Pharmacological evaluation of 3-carbomethoxy fentanyl in mice
2011
Аутори
Vuckovic, S.Prostran, M.
Ivanović, Milovan
Došen-Mićović, Ljiljana
Savic Vujovic, K.
Vucetic, C.
Kadija, M.
Mikovic, Z.
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
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 fenta...nyl skeleton reduced the potency, but did not affect tolerability and safety of the compound. © 2011 by the authors.
Кључне речи:
3-carbomethoxy fentanyl / Acute toxicity / Fentanyl / Hot plate / Mice / RotarodИзвор:
Pharmaceuticals, 2011, 4, 2, 233-243Финансирање / пројекти:
- Базична и клиничко-фармаколошка истраживања механизама дејства и интеракција лекова у нервном и кардиоваскуларном систему (RS-MESTD-Basic Research (BR or ON)-175023)
Колекције
Институција/група
Hemijski fakultet / Faculty of ChemistryTY - 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 . .