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Pharmacological Evaluation of 3-Carbomethoxy Fentanyl in Mice

Author(s): Sonja Vuckovic | Milica Prostran | Milovan Ivanovic | Ljiljana Dosen-Micovic | Katarina Savic Vujovic | Cedomir Vucetic | Marko Kadija | Zeljko Mikovic

Journal: Pharmaceuticals
ISSN 1424-8247

Volume: 4;
Issue: 2;
Start page: 233;
Date: 2011;
Original page

Keywords: fentanyl | 3-carbomethoxy fentanyl | hot plate | rotarod | acute toxicity | mice

In many animal species, as well as in humans, high doses of fentanyl (F) produce marked neurotoxic effects, such as muscular rigidity and respiratory depression. The antinociception (hot-plate test), impairment of motor coordination (rotarod test) and acute toxicity of intraperitoneal newly synthesized analogs, (±)cis-3-carbomethoxy- fentanyl (C) and (±)trans-3-carbomethoxyfentanyl (T) were evaluated in mice. The compounds tested induced antinociception, impairment of performance on the rotarod, and lethality in a dose-dependent manner. The relative order of antinociceptive potency was similar to motor impairment potency, as well as lethality: F > C > T. Naloxone hydrochloride (1 mg/kg; sc) abolished all the effects observed, suggesting that they are mediated via opioid receptors, most probably of m type. There were no significant differences between the therapeutic indices of F, C and T. It is concluded, the introduction of 3-carbomethoxy group in the piperidine ring of the fentanyl skeleton reduced the potency, but did not affect tolerability and safety of the compound.
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