John O’Brien

2 papers in the library · 60 citations · publishing 2014-2016

Papers

Characterization of a novel and potentially lethal designer drug (±)‐cis‐para‐methyl‐4‐methylaminorex (4,4'‐DMAR, or ‘Serotoni’)

Drug Testing and Analysis May 19, 2014 Simon D. Brandt, Michael H. Baumann, John S. Partilla et al. 37 citations

A new designer drug, para-methyl-4-methylaminorex (4,4'-DMAR), was linked to 26 deaths in Europe in 2013. Laboratory analysis of samples from online vendors identified the (±)-cis isomer in at least 18 cases. The drug acts as a potent releaser at dopamine, norepinephrine, and serotonin transporters, with EC50 values of 8.6 nM, 26.9 nM, and 18.5 nM respectively. Its potency at dopamine and norepinephrine transporters rivaled that of d-amphetamine and aminorex, but it was far more potent at the serotonin transporter. This broad activity predicts serious side effects including psychosis, agitation, hyperthermia, and cardiovascular stimulation, especially at high doses or with other stimulants.

DOI: 10.1002/dta.1668 Full text Serotonin Designer drug Amphetamine Monoamine neurotransmitter +8

Synthesis, characterization and monoamine transporter activity of the new psychoactive substance mexedrone and its N‐methoxy positional isomer, N‐methoxymephedrone

Drug Testing and Analysis August 15, 2016 Gavin McLaughlin, Noreen Morris, Pierce V. Kavanagh et al. 23 citations

Mexedrone, a derivative of mephedrone that appeared in 2015, was synthesized and analytically characterized. It was a weak non-selective uptake blocker at dopamine, norepinephrine, and serotonin transporters with IC50 values in the low micromolar range, and lacked releasing activity at dopamine and norepinephrine transporters but showed weak releasing activity at serotonin transporters (EC50 = 2.5 μM). Its isomer, N-methoxymephedrone, acted as a weak uptake blocker and a fully efficacious substrate-type releasing agent across all three transporters with EC50 values in the low micromolar range. A synthesis by-product, α-chloromethylmephedrone, was inactive in all assays.

DOI: 10.1002/dta.2053 Full text Mephedrone Monoamine neurotransmitter Norepinephrine transporter Serotonin transporter +7