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Pharmacological evaluation of 3-carbomethoxy fentanyl in mice
dc.creator | Vuckovic, S. | |
dc.creator | Prostran, M. | |
dc.creator | Ivanović, Milovan | |
dc.creator | Došen-Mićović, Ljiljana | |
dc.creator | Savic Vujovic, K. | |
dc.creator | Vucetic, C. | |
dc.creator | Kadija, M. | |
dc.creator | Mikovic, Z. | |
dc.date.accessioned | 2018-11-22T00:17:39Z | |
dc.date.available | 2018-11-22T00:17:39Z | |
dc.date.issued | 2011 | |
dc.identifier.issn | 1424-8247 | |
dc.identifier.uri | https://cherry.chem.bg.ac.rs/handle/123456789/106 | |
dc.description.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. | en |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/175023/RS// | |
dc.rights | openAccess | |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | |
dc.source | Pharmaceuticals | |
dc.subject | 3-carbomethoxy fentanyl | en |
dc.subject | Acute toxicity | en |
dc.subject | Fentanyl | en |
dc.subject | Hot plate | en |
dc.subject | Mice | en |
dc.subject | Rotarod | en |
dc.title | Pharmacological evaluation of 3-carbomethoxy fentanyl in mice | en |
dc.type | article | |
dc.rights.license | BY | |
dc.citation.volume | 4 | |
dc.citation.issue | 2 | |
dc.citation.spage | 233 | |
dc.citation.epage | 243 | |
dc.identifier.doi | 10.3390/ph4020233 | |
dc.citation.other | 4(2): 233-243 | |
dc.type.version | publishedVersion | |
dc.identifier.scopus | 2-s2.0-79551591943 | |
dc.identifier.fulltext | https://cherry.chem.bg.ac.rs/bitstream/id/8257/104.pdf |