Antiaritmički efekti novosintetisanih derivata propafenona

  • Branka Ivković Univerzitet u Beogradu – Farmaceutski fakultet, Katedra za farmaceutsku hemiju
  • Dragan Opačić Univerzitet u Beogradu – Medicinski fakultet, Katedra za farmakologiju, kliničku farmakologiju i toksikologiju
  • Boris Džudović Klinika za urgentnu internu medicinu, Vojnomedicinska akademija
  • Milkica Crevar Univerzitet u Beogradu – Farmaceutski fakultet, Katedra za farmaceutsku hemiju
  • Ljiljana Gojković-Bukarica Univerzitet u Beogradu – Medicinski fakultet, Katedra za farmakologiju, kliničku farmakologiju i toksikologiju
Ključne reči: derivati propafenona, eksperimentalna aritmija, akonitin, pacovi

Sažetak


Dobro je poznato da prisustvo različitih hemijskih grupa u molekulima leka utiče na njegova farmakološka svojstva. Cilj našeg istraživanja je ispitati da li novosintetisani derivati ​​propafenona, s promenama u benzilnoj grupi, imaju drugačiji efekat na aritmiju u odnosu na propafenon. 5OCl-PF i 5OF-PF su derivati ​​propafenona sa -Cl ili –F supstituentom na orto položaju benzilnog dela. Za proveru njihovog antiaritmičnog efekta koristili smo in vivo model na pacovima sa aritmijom izazvanom akonitinom. 5OCl-PF je ubrzao pojavu supraventrikularnih prevremenih otkucaja (SVPB) i smrt više nego akonitin. Sve životinje lečene sa 5OCl-PF razvile su ventrikularne prevremene otkucaje (VPBS i VPBB) i paroksizmalnu ventrikularnu tahikardiju (PVT). 5OF-PF je imao negativan hronotropni efekat i potencirao atrijalnu ekscitabilnost (više SVPB). Pozitivno je uticao na pojavu i vreme početka supraventrikularne tahikardije, VPBS i PVT. Na osnovu dobijenih rezultata se može zaključiti da novosintetisani derivati propafenona nemaju bolji antiaritmijski efekat od polaznog jedinjenja. U budućnosti, istraživanje će biti usmereno ka sintezi hemijski drugačijih derivata i ispitivanju njihovog antiaritmijskog efekta.

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2022/08/31
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