Pentylone (β-Keto-Methyl
It is a substituted cathinone (a type of substituted phenethylamine). It has been identified in some samples of powders sold as “NRG-1”, along with varying blends of other cathinone derivatives including flephedrone, MDPBP, MDPV and 4-MePPP.
It was also found in combination with 4-MePPP being sold as “NRG-3”. Reports indicate side effects include feelings of paranoia, agitation and inability to sleep, with effects lasting for several days at high doses.
Pentylone
Rationale
Synthetic cathinones continue to emerge in recreational drug markets worldwide. l-(l,3-Benzodioxol-5-yl)-2-
(methylamino)butan-1-one (butylone) and 1-(1,3-Benzodioxol-5-yl)-2-(methylamino)pentan-1-one (pentylone) are
derivatives of the cathinone compound, 1-(1,3-benzodioxol-5-yl)-2-(methylamino)propan-1-one (methylone), that are being detected in drug products and human casework.
Objectives
The purpose of the present study was to examine the neuropharmacology of butylone and pentylone using in vitro and in vivo methods.
Methods
In vitro uptake and release assays were carried out in rat brain synaptosomes and in cells expressing human dopamine transporters (DAT) and 5-HT transporters (SERT). In vivo microdialysis was performed in the nucleus accumbens of conscious rats to assess drug-induced changes in neurochemistry.
Results
Butylone and pentylone were efficacious uptake blockers at DAT and SERT, though pentylone was more DAT-
selective. Both drugs acted as transporter substrates that evoked release of [3H]5-HT at SERT, while neither evoked
release at DAT. Consistent with the release data, butylone and pentylone induced substrate-associated inward
currents at SERT but not DAT. Administration of butylone or pentylone to rats (1 and 3 mg/kg, i.v.) increased
extracellular monoamines and motor activity, but pentylone had weaker effects on 5-HT and stronger effects on motor stimulation.
Conclusions
Our data demonstrate that increasing the α-carbon chain length of methylone creates “hybrid” transporter
compounds which act as DAT blockers but SERT substrates. Nevertheless, butylone and pentylone elevate
extracellular dopamine and stimulate motor activity, suggesting both drugs possess significant risk for abuse.
