Pharmaceuticals 2011, 4(2), 233-243; doi:10.3390/ph4020233
Article

Pharmacological Evaluation of 3-Carbomethoxy Fentanyl in Mice

1,* email, 1, 2, 2, 1, 3, 3 and 4
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)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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.

AMA Style

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.

Chicago/Turabian Style

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.


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