TY  - 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 . .