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Mephedrone (4-Methylmethcathinone): acute behavioral effects, hyperthermic, and pharmacokinetic profile in rats

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00023752%3A_____%2F18%3A43919216" target="_blank" >RIV/00023752:_____/18:43919216 - isvavai.cz</a>

  • Alternative codes found

    RIV/00216208:11110/18:10371152 RIV/00216208:11120/18:43916063 RIV/00064165:_____/18:10371152 RIV/00216208:11310/18:10371152

  • Result on the web

    <a href="https://www.frontiersin.org/articles/10.3389/fpsyt.2017.00306/full#h2" target="_blank" >https://www.frontiersin.org/articles/10.3389/fpsyt.2017.00306/full#h2</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.3389/fpsyt.2017.00306" target="_blank" >10.3389/fpsyt.2017.00306</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Mephedrone (4-Methylmethcathinone): acute behavioral effects, hyperthermic, and pharmacokinetic profile in rats

  • Original language description

    Mephedrone (MEPH) is a synthetic cathinone derivative with effects that mimic MDMA and/or cocaine. Our study in male Wistar rats provides detailed investigations of MEPH’s and its primary metabolite nor-mephedrone’s (nor-MEPH) pharmacokinetics and bio-distribution to four different substrates (serum, brain, lungs, and liver), as well as comparative analysis of their effects on locomotion [open field test (OFT)] and sensorimotor gating [prepulse inhibition of acoustic startle reaction (PPI ASR)]. Furthermore, in order to mimic the crowded condition where MEPH is typically taken (e.g., clubs), the acute effect of MEPH on thermoregulation in singly- and group-housed rats was evaluated. Pharmacokinetics of MEPH and nor-MEPH after MEPH (5 mg/kg, sc.) were analyzed over 8 h using liquid chromatography with mass spectrometry. MEPH (2.5, 5, or 20 mg/kg, sc.) and nor-MEPH (5 mg/kg, sc.) were administered 5 or 40 min before the behavioral testing in the OFT and PPI ASR; locomotion and its spatial distribution, ASR, habituation and PPI itself were quantified. The effect of MEPH on rectal temperature was measured after 5 and 20 mg/kg, sc. Both MEPH and nor-MEPH were detected in all substrates, with the highest levels detected in lungs. Mean brain: serum ratios were 1:1.19 (MEPH) and 1:1.91 (nor-MEPH), maximum concentrations were observed at 30 min; at 2 and 4 h after administration, nor-MEPH concentrations were higher compared to the parent drug. While neither of the drugs disrupted PPI, both increased locomotion and affected its spatial distribution. The effects of MEPH were dose dependent, rapid, and short-lasting, and the intensity of locomotor stimulant effects was comparable between MEPH and nor-MEPH. Despite the disappearance of behavioral effects within 40 min after administration, MEPH induced rectal temperature elevations that persisted for 3 h even in singly housed rats. To conclude, we observed a robust, short-lasting, and most likely synergistic stimulatory effect of both drugs which corresponded to brain pharmacokinetics. The dissociation between the duration of behavioral and hyperthermic effects is indicative of the possible contribution of nor-MEPH or other biologically active metabolites. This temporal dissociation may be related to the risk of prolonged somatic toxicity when stimulatory effects are no longer present.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    30215 - Psychiatry

Result continuities

  • Project

    Result was created during the realization of more than one project. More information in the Projects tab.

  • Continuities

    P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Others

  • Publication year

    2018

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    Frontiers in Psychiatry

  • ISSN

    1664-0640

  • e-ISSN

  • Volume of the periodical

    8

  • Issue of the periodical within the volume

    "Article Number: 306"

  • Country of publishing house

    CH - SWITZERLAND

  • Number of pages

    11

  • Pages from-to

    1-11

  • UT code for WoS article

    000419702000001

  • EID of the result in the Scopus database

    2-s2.0-85040465705