TY  - JOUR
AU  - Vuckovic, S.
AU  - Prostran, M.
AU  - Ivanović, Milovan
AU  - Došen-Mićović, Ljiljana
AU  - Savic Vujovic, K.
AU  - Vucetic, C.
AU  - Kadija, M.
AU  - Mikovic, Z.
PY  - 2011
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/106
AB  - 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 dosedependent manner. The relative order of antinociceptive potency was similar to motor impairment potency, as well as lethality: F  gt  C  gt  T. Naloxone hydrochloride (1 mg/kg; sc) abolished all the effects observed, suggesting that they are mediated via opioid receptors, most probably of μ 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. © 2011 by the authors.
T2  - Pharmaceuticals
T1  - Pharmacological evaluation of 3-carbomethoxy fentanyl in mice
VL  - 4
IS  - 2
SP  - 233
EP  - 243
DO  - 10.3390/ph4020233
ER  - 

@article{
author = "Vuckovic, S. and Prostran, M. and Ivanović, Milovan and Došen-Mićović, Ljiljana and Savic Vujovic, K. and Vucetic, C. and Kadija, M. and Mikovic, Z.",
year = "2011",
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 dosedependent manner. The relative order of antinociceptive potency was similar to motor impairment potency, as well as lethality: F  gt  C  gt  T. Naloxone hydrochloride (1 mg/kg; sc) abolished all the effects observed, suggesting that they are mediated via opioid receptors, most probably of μ 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. © 2011 by the authors.",
journal = "Pharmaceuticals",
title = "Pharmacological evaluation of 3-carbomethoxy fentanyl in mice",
volume = "4",
number = "2",
pages = "233-243",
doi = "10.3390/ph4020233"
}

Vuckovic, S., Prostran, M., Ivanović, M., Došen-Mićović, L., Savic Vujovic, K., Vucetic, C., Kadija, M.,& Mikovic, Z.. (2011). Pharmacological evaluation of 3-carbomethoxy fentanyl in mice. in Pharmaceuticals, 4(2), 233-243.
https://doi.org/10.3390/ph4020233

Vuckovic S, Prostran M, Ivanović M, Došen-Mićović L, Savic Vujovic K, Vucetic C, Kadija M, Mikovic Z. Pharmacological evaluation of 3-carbomethoxy fentanyl in mice. in Pharmaceuticals. 2011;4(2):233-243.
doi:10.3390/ph4020233 .

Vuckovic, S., Prostran, M., Ivanović, Milovan, Došen-Mićović, Ljiljana, Savic Vujovic, K., Vucetic, C., Kadija, M., Mikovic, Z., "Pharmacological evaluation of 3-carbomethoxy fentanyl in mice" in Pharmaceuticals, 4, no. 2 (2011):233-243,
https://doi.org/10.3390/ph4020233 . .