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Pharmacological Evaluation of 3-Carbomethoxy Fentanyl in Mice
Department of Pharmacology, Clinical Pharmacology and Toxicology, School of Medicine, University of Belgrade, P.O. Box 38, 11129, Belgrade, Serbia
Faculty of Chemistry, University of Belgrade, Belgrade, Serbia
Institute for Orthopaedic Surgery and Traumatology, Clinical Center of Serbia, School of Medicine, University of Belgrade, Belgrade, Serbia
Department of High-Risk Pregnancies, University Clinic of Gynaecology and Obstetrics “Narodni Front”, Belgrade, Serbia
* Author to whom correspondence should be addressed.
Received: 15 December 2010; in revised form: 13 January 2011 / Accepted: 18 January 2011 / Published: 25 January 2011
(This article belongs to the Special Issue Opioids
Abstract: 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.
Keywords: fentanyl; 3-carbomethoxy fentanyl; hot plate; rotarod; acute toxicity; mice
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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.
Vuckovic S, Prostran M, Ivanovic M, Dosen-Micovic L, Vujovic KS, Vucetic C, Kadija M, Mikovic Z. Pharmacological Evaluation of 3-Carbomethoxy Fentanyl in Mice. Pharmaceuticals. 2011; 4(2):233-243.
Vuckovic, Sonja; Prostran, Milica; Ivanovic, Milovan; Dosen-Micovic, Ljiljana; Vujovic, Katarina Savic; Vucetic, Cedomir; Kadija, Marko; Mikovic, Zeljko. 2011. "Pharmacological Evaluation of 3-Carbomethoxy Fentanyl in Mice." Pharmaceuticals 4, no. 2: 233-243.