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  1. Article: Acute pharmacological profile of 2C-B-Fly-NBOMe in male Wistar rats-pharmacokinetics, effects on behaviour and thermoregulation.

    Syrová, Kateřina / Šíchová, Klára / Danda, Hynek / Lhotková, Eva / Jorratt, Pascal / Pinterová-Leca, Nikola / Vejmola, Čestmír / Olejníková-Ladislavová, Lucie / Hájková, Kateřina / Kuchař, Martin / Horáček, Jiří / Páleníček, Tomáš

    Frontiers in pharmacology

    2023  Volume 14, Page(s) 1120419

    Abstract: Introduction: ...

    Abstract Introduction:
    Language English
    Publishing date 2023-03-09
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2587355-6
    ISSN 1663-9812
    ISSN 1663-9812
    DOI 10.3389/fphar.2023.1120419
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Pharmacokinetics, systemic toxicity, thermoregulation and acute behavioural effects of 25CN-NBOMe.

    Šíchová, Klára / Syrová, Kateřina / Kofroňová, Edita / Pinterova-Leca, Nikola / Vejmola, Čestmír / Nykodemová, Jitka / Palivec, Petr / Olejníková, Lucie / Danda, Hynek / Jorratt, Pascal / Adam, Šafanda / Hiep, Bui Quang / Štefková-Mazochová, Kristýna / Končická, Markéta / Kuchař, Martin / Páleníček, Tomáš

    Addiction biology

    2022  Volume 27, Issue 5, Page(s) e13216

    Abstract: N-(2-methoxybenzyl)phenethylamines (NBOMes) are a family of potent 5- ... ...

    Abstract N-(2-methoxybenzyl)phenethylamines (NBOMes) are a family of potent 5-HT
    MeSH term(s) Animals ; Body Temperature Regulation ; Dose-Response Relationship, Drug ; Hallucinogens/pharmacology ; Phenethylamines ; Rats ; Rats, Wistar
    Chemical Substances Hallucinogens ; Phenethylamines
    Language English
    Publishing date 2022-09-02
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1324314-7
    ISSN 1369-1600 ; 1355-6215
    ISSN (online) 1369-1600
    ISSN 1355-6215
    DOI 10.1111/adb.13216
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4586: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
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    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  3. Article ; Online: Effects of synthetic cathinone naphyrone in the conditioned place preference test - Evidence of its addictive potential.

    Danda, Hynek / Pinterová-Leca, Nikola / Šíchová, Klára / Štefková-Mazochová, Kristýna / Syrová, Kateřina / Olejníková, Lucie / Končická, Markéta / Mazoch, Vladimír / Lhotková, Eva / Kuchař, Martin / Páleníček, Tomáš

    Behavioural brain research

    2021  Volume 421, Page(s) 113713

    Abstract: Naphyrone, also known as NRG-1, is a novel psychoactive substance (NPS), a cathinone with stimulatory properties available on the grey/illicit drug market for almost a decade. It is structurally related to infamously known powerful stimulants with the ... ...

    Abstract Naphyrone, also known as NRG-1, is a novel psychoactive substance (NPS), a cathinone with stimulatory properties available on the grey/illicit drug market for almost a decade. It is structurally related to infamously known powerful stimulants with the pyrovalerone structure, such as alpha-pyrrolidinovalerophenone (α-PVP) or methylenedioxypyrovalerone (MDPV) that are labeled as a cheap replacement for cocaine and other stimulants. Despite the known addictive potential of α-PVP and MDPV, there are no studies directly evaluating naphyrone's addictive potential e.g., in conditioned place preference (CPP) test or using self-administration. Therefore, our study was designed to evaluate the addictive potential in a CPP test in male Wistar rats and compare its effect to another powerful stimulant with a high addictive potential - methamphetamine. Naphyrone increased time spent in the drug-paired compartment with 5 and 20 mg/kg s.c. being significant and 10 mg/kg s.c. reaching the threshold (p = 0.07); the effect was comparable to that of methamphetamine 1.5 mg/kg s.c. The lowest dose, naphyrone 1 mg/kg s.c., had no effect on CPP. Interestingly, no dose response effect was detected. Based on these data, we are able to conclude that naphyrone has an addictive potential and may possess a significant risk to users.
    MeSH term(s) Alkaloids/pharmacology ; Animals ; Behavior, Animal/drug effects ; Central Nervous System Stimulants/administration & dosage ; Central Nervous System Stimulants/pharmacology ; Conditioning, Classical/drug effects ; Disease Models, Animal ; Dose-Response Relationship, Drug ; Male ; Methamphetamine/administration & dosage ; Methamphetamine/pharmacology ; Pentanones/administration & dosage ; Pentanones/pharmacology ; Pyrrolidines/administration & dosage ; Pyrrolidines/pharmacology ; Rats ; Rats, Wistar ; Substance-Related Disorders
    Chemical Substances 1-naphthalen-2-yl-2-pyrrolidin-1-ylpentan-1-one ; Alkaloids ; Central Nervous System Stimulants ; Pentanones ; Pyrrolidines ; Methamphetamine (44RAL3456C) ; cathinone (540EI4406J)
    Language English
    Publishing date 2021-12-11
    Publishing country Netherlands
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 449927-x
    ISSN 1872-7549 ; 0166-4328
    ISSN (online) 1872-7549
    ISSN 0166-4328
    DOI 10.1016/j.bbr.2021.113713
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 1599: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

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  4. Article ; Online: Naphyrone (naphthylpyrovalerone): Pharmacokinetics, behavioural effects and thermoregulation in Wistar rats.

