote and Novaković, Radmila and Ćupić, Vitomir and Heinle, H. and Gojković-Bukarica, Ljiljana", year = "2012", 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.", publisher = "Georg Thieme Verlag Kg, Stuttgart", journal = "Arzneimittelforschung-Drug Research", title = "The Novel Phenylpropiophenone Derivates Induced Relaxation of Isolated Rat Aorta", volume = "62", number = "7", pages = "345-350", doi = "10.1055/s-0032-1312617" }
Ivković, B., Vladimirov, S., Novaković, R., Ćupić, V., Heinle, H.,& Gojković-Bukarica, L.. (2012). The Novel Phenylpropiophenone Derivates Induced Relaxation of Isolated Rat Aorta. in Arzneimittelforschung-Drug Research Georg Thieme Verlag Kg, Stuttgart., 62(7), 345-350. https://doi.org/10.1055/s-0032-1312617
Ivković B, Vladimirov S, Novaković R, Ćupić V, Heinle H, Gojković-Bukarica L. The Novel Phenylpropiophenone Derivates Induced Relaxation of Isolated Rat Aorta. in Arzneimittelforschung-Drug Research. 2012;62(7):345-350. doi:10.1055/s-0032-1312617 .
Ivković, B., Vladimirov, Sote, Novaković, Radmila, Ćupić, Vitomir, Heinle, H., Gojković-Bukarica, Ljiljana, "The Novel Phenylpropiophenone Derivates Induced Relaxation of Isolated Rat Aorta" in Arzneimittelforschung-Drug Research, 62, no. 7 (2012):345-350, https://doi.org/10.1055/s-0032-1312617 . .