Patterns of use and toxicity of new para‐halogenated substituted cathinones: 4‐<scp>CMC</scp> (clephedrone), 4‐<scp>CEC</scp> (4‐chloroethcatinone) and 4‐<scp>BMC</scp> (brephedrone)

Grifell, M.; Ventura, Montserrat Carbonell; Carbón, Xoán; Quintana, P.; Galindo, L.; Palma, Á.; Fornís, I.; Gil, Cristina; Farré, Magı́; Torrens, Marta

doi:10.1002/hup.2621

Cited by 34 publications

(26 citation statements)

References 48 publications

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“…Despite the growing popularity of chloromethcathinones on the recreational drugs' market and documented cases of acute intoxication in humans, little is known on their cytotoxic activity (Adamowicz et al 2020;Grifell et al 2017;Odoardi et al 2016;Taschwer et al 2014;Tomczak et al 2018). The present study demonstrates that 3-CMC does not produce significant cytotoxicity against SH-SY5Y neuroblastoma cells after 24-h incubation, while 4-CMC slightly, but statistically significantly decreases cell viability, measured as mitochondrial function, at 200 and 300 μM.…”

Section: -Meo-pvpmentioning

confidence: 46%

Four Synthetic Cathinones: 3-Chloromethcathinone, 4-Chloromethcathinone, 4-Fluoro-α-Pyrrolidinopentiophenone, and 4-Methoxy-α-Pyrrolidinopentiophenone Produce Changes in the Spontaneous Locomotor Activity and Motor Performance in Mice with Varied Profiles

2020

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Two chloromethcathinones, 3-chloromethcathinone (3-CMC) and 4-chloromethcathinone (4-CMC), and two para-substituted α-pyrrolidinophenones, 4-methoxy-α-pyrrolidinopentiophenone (4-MeO-PVP) and 4-fluoro-α-pyrrolidinopentiophenone (4-F-PVP), represent synthetic cathinones, the second most frequently abused group of new psychoactive substances (NPSs), which has aroused a worldwide health concern in the last decade. Synthetic cathinones act as psychostimulants by elevating extracellular levels of monoaminergic neurotransmitters. This study investigates effects of 3-CMC, 4-CMC, 4-MeO-PVP, and 4-F-PVP on the spontaneous locomotor activity and motor performance of mice. Additionally, neurotoxicity of substituted methcathinones against SH-SY5Y neuroblastoma cells was evaluated. All test cathinones stimulate in a dose-dependent manner horizontal locomotor activity of mice. Consistently to our prior findings, pyrrovalerones, but not methcathinone derivatives, produce dose-dependent elevation of vertical locomotor activity (rearing behavior). None of the tested compounds decreases the time spent on the accelerating rotarod, pointing to the lack of considerable motor disability in mice after acute exposition. Only 4-MeO-PVP at the high tested dose (20 mg/kg) increases motor performance of mice. Considering that α-pyrrolidinophenones are highly potent and selective DA uptake inhibitors, while chloromethcathinones enhance non-selective DA/5-HT release, we suggest that the increase of vertical locomotor activity and performance on rotarod in mice may serve as a behavioral indicator of the monoaminergic profile of synthetic cathinones. Finally, this study gives first insights into cytotoxicity of both 3-CMC and 4-CMC displayed against SH-SY5Y cells, which emerges and intensifies after prolonged incubation, suggesting the indirect mechanism of action, unrelated to interactions with monoamine transporters.

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Section: -Meo-pvpmentioning

confidence: 46%

Four Synthetic Cathinones: 3-Chloromethcathinone, 4-Chloromethcathinone, 4-Fluoro-α-Pyrrolidinopentiophenone, and 4-Methoxy-α-Pyrrolidinopentiophenone Produce Changes in the Spontaneous Locomotor Activity and Motor Performance in Mice with Varied Profiles

2020

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“…The 2C-B pill content was previously analyzed by means of gas chromatography associated with mass spectrometry (GC/MS). The method used permits to check for most common drugs of abuse including cocaine, MDMA, LSD, amphetamine and methamphetamine, heroin, 2C-B and other phenethylamines, DMT and other tryptamines, ketamine, psilocybin, salvinorin A, natural and synthetic cannabinoids, and most of the NPSs ( Caudevilla-Gálligo et al, 2012 ; González et al, 2015 ; Grifell et al, 2017 ; Palma-Conesa et al, 2017 ; Quintana et al, 2017 ). Participants were given a choice of three doses to choose from, 10, 15 or 20 mg 2C-B, based on their stated preference from previous experience.…”