    Pinterova-Leca, Nikola / Horsley, Rachel R / Danda, Hynek / Žídková, Monika / Lhotková, Eva / Šíchová, Klára / Štefková, Kristýna / Balíková, Marie / Kuchař, Martin / Páleníček, Tomáš

    Addiction biology

    2020  Volume 26, Issue 2, Page(s) e12906

    Abstract: Naphthylpyrovalerone (naphyrone) is a pyrovalerone cathinone that potently inhibits monoamine transporters and provides stimulatory-entactogenic effects. Little is known about the safety of naphyrone or its effects in vivo, and more research is needed to ...

    Abstract Naphthylpyrovalerone (naphyrone) is a pyrovalerone cathinone that potently inhibits monoamine transporters and provides stimulatory-entactogenic effects. Little is known about the safety of naphyrone or its effects in vivo, and more research is needed to acquire knowledge about its fundamental effects on physiology and behaviour. Our objective was to investigate naphyrone's pharmacokinetics, acute toxicity, hyperthermic potential and stimulatory and psychotomimetic properties in vivo in male Wistar rats. Pharmacokinetics after 1 mg/kg subcutaneous (sc.) naphyrone were measured over 6 h in serum, the brain, liver and lungs. Rectal temperature (degree Celsius) was measured over 10 h in group-versus individually housed rats after 20 mg/kg sc. In the behavioural experiments, 5, 10 or 20 mg/kg of naphyrone was administered 15 or 60 min prior to testing. Stimulation was assessed in the open field, and sensorimotor processing in a prepulse inhibition (PPI) task. Peak concentrations of naphyrone in serum and tissue were reached at 30 min, with a long-lasting elevation in the brain/serum ratio, consistent with observations of lasting hyperlocomotion in the open field and modest increases in body temperature. Administration of 20 mg/kg transiently enhanced PPI. Naphyrone crosses the blood-brain barrier rapidly and is eliminated slowly, and its long-lasting effects correspond to its pharmacokinetics. No specific signs of acute toxicity were observed; therefore, clinical care and harm-reduction guidance should be in line with that available for other stimulants and cathinones.
    MeSH term(s) Animals ; Body Temperature/drug effects ; Body Temperature Regulation/drug effects ; Central Nervous System Stimulants/pharmacokinetics ; Central Nervous System Stimulants/pharmacology ; Illicit Drugs/pharmacokinetics ; Illicit Drugs/pharmacology ; Male ; Pentanones/pharmacokinetics ; Pentanones/pharmacology ; Pyrrolidines/pharmacokinetics ; Pyrrolidines/pharmacology ; Rats ; Rats, Wistar
    Chemical Substances 1-naphthalen-2-yl-2-pyrrolidin-1-ylpentan-1-one ; Central Nervous System Stimulants ; Illicit Drugs ; Pentanones ; Pyrrolidines
    Language English
    Publishing date 2020-05-07
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1324314-7
    ISSN 1369-1600 ; 1355-6215
    ISSN (online) 1369-1600
    ISSN 1355-6215
    DOI 10.1111/adb.12906
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4586: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  5. Article ; Online: Pharmacokinetic, pharmacodynamic, and behavioural studies of deschloroketamine in Wistar rats.

    Štefková-Mazochová, Kristýna / Danda, Hynek / Dehaen, Wim / Jurásek, Bronislav / Šíchová, Klára / Pinterová-Leca, Nikola / Mazoch, Vladimír / Krausová, Barbora Hrčka / Kysilov, Bohdan / Smejkalová, Tereza / Vyklický, Ladislav / Kohout, Michal / Hájková, Kateřina / Svozil, Daniel / Horsley, Rachel R / Kuchař, Martin / Páleníček, Tomáš

    British journal of pharmacology

    2021  Volume 179, Issue 1, Page(s) 65–83

    Abstract: 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 ... ...

    Abstract 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·kg
    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.
    MeSH term(s) Animals ; Behavior, Animal/drug effects ; Illicit Drugs/adverse effects ; Illicit Drugs/pharmacokinetics ; Illicit Drugs/pharmacology ; Ketamine/administration & dosage ; Ketamine/adverse effects ; Ketamine/analogs & derivatives ; Ketamine/pharmacokinetics ; Ketamine/pharmacology ; Locomotion/drug effects ; Rats ; Rats, Wistar ; Receptors, N-Methyl-D-Aspartate/metabolism
    Chemical Substances Illicit Drugs ; Receptors, N-Methyl-D-Aspartate ; Ketamine (690G0D6V8H)
    Language English
    Publishing date 2021-10-31
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 80081-8
    ISSN 1476-5381 ; 0007-1188
    ISSN (online) 1476-5381
    ISSN 0007-1188
    DOI 10.1111/bph.15680
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Uf I Zs.146: Show issues Location:
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