Methylone and mCPP, two new drugs of abuse? Addic Biol

Drugs Information and Monitoring System (DIMS), Trimbos Institute for Mental Health and Addiction, Utrecht, the Netherlands.
Addiction Biology (Impact Factor: 5.36). 01/2006; 10(4):321-3. DOI: 10.1080/13556210500350794
Source: PubMed


Recently, two new ecstasy-like substances, methylone and mCPP, were found in street drugs in the Netherlands by the Drugs Information and Monitoring System (DIMS). Methylone (3,4-methylenedioxymethcathinone) is the main ingredient of a new liquid designer drug that appeared on the Dutch drug market, called 'Explosion'. mCPP (meta-chlorophenylpiperazine) is a substance often used as a probe for the serotonin function in psychiatric research, and has now been found in street drugs, both in tablets and powders. Methylone as well as mCPP act on monoaminergic systems, resembling MDMA (3,4-methylenedioxymethamphetamine), with mCPP mainly affecting the serotonin system. The subjective effects of both new substances exhibit subtle differences with those of MDMA. Only little is known about the harmfulness of both methylone and mCPP. However, because of similarities between these substances and MDMA, risks common to MDMA cannot be excluded.

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Available from: Matthijs G Bossong
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    • "mCPP presents lower neurotoxic potential than methylenedioxymethamphetamine (MDMA), but its negative effects can be very harmful to the body (dizziness, confusion, tremors, headache and even panic attacks), similar to serotonin syndrome in psychiatric patients (Feuchtl et al., 2004; Gijsman et al., 1998; Gobbi et al., 2002). Adverse effects reported after abuse of mCPP include hallucinations , dizziness, and panic attacks, with high doses leading to respiratory depression and death (Bossong et al., 2005; EMCDDA, 2007; Gee et al., 2005). "
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    ABSTRACT: Chlorophenylpiperazines (CPP) are psychotropic drugs used in nightclub parties and are frequently used in a state of sleep deprivation, condition which can potentiate the effects of psychoactive drugs. This study aimed to investigate the effects of sleep deprivation and sleep rebound (RB) on anxiety-like measures in mCPP-treated mice using the open field test. We first optimized our procedure by performing dose-effect curves and examining different pretreatment times in naïve male Swiss mice. Subsequently, a separate cohort of mice underwent paradoxical sleep deprivation (PSD) for 24 or 48 hours. In the last experiment, immediately after the 24h-PSD period, mice received an injection of saline or mCPP, but their general activity was quantified in the open field only after the RB period (24 or 48 hours). The dose of 5 mg.mL(-1) of mCPP was the most effective at decreasing rearing behavior, with peak effects 15 minutes after injection. PSD decreased locomotion and rearing behaviors, thereby inhibiting a further impairment induced by mCPP. Plasma concentrations of mCPP were significantly higher in PSD 48h animals compared to the non PSD control group. Twenty-four hours of RB combined with mCPP administration produced a slight reduction in locomotion. Our results show that mCPP was able to significantly change the behavior of naïve, PSD, and RB mice. When combined with sleep deprivation, there was a higher availability of drug in plasma levels. Taken together, our results suggest that sleep loss can enhance the behavioral effects of the potent psychoactive drug, mCPP, even after a period of rebound sleep.
    Full-text · Article · Nov 2013 · Progress in Neuro-Psychopharmacology and Biological Psychiatry
    • "Therefore, there is a need for methods to distinguish mCPP among its positional isomers in confiscated materials. The 1-(3-chlorophenyl)piperazine (mCPP), originally known as a serotonine probe in psychiatric research or as the active metabolite of the antidepressant Trazodone, has been recently abused aspsychoactive substance in clandestine party pills[4]. The subjective experiences after mCPP ingestion are described to be similar to those of 3,4-methylenedioxymethamphetamine (MDMA, ecstasy) of both negative (dysphoria, anxiety) and positive (euphoria) effects[5]. "
