We report the presence of a new substance detected in the hidden web as an adulterant of heroin, ocfentanil. It has short acting opioid-like effects, roughly the same potency as fentanyl, and can be injected, snorted or smoked. Severe side effects have been associated with its use, including one death. No discussion about this substance could be found in the Internet, which suggests this substance has not been sold as such. Available data about purities of drugs purchased in cryptomarkets suggest that adulteration is not a severe problem and this agrees with users' perceptions. However, this study suggests that adulteration is a real threat not only at the street level, but also for users that buy substances in cryptomarkets, and suggest the need for harm reduction initiatives in this setting.
New psychoactive substances have been rapidly growing in popularity in the drug market as non-illegal drugs. In the last few years, an increment has been reported on the use of synthetic alternatives to heroin, the synthetic opioids. Based on the information provided by the European Monitoring Centre for Drug and Drug Addiction, these synthetic opioids have been related to overdoses and deaths in Europe and North America. One of these opioids is the U-47700. A few months ago, U-47700 was scheduled in the U.S. and other countries, and other opioid derivatives have been appearing in order to replace it. One of these compounds is U-49900, an analog of U-47700. A white powder sample was obtained from an anonymous user in Spain. After an accurate characterization by gas chromatography-mass spectrometry, ultra-high performance liquid chromatography-high resolution mass spectrometry, nuclear magnetic resonance and single-crystal X-ray diffraction; and complemented by Fourier-transformed infrared spectroscopy, ultraviolet and circular dichroism spectrophotometry, the drug sample was unequivocally identified as U-49900. The information provided will be useful for the Early Warning System and forensic laboratories for future identifications of the U-49900, as well as in tentative identifications of other related opioids.
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.
In this work, the identification and characterization of the novel synthetic cathinone 5-PPDI found in a suspect drug sample was performed.
MethodsThe suspect sample was analyzed by gas chromatography-mass spectrometry (GC-MS), Fourier-transformed infrared spectroscopy (FTIR), ultra-high performance liquid chromatography-high-resolution mass spectrometry (UHPLC-HRMS) and nuclear magnetic resonance (NMR).
ResultsThe fragmentation observed in GC-MS and the identification of functional groups by FTIR were not enough for compound identification. After an exhaustive analysis of the accurate-mass fragmentation observed in HRMS, the compound was tentatively identified as the novel cathinone 5-PPDI. Finally, five different NMR experiments were used for the unequivocal identification and complete characterization of the compound. In addition, the origin of this cathinone was investigated in depth.
ConclusionsThe analytical data provided in this work will be useful for the identification of 5-PPDI by forensic laboratories. In addition, the origin of this cathinone has been investigated, which could be of interest for the identification of future synthetic cathinones prepared following the same synthesis route than that employed for obtaining 5-PPDI.
Despite the fact that 33% of the new psychoactive substances seized in 2015 were synthetic cathinones, the number of these derivatives has been decreasing in the last years, probably as a consequence of the unfavourable effects reported by users. Thus, the list of possible cathinone analogues is expected to get shorter, and it is likely that the same moiety changes applied for the preparation of synthetic cathinones will be applied in the near future to other stimulants in the search for favourable alternatives to controlled substances. This is evidenced by the increase in newly reported substances belonging to stimulant classes other than cathinones. One of the possible candidates for a new backbone from which to base new stimulants is aminorex, which is classified as a Schedule I substance by the Drug Enforcement Administration. Three derivatives have been reported until now: 4-methylaminorex or 4-MAR (also categorized as a Schedule I substance), para-methyl-4-methylaminorex (4,4′-DMAR) and 3′,4′-methylenedioxy-4-methylaminorex (MDMAR). Recently, the new halogenated 4-MAR derivative, para-fluoro-4-methylaminorex, characterised in this work (and abbreviated as pF-4-methylaminorex or 4′F-4-MAR) was detected by the Slovenian police. In the present work, 4′F-4-MAR has been characterized by high resolution mass spectrometry and nuclear magnetic resonance in a sample obtained from an anonymous consumer. This research shows that the same modifications applied for the preparation of synthetic cathinones are being used to prepare new stimulants based on the aminorex backbone.
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