EWS_EU: neue psychoaktive Sub......
#1 Geschrieben : Samstag, 8. November 2014 15:58:06(UTC)
Rang: Advanced Member

Beiträge: 213

Sehr geehrte Fachleute,
hiermit leite ich Ihnen die aktuellsten Informationen der EMCDDA zu neuen psychoaktiven Substanzen weiter.

In Polen wurde die neue psychoaktive Substanz 3-(2,4-dimethylphenyl)-2-methylquinazolin-4(3H)-one (methylmethaqualone) identifiziert.

Methylmethaqualone (also known as MMQ) belongs to the quinazoline class of drugs and is the methyl analogue of methaqualone, which is reported as exhibiting sedative-hypnotic, anticonvulsant and anxiolytic properties via action on the GABA-A receptor [1]. Methylmethaqualone was identified in a seizure of 0.3g of white powder, seized by Polish customs in Warsaw in January 2013. The substance was analytically confirmed by GC-MS.
A serious adverse event associated with methylmethaqualone was reported in the literature in 2013, documenting the case of a 24 year old male who was admitted to hospital with "severe psychomotor agitation with generalized clonic muscle contractions and urinary incontinence" following ingestion of up to two 500mg tablets of methylmethaqualone [1]. Subsequently, 10mg of midazolam was administered resulting in an improvement in agitation. A neurological examination performed in hospital revealed mild generalised resting tremor of the upper and lower limbs. Toxicological analysis identified methylmethaqualone as the only substance present. The same individual attended the hospital ten days later presenting the same symptoms following ingestion of the same quantity of methylmethaqualone [1]. Methylmethaqualone was first identified in Germany in 1997 and subsequently placed under control there in 1999 [4,5]. There are also online user reports discussing methylmethaqualone [2,3].

[1]. Ceschi, A., Giardelli, G., Müller, D. M., Elavumkudy, S., Manini, A. F., Rauber-Lüthy, C., & Hofer, K. E. (2013). Acute neurotoxicity associated with recreational use of methylmethaqualone confirmed by liquid chromatography tandem mass spectrometry. Clinical Toxicology, 51(1), 54-57.
[2]. https://www.drugs-forum..../showthread.php?t=55414
[3]. http://www.chemsrus.com/...5931-methylmethaqualone
[4]. King L, Pooriman-van Der Meer A. New synthetic drugs in the European Union. Journal of the Clandestine Laboratory Investigating Chemists Association. 1998;8(3):13–4.
[5]. http://www.emcdda.europa...677&lang=en&T=2
Angelos SA, Lankin DC, Meyers JA, Raney JK. The structural identification of a methyl analog of methaqualone via 2-dimensional NMR techniques. J Forensic Sci 1993;38(2):455.

In Schweden wurden folgende drei neue psychoaktive Substanzen identifiziert.

1. N-(2-amino-1-benzyl-2-oxo-ethyl)-1-[(4-fluorophenyl)methyl]indazole-3-carboxamide is a synthetic cannabinoid which is also known as N-(1-amino-3-phenyl-1-oxopropan-2-yl)-1-[(4-fluorophenyl)methyl]-1H-indazole-3-carboxamide. We suggest APP-FUBINACA as a short name for this substance based on the naming conventions put forward for similar structures that have been notified to the EWS. We have opted for the acronym 'APP' to signify the 'amino', 'phenyl' and 'propanone' elements of the structure. Thus, this substance is structurally similar to that of AB-FUBINACA (where the AB relates to 'amino' and 'butanone') which was first reported to the EWS in July 2013.

2. N-(2-amino-1-benzyl-2-oxo-ethyl)-1-(5-fluoropentyl)indazole-3-carboxamide is also known as the following: N-(1-amino-1-oxo-3-phenylpropan-2-yl)-1-(5-fluoropentyl)-1H-indazole-3-carboxamide and is available online as PX-2 (PX 2) [1]. We suggest 5F-APP-PINACA as a naming convention for this substance based on the rationale outlined above. 5F-APP-PINACA is an analogue of 5F-AB-PINACA.
APP-FUBINACA and 5F-APP-PINACA were identified in a seizure of 11.5 g of white powder, seized by Swedish Customs in Stockholm on the 19th of September 2014. The substances were analytically confirmed by GC-MS, LC-MS and NMR.
[1]. https://www.caymanchem.c...roduct.vm/catalog/16434

3. MDPHP = 1-(1,3-benzodioxol-5-yl)-2-pyrrolidin-1-yl-hexan-1-one is a synthetic cathinone which is a higher homologue of MDPV, the alkyl chain being extended by one carbon. It can also be considered to be the 3,4-methylenedioxy analogue of α-PHP. There has been some discussion of this substance on drug forums [1,2]. MDPHP was identified in a seizure of 10 g of brown powder, seized by Swedish Police in Västerås on the 18th of September 2014. The substance was analytically confirmed by GC-MS, GC-IRD and NMR.
[1]. http://www.chemsrus.com/...mphp-not-mdph-but-mdphp
[2]. http://www.bluelight.org...uran-analogue-of-PVP%29

