PLoS ONE
June 14, 2016
Bryan L Roth, Simon Gibbons, Warunya Arunotayanun et al.
153 citations
Novel ketamine and phencyclidine analogues sold as designer drugs bind with high affinity to the same NMDA receptor site as the parent compounds, based on radioligand binding assays conducted through a national screening program. Methoxetamine and 3-MeO-PCE, along with the 3- and 4-methoxy analogues of phencyclidine, all showed strong affinity for the PCP-site on the glutamate NMDA receptor. Methoxetamine and phencyclidine and its analogues also bound appreciably to the serotonin transporter, while the PCP analogues had high affinity for sigma receptors. NMDA receptor antagonism likely explains their dissociative and psychotomimetic effects in humans; additional receptor actions may contribute to side effects.
Bioorganic & medicinal chemistry letters
June 1, 2013
Warunya Arunotayanun, Jeffrey W Dalley, Xi-Ping Huang et al.
41 citations
Two widely marketed novel psychoactive drugs, alpha-methyl-tryptamine and 5-methoxy-N,N-diallyl-tryptamine, were analyzed for their chemical structure and binding to serotonin receptor subtypes. These tryptamine-derived compounds, sold without restriction, can cause psychosis and hallucinations that may lead to injury or death. The study elucidates their structures and receptor binding profiles, providing insight into their pharmacological actions.
Journal of analytical toxicology
May 20, 2022
Caroline S Copeland, Simon Hudson, Ric Treble et al.
9 citations
The dissociative hallucinogen 3-MeO-PCP, a phencyclidine derivative, can cause severe psychological agitation and life-threatening cardiorespiratory effects. The United Nations classified it as a Schedule II substance in 2021. This report describes the first UK fatality solely attributable to 3-MeO-PCP intoxication, adding to 15 previous fatal cases worldwide. The authors note that blood concentrations associated with toxicity remain uncertain but provide detailed sample information to aid future interpretation. They suggest that exercise may worsen toxicity, cautioning against use as a club drug where elevated heart rate, body temperature, and blood pressure are likely.