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Open AccessArticle

Pharmacological Evaluation of 3-Carbomethoxy Fentanyl in Mice

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Department of Pharmacology, Clinical Pharmacology and Toxicology, School of Medicine, University of Belgrade, P.O. Box 38, 11129, Belgrade, Serbia
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Faculty of Chemistry, University of Belgrade, Belgrade, Serbia
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Institute for Orthopaedic Surgery and Traumatology, Clinical Center of Serbia, School of Medicine, University of Belgrade, Belgrade, Serbia
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Department of High-Risk Pregnancies, University Clinic of Gynaecology and Obstetrics “Narodni Front”, Belgrade, Serbia
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2011, 4(2), 233-243; https://doi.org/10.3390/ph4020233
Received: 15 December 2010 / Revised: 13 January 2011 / Accepted: 18 January 2011 / Published: 25 January 2011
(This article belongs to the Special Issue Opioids)
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. View Full-Text
Keywords: fentanyl; 3-carbomethoxy fentanyl; hot plate; rotarod; acute toxicity; mice fentanyl; 3-carbomethoxy fentanyl; hot plate; rotarod; acute toxicity; mice
MDPI and ACS Style

Vuckovic, S.; Prostran, M.; Ivanovic, M.; Dosen-Micovic, L.; Vujovic, K.S.; Vucetic, C.; Kadija, M.; Mikovic, Z. Pharmacological Evaluation of 3-Carbomethoxy Fentanyl in Mice. Pharmaceuticals 2011, 4, 233-243.

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