Počet záznamů: 1
Pharmacokinetic, pharmacodynamic, and behavioural studies of deschloroketamine in Wistar rats
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SYSNO ASEP 0555872 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Pharmacokinetic, pharmacodynamic, and behavioural studies of deschloroketamine in Wistar rats Tvůrce(i) Štefková-Mazochová, K. (CZ)
Danda, H. (CZ)
Dehaen, W. (CZ)
Jurásek, B. (CZ)
Šíchová, K. (CZ)
Pinterová-Leca, N. (CZ)
Mazoch, V. (CZ)
Hrčka Krausová, Barbora (FGU-C) ORCID, RID
Kysilov, Bohdan (FGU-C) ORCID, SAI
Smejkalová, Tereza (FGU-C) RID, ORCID
Vyklický ml., Ladislav (FGU-C) RID, ORCID, SAI
Kohout, M. (CZ)
Hájková, K. (CZ)
Svozil, Daniel (UMG-J)
Horsley, R. R. (CZ)
Kuchař, M. (CZ)
Páleníček, T. (CZ)Zdroj.dok. British Journal of Pharmacology. - : Wiley - ISSN 0007-1188
Roč. 179, č. 1 (2022), s. 65-83Poč.str. 19 s. Jazyk dok. eng - angličtina Země vyd. GB - Velká Británie Klíč. slova deschloroketamine ; enantiomers ; locomotion ; NMDA receptor ; pharmacokinetics ; pharmacokinetics Obor OECD Pharmacology and pharmacy CEP GA20-17945S GA ČR - Grantová agentura ČR EF16_025/0007444 GA MZd - Ministerstvo zdravotnictví LM2018130 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy Výzkumná infrastruktura CZ-OPENSCREEN III - 90130 - Ústav molekulární genetiky AV ČR, v. v. i. Způsob publikování Open access Institucionální podpora FGU-C - RVO:67985823 ; UMG-J - RVO:68378050 UT WOS 000713032600001 EID SCOPUS 85118308442 DOI 10.1111/bph.15680 Anotace Background and purpose: Deschloroketamine (DCK), a structural analogue of ketamine, has recently emerged on the illicit drug market as a recreational drug with a modestly long duration of action. Despite it being widely used by recreational users, no systematic research on its effects has been performed to date. Experimental approach: Pharmacokinetics, acute effects, and addictive potential in a series of behavioural tests in Wistar rats were performed following subcutaneous (s.c.) administration of DCK (5, 10, and 30 mg center dot kg(-1)) and its enantiomers S-DCK (10 mg center dot kg(-1)) and R-DCK (10 mg center dot kg(-1)). Additionally, activity at human N-methyl-d-aspartate (NMDA) receptors was also evaluated. Key results: DCK rapidly crossed the blood brain barrier, with maximum brain levels achieved at 30 min and remaining high at 2 h after administration. Its antagonist activity at NMDA receptors is comparable to that of ketamine with S-DCK being more potent. DCK had stimulatory effects on locomotion, induced place preference, and robustly disrupted PPI. Locomotor stimulant effects tended to disappear more quickly than disruptive effects on PPI. S-DCK had more pronounced stimulatory properties than its R-enantiomer. However, the potency in disrupting PPI was comparable in both enantiomers. Conclusion and implications: DCK showed similar behavioural and addictive profiles and pharmacodynamics to ketamine, with S-DCK being in general more active. It has a slightly slower pharmacokinetic profile than ketamine, which is consistent with its reported longer duration of action. These findings have implications and significance for understanding the risks associated with illicit use of DCK. Pracoviště Fyziologický ústav Kontakt Lucie Trajhanová, lucie.trajhanova@fgu.cas.cz, Tel.: 241 062 400 Rok sběru 2023 Elektronická adresa https://doi.org/10.1111/bph.15680
Počet záznamů: 1