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    ABSTRACT: A simple capillary electrophoretic method with spectrophotometric UV detection at 236nm has been developed for the selective separation and determination of 1-(2-chlorophenyl)piperazine (oCPP), 1-(3-chlorophenyl)piperazine (mCPP) and 1-(4-chlorophenyl)piperazine (pCPP) in confiscated pills. Several cyclodextrin derivatives were tested to compose the background electrolyte (BGE). The optimized BGE contained 20mmol/L phosphoric acid adjusted to pH 2.5 with triethylamine and 10mmol/L α-cyclodextrin, which provided acceptable resolution of analytes and candidate interferents in less than 15min. The analyses were performed at constant voltage of 25kV in 60cm (effective length 50cm; 50μm i.d.) uncoated fused-silica capillary maintained at 25°C with sample injection at 4826Pa for 8s. Procaine at a concentration of 0.1mg/mL was used as internal standard (IS). Possible interference from other drugs such as amphetamine, methamphetamine, 3,4-methylenedioxyamphetamine, 3,4-methylenedioxymethamphetamine, 3,4-methylenedioxy-N-ethylamphetamine, 1-(3-trifluoromethylphenyl)piperazine and cocaine was also examined. The analytical curves were linear (R(2)=0.9994-0.9995) in the range of 10-200μg/mL (for oCPP and mCPP) and 20-200μg/mL for pCPP. Limits of detection (LODs) were 2.0μg/mL (oCPP), 2.5μg/mL (mCPP) and 3.5μg/mL (pCPP). Intraday precision at three concentration levels and six replicates of each level (10, 100, 200μg/mL of each analyte; n=18) was evaluated for the corrected peak area ratio of analyte to IS and the migration times giving RSDs≤4.9%. The accuracy was estimated for mCPP by a recovery test at the same three concentration levels and recoveries varied from 101.0 to 101.6%. The method has been successively applied to the analysis of 17 confiscated pills based mostly on mCPP.
    No preview · Article · Jun 2013 · Journal of pharmaceutical and biomedical analysis
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    • "A primary goal of this study was to determine the mechanism of action for the designer methcathinone analogs, mephedrone, and methylone. Despite widespread nonmedical use of these agents (Bossong et al, 2005; Karila Figure 8 Acute and long-term effects of repeated administrations of methylone (MDMC) in single-housed male rats. MDMC-treated rats received s.c. "
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    ABSTRACT: The nonmedical use of ‘designer’ cathinone analogs, such as 4-methylmethcathinone (mephedrone) and 3,4-methylenedioxymethcathinone (methylone), is increasing worldwide, yet little information is available regarding the mechanism of action for these drugs. Here, we employed in vitro and in vivo methods to compare neurobiological effects of mephedrone and methylone with those produced by the structurally related compounds, 3,4-methylenedioxymethamphetamine (MDMA) and methamphetamine. In vitro release assays using rat brain synaptosomes revealed that mephedrone and methylone are nonselective substrates for plasma membrane monoamine transporters, similar to MDMA in potency and selectivity. In vivo microdialysis in rat nucleus accumbens showed that i.v. administration of 0.3 and 1.0 mg/kg of mephedrone or methylone produces dose-related increases in extracellular dopamine and serotonin (5-HT), with the magnitude of effect on 5-HT being greater. Both methcathinone analogs were weak motor stimulants when compared with methamphetamine. Repeated administrations of mephedrone or methylone (3.0 and 10.0 mg/kg, s.c., 3 doses) caused hyperthermia but no long-term change in cortical or striatal amines, whereas similar treatment with MDMA (2.5 and 7.5 mg/kg, s.c., 3 doses) evoked robust hyperthermia and persistent depletion of cortical and striatal 5-HT. Our data demonstrate that designer methcathinone analogs are substrates for monoamine transporters, with a profile of transmitter-releasing activity comparable to MDMA. Dopaminergic effects of mephedrone and methylone may contribute to their addictive potential, but this hypothesis awaits confirmation. Given the widespread use of mephedrone and methylone, determining the consequences of repeated drug exposure warrants further study.Keywords: dopamine; MDMA; mesolimbic; microdialysis; serotonin (5-HT); transporters
    Full-text · Article · Dec 2011 · Neuropsychopharmacology
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