Naphyrone

Use in the United Kingdom

Naphyrone emerged as a new legal high in the United Kingdom only months after the ban of similar drug mephedrone (which was also a cathinone derivative). Until July 2010 the substance was not controlled by the Misuse of Drugs Act 1971 and was therefore not illegal for someone to possess. The Medicines Act prevented naphyrone from being sold for human consumption, and therefore it was sometimes sold as 'pond cleaner' or as another substance not normally consumed by humans.

A study by researchers at Liverpool John Moores University found that only one out of ten products labelled as "NRG-1" actually contained naphyrone when they were subjected to laboratory analysis. Compounds found in products labelled NRG-1 included MDPV, flephedrone, mephedrone, butylone and caffeine, one product tested was inorganic in composition. In the case of an individual possessing a product labelled NRG-1 that contains MDPV or other illegal substances, they are in possession of a controlled substance.

On 12 July 2010, the Home Office announced that naphyrone had been banned and made a Class B drug, following a report from the Advisory Council on the Misuse of Drugs.

Pharmacology

As a triple reuptake inhibitor, naphyrone has been shown in vitro to affect the reuptake of the neurotransmitters serotonin, dopamine and norepinephrine by interacting with the serotonin transporter (SERT), dopamine transporter (DAT), and norepinephrine transporter (NET).

One study found that the dissociation constant of naphyrone interacting with SERT is 33.1 nM ± 1.1, with DAT is 20.1 nM ± 7.1 and with NET is 136 nM ± 27. The concentration of naphyrone required to inhibit the transporters by 50% is 46.0 nM ± 5.5 for SERT, 40.0 nM ± 13 for DAT and 11.7 nM ± 0.9 for NET. Of a number of pyrovalerone analogues tested, naphyrone was found to be the only serotonin–norepinephrine–dopamine reuptake inhibitor found to be active at nM concentrations.

Some samples of β-naphyrone sold have also been found to contain the alternative isomer α-naphyrone, presumably produced accidentally as an impurity in synthesis. The in vitro data available in the scientific literature was all obtained using pure β-naphyrone, and the pharmacological properties of α-naphyrone are unknown, further complicating the pharmacological profile of this little-studied designer drug.

Legal status

Finland

Naphyrone is scheduled in the "government decree on psychoactive substances banned from the consumer market".

References

References

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4. (February 2006). "1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors". Journal of Medicinal Chemistry.
5. (2010-04-01). "NRG-1 may be next legal high to face ban by ministers | Politics". The Guardian.
6. (2 April 2010). "New 50c legal drug 'is more evil' than any head shop high". The Herald.
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8. (August 2010). "Analyses of second-generation 'legal highs' in the UK: initial findings". Drug Testing and Analysis.
9. (December 2011). "Energy-1 ('NRG-1'): don't believe what the newspapers say about it being legal". Emergency Medicine Journal.
10. (October 2010). "The naphyrone story: The alpha or beta-naphthyl isomer?". Drug Testing and Analysis.
11. (February 2011). "Naphyrone: analytical profile of the new "legal high" substitute for mephedrone". Journal of Forensic and Legal Medicine.
12. (2010-07-12). "NRG-1 'legal high' drug is banned". BBC News.
13. (2010-07-07). "Advisory Council on the Misuse of Drugs Naphyrone Report (2010)". Home Office.
14. "The Misuse of Drugs (Amendment No. 2) (England, Wales and Scotland) Regulations 2010 No. 1799". Opsi.gov.uk.
15. "Explanatory Memorandum To The Misuse of Drugs (Amendment No. 2) (England, Wales and Scotland) Regulations 2010 No. 1799". Opsi.gov.uk.
16. (October 2010). "The naphyrone story: The alpha or beta-naphthyl isomer?". Drug Testing and Analysis.
17. (2011). "An overview of new psychoactive substances and the outlets supplying them". National Advisory Committee on Drugs.
18. "Valtioneuvoston asetus kuluttajamarkkinoilta kielletyistä psykoaktiivisista aineista | 1130/2014 | Lainsäädäntö | Finlex".