Svante Vikingsson

2 papers in the library · 21 citations · publishing 2020-2026

Papers

In vitro characterization of new psychoactive substances at the μ-opioid, CB1, 5HT1A, and 5-HT2A receptors—On-target receptor potency and efficacy, and off-target effects

Forensic Science International October 23, 2020 Anna Åstrand, Davide Guerrieri, Svante Vikingsson et al. 21 citations

Sixty new psychoactive substances (NPS) and their metabolites, including opioids, cannabinoids, and serotonergic hallucinogens, were screened for their ability to activate μ-opioid, CB1, 5-HT1A, and 5-HT2A receptors. Most substances activated their intended target receptor. Among μ-opioid agonists, 2-fluorofentanyl (EC50 = 1.0 nM), carfentanil (EC50 = 2.7 nM), and acrylfentanyl (EC50 = 2.8 nM) were the most potent, with a >1500-fold potency range across compounds. Furanylfentanyl, 4-methoxybutyrylfentanyl, and valerylfentanyl acted as partial agonists. On the 5-HT2A receptor, bromo-dragonfly was the most potent (EC50 = 0.05 nM, 400 times more potent than LSD), followed by NBOMe compounds (EC50 0.11–1.3 nM). Off-target μ-opioid activation occurred for piperazines, phenethylamines, and tryptamines. The synthetic cannabinoid metabolite 3-carboxy indole PB-22 activated 5-HT2A. Bromo-dragonfly activated all four receptors. These findings highlight complex, often overlapping targets among NPS.

DOI: 10.1016/j.forsciint.2020.110553 Serotonin Pharmacology Chemistry Cannabinoid receptor agonists +6

Comprehensive in vitro profiling of traditional and emerging stimulants at monoamine transporters and the 5-HT2A receptor.

British journal of pharmacology July 14, 2026 Darta Stalberga, Robert Kronstrand, Bianca Schranz et al.

Synthetic cathinones, a large class of new psychoactive substances, primarily inhibit dopamine, norepinephrine, and serotonin transporters, with high dopamine transporter selectivity linked to abuse potential. In vitro testing of 58 substances showed that N-pyrrolidine cathinones combined with methylenedioxy groups—MDPiHP, MDPEP, and MDPV—had the highest potency at the dopamine transporter. Other N-pyrrolidine cathinones, such as 3F-α-PHP, 3F-α-PiHP, and 4F-α-PiHP, showed the greatest dopamine transporter selectivity relative to the serotonin transporter. Chloromethcathinone and methylmethcathinone compounds, like 3-CMC, displayed an amphetamine-like profile with comparable potency at dopamine and norepinephrine transporters. Some cathinones at high concentrations and phenethylamines at micromolar concentrations also activated the 5-HT2A receptor, while 2C-like arylcyclohexylamines targeted the receptor without transporter inhibition. The majority of compounds, especially N-pyrrolidine cathinones, suggest high abuse potential based on their dopamine transporter selectivity.

DOI: 10.1111/bph.70587 Full text 5‐ht2a receptor Monoamine transporters Neurotransmitter uptake inhibitors New psychoactive substances +1