Des Weiteren informierte uns die EMCDDA über zwei Todesfälle in Schweden im Zusammenhang mit dem Konsum von 4F-α-PVP (1-(4-fluorophenyl)-2-(pyrrolidin-1-yl)pentan-1-one). Im ersten Fall wurde diese Substanz zusammen mit weiteren Substanzen im Obduktionsgut (femoral blood: 0.42μg/g 4F-α-PVP, methadone 0.38μg/g, MT-45 0.14μg/g, flubromazepam 0.14μg/g) nachgewiesen. Im zweiten Fall verstarb die Person unmittelbar durch einen Sturz aus dem Fenster. Im Obduktiongut (femoral blood) dieser Person wurde die Substanz 4F-α-PVP (4.6μg/g) nachgewiesen.

Betreff: EWS Alert 4F-α-PVP

Dear Colleagues,
2 deaths associated with 4F-α-PVP (1-(4-fluorophenyl)-2-(pyrrolidin-1-yl)pentan-1-one). The Swedish National Focal Point has reported 2 deaths associated with 4F-α-PVP. The cases occurred in 2014. These are the first such case to be reported to the Early Warning System. Case 1: Substances
detected post-mortem: 4F-α-PVP (0.42μg/g femoral blood); methadone (0.38μg/g femoral blood); MT-45 (0.14μg/g femoral blood); flubromazepam (0.14μg/g femoral blood). Case 2: Substances detected post-mortem: 4F-α-PVP (4.6μg/g femoral blood). The person fell out of a window. The data was provided by the National Board of Forensic Medicine, Department of Forensic Genetics and Forensic Toxicology.

4F-α-PVP was first notified by Sweden in February 2014 based on its identification in a seizure made by Swedish Customs of 24.6 grams of white powder. The structure was verified with GC-MS and NMR at the Swedish National Laboratory of Forensic Science. 4F-α-PVP has also been detected in 3 other countries (BE, FI, RO). Chemical and analytical details: 4F-α-PVP is a synthetic cathinone and an isomer of α-PVP, characterised by the addition of a fluorine group at the 4 position of the phenyl ring. The synthesis of 4F-α-PVP is described by Meltzer et al., (see compound 4e) [1]. Other names and abbreviations: 4-fluoro-α-PVP; 4F-PVP; 4-fluoro-α-2-(1-pyrrolidinyl)-valerophenone; 4-fluoro-α-pyrollidinovalerophenone; O-2370. Pharmacology and toxicology: Meltzer et al., determined the ligand affinity (Ki, nM) of 4F-α-PVP and a range of other pyrovalerone derivatives for inhibition of the dopamine, norepinephrine, and serotonin transporters in competition studies with [125I]RTI 55. In addition, the inhibition of monoamine uptake (IC50, nM) was evaluated in competition with [3H]dopamine, [3H] serotonin, and [3H]norepinephrine. The comparator was cocaine. 4F-α-PVP (compound 4e) was found to be a potent inhibitor of the dopamine transporter (DAT) (82.0 ± 25 nM cf. 33.7 ± 5.4 for α-PVP cf. 432 ± 29 for cocaine) and of dopamine reuptake (185 ± 62 nM cf. 52.3 ± 6.2 α-PVP cf. 461 ± 46 cocaine); a less potent inhibitor of the noradrenaline transporter (NET) (830±140 nM cf. 199 ± 45 α-PVP cf. 2150 ± 190 cocaine) and of noradrenaline reuptake (171 ± 35 nM cf. 56.0 ± 13 α-PVP cf. 378 ± 48 cocaine); and no significant effect at the serotonin transporter (SERT) (>10μM cf. >10μM α-PVP cf. 358 ± 24 nM cocaine) and on serotonin uptake [1]. Note α-PVP is compound 4d in the paper. Self-reported user experiences suggests that 4F-α-PVP may have stimulant-type effects. Data are not available on the toxicology of 4F-α-PVP. Epidemiology: Information on the use of 4F-α-PVP is largely limited to self-reported experiences on user websites, see: https://www.google.pt/se...?q="4F-α-PVP" OR "4F-PVP"
1. Meltzer PC, Butler D, Deschamps JR, Madras BK. 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. J Med Chem. 2006;49(4):1420–32.

Sollten zu den oben genannten Substanzen Informationen aus Österreich vorliegen, bitten wir um Weiterleitung an ews@goeg.at.

Mit freundlichen Grüßen
Andrea Bodenwinkler

Informations – und Frühwarnsystem über besondere Gesundheitsgefahren im Zusammenhang mit Substanzkonsum
Aktuelle Informationen und Warnungen: https://forum.goeg.at/ewsforum/

Dr. Andrea Bodenwinkler
Gesundheit Österreich GmbH
Stubenring 6
1010 Wien
T: +43 1 515 61-187
F: +43 1 513 84 72

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