Section: Methodsmentioning

confidence: 99%

Acute Pharmacological Effects of 2C-B in Humans: An Observational Study

et al. 2018

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2,5-dimethoxy-4-bromophenethylamine (2C-B) is a psychedelic phenylethylamine derivative, structurally similar to mescaline. It is a serotonin 5-hydroxytryptamine-2A (5-HT2A), 5-hydroxytryptamine-2B (5-HT2B), and 5-hydroxytryptamine-2C (5-HT2C) receptor partial agonist used recreationally as a new psychoactive substance. It has been reported that 2C-B induces mild psychedelic effects, although its acute pharmacological effects and pharmacokinetics have not yet been fully studied in humans. An observational study was conducted to assess the acute subjective and physiological effects, as well as pharmacokinetics of 2C-B. Sixteen healthy, experienced drug users self-administered an oral dose of 2C-B (10, 15, or 20 mg). Vital signs (blood pressure and heart rate) were measured at baseline 1, 2, 3, 4, and 6 hours (h). Each participant completed subjective effects using three rating scales: the visual analog scale (VAS), the Addiction Research Centre Inventory (ARCI), and the Evaluation of the Subjective Effects of Substances with Abuse Potential (VESSPA-SSE) at baseline, 2–3 and 6 h after self-administration (maximum effects along 6 h), and the Hallucinogenic Rating Scale (maximum effects along 6 h). Oral fluid (saliva) was collected to assess 2C-B and cortisol concentrations during 24 h. Acute administration of 2C-B increased blood pressure and heart rate. Scores of scales related to euphoria increased (high, liking, and stimulated), and changes in perceptions (distances, colors, shapes, and lights) and different body feelings/surrounding were produced. Mild hallucinating effects were described in five subjects. Maximum concentrations of 2C-B and cortisol were reached at 1 and 3 h after self-administration, respectively. Oral 2C-B at recreational doses induces a constellation of psychedelic/psychostimulant-like effects similar to those associated with serotonin-acting drugs.

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“…A public service group in New Zealand that tracks drug information and offers onsite chemical testing published a warning about severe adverse effects following N-ethylpentylone use, including that 13 people were hospitalized following its use (https://knowyourstuff.nz, 2018). Dibutylone, clephedrone and TH-PVP have been identified in seizures of illicit drugs (Grifell et al, 2017;Russell and Brogun 2011), and samples from postmortem examinations and testing for driving under intoxication (Krotulski et al, 2018a(Krotulski et al, , 2018bTomczak et al, 2018;Wille et al, 2018).…”

Section: Introductionmentioning

confidence: 99%

Locomotor activity and discriminative stimulus effects of five novel synthetic cathinone analogs in mice and rats

Gatch

Dolan

Forster

2019

Drug and Alcohol Dependence

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Background: The development of novel synthetic psychoactive substances continues to accelerate. There are little or no data on the pharmacological mechanisms, behavioral effects, or abuse liability of many of the newer compounds, despite increasing reports of severe adverse effects in recreational users. Methods: The current study investigated the discriminative stimulus and locomotor stimulant effects of a group of synthetic cathinone analogs: N-ethylpentylone, dimethylone, dibutylone, clephedrone, 3',4'-tetramethylene-α-pyrrolidinovalerophenone (TH-PVP). Locomotor activity was assessed in an open-field assay using Swiss-Webster mice. Discriminative stimulus effects were assessed in Sprague-Dawley rats trained to discriminate either cocaine, methamphetamine or MDMA from vehicle. Results: N-ethylpentylone, dimethylone, dibutylone and clephedrone increased locomotor activity. Maximal effects were similar among the test compounds. Relative potencies were: methamphetamine>N-ethylpentylone>clephedrone> dimethylone>MDMA> cocaine>dibutylone. TH-PVP dose-dependently depressed locomotor activity. N-ethylpentylone, dimethylone, dibutylone and clephedrone substituted fully for the discriminative stimulus effects of methamphetamine. N-ethylpentylone, dibutylone and clephedrone fully substituted for cocaine, whereas dimethylone produced a maximum of 67% drug-appropriate responding. Dimethylone, dibutylone and clephedrone fully substituted for MDMA, whereas N-ethylpentylone produced only 50% drug-appropriate responding. TH-PVP produced a maximum of 38% methamphetamine-appropriate responding, 50% cocaine-appropriate responding, and less than 1% MDMA-appropriate responding.

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Patterns of use and toxicity of new para‐halogenated substituted cathinones: 4‐CMC (clephedrone), 4‐CEC (4‐chloroethcatinone) and 4‐BMC (brephedrone)

Abstract: Since the emergence of these substances could prove to be the next step to the cat-and-mouse game existing between drug producers and legislation, further clinical and epidemiological research should be carried out in order to build evidence to support policy for public health issues.

Cited by 34 publications

References 48 publications

Four Synthetic Cathinones: 3-Chloromethcathinone, 4-Chloromethcathinone, 4-Fluoro-α-Pyrrolidinopentiophenone, and 4-Methoxy-α-Pyrrolidinopentiophenone Produce Changes in the Spontaneous Locomotor Activity and Motor Performance in Mice with Varied Profiles

Four Synthetic Cathinones: 3-Chloromethcathinone, 4-Chloromethcathinone, 4-Fluoro-α-Pyrrolidinopentiophenone, and 4-Methoxy-α-Pyrrolidinopentiophenone Produce Changes in the Spontaneous Locomotor Activity and Motor Performance in Mice with Varied Profiles

Acute Pharmacological Effects of 2C-B in Humans: An Observational Study

Locomotor activity and discriminative stimulus effects of five novel synthetic cathinone analogs in mice and rats

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