Toxicology letters
April 5, 2007
C Sogawa, N Sogawa, J Tagawa et al.
47 citations
5-MeO-DIPT, a synthetic hallucinogenic tryptamine, acts as a competitive inhibitor of the serotonin transporter (SERT), blocking serotonin uptake with high affinity and at concentrations similar to cocaine. It does not stimulate reverse transport of serotonin through SERT, and it prevents the serotonin-releasing action of methamphetamine. At high concentrations, the compound is toxic to cells, but this toxicity is not influenced by SERT expression. These findings clarify the serotonergic mechanism of 5-MeO-DIPT.
Toxicology letters
April 21, 2008
Miroslava Rohanová, Tomáš Páleníček, Marie Balíková
33 citations
The psychedelic compound 2C-B, involved in human drug abuse and overdose cases, was studied in rats to determine its distribution and kinetics after subcutaneous injection. The drug had an estimated half-life of 1.1 hours and a volume of distribution of 16 L/kg. 2C-B entered the brain without significant delay, and its brain-to-serum ratio peaked at 13.9, remaining above 6.5 for six hours. The lungs showed a tendency to retain the drug and release it gradually over time, similar to the brain. The major metabolite 2H5M-BPEA was found in lung, brain, and liver tissues but distributed less efficiently into the brain than the parent compound. These findings help assess the drug's psychotropic and toxic effects.
Toxicology letters
March 27, 2013
M Coppola, R Mondola
20 citations
5-iodo-2-aminoindan (5-IAI), a psychoactive derivative of 2-aminoindane, was identified in recreational products in the United Kingdom in 2011 after being anticipated by the EMCDDA in 2010. It is a rigid analogue of p-iodoamphetamine that produces MDMA-like effects. This paper summarizes the clinical, pharmacological, and toxicological information about this potential new drug of abuse.
Toxicology letters
October 1, 2018
Carolina Noble, Niels Bjerre Holm, Marie Mardal et al.
17 citations
Bromo-dragonfly, a potent and long-acting hallucinogen linked to severe vasoconstriction and fatal intoxications, was not metabolized in human liver microsomes, cytosol, or recombinant enzyme systems, unlike its analogue 2C-B-fly, which underwent monohydroxylation and N-acetylation via CYP2D6 and MAO-A. Bromo-dragonfly competitively inhibited monoamine oxidase A (MAO-A) with a Ki of 0.352 μM, and its IC50 suggested clinically relevant MAO-A inhibition, though further data are needed to assess its impact on serotonin levels in the body. Protein binding and pharmacokinetic parameters were also investigated.
Toxicology letters
April 1, 2025
Ting-Ting Yang, Zi-Wen Guo, Fang Zhang et al.
2 citations
Repeated ketamine exposure in neonatal rats reduces levels of DISC1 and several signaling proteins (pGSK-3β, β-catenin, pERK, pCREB, PSD95), leading to neuroapoptosis, inhibited neurite growth, and cognitive deficits in adolescence. Lithium treatment upregulates DISC1 and activates the GSK-3β/β-catenin and ERK/CREB pathways, thereby ameliorating these harmful effects. The findings suggest lithium may protect against ketamine-induced long-term neurotoxicity during brain development.
Toxicology letters
March 15, 2018
Achim T Caspar, Markus R Meyer, Hans H Maurer
Six NBOMe-derived new psychoactive substances (25B-, 25C-, 25I-, 3,4-DMA-, 4-EA-, and 4-MMA-NBOMe) are metabolized by multiple cytochrome P450 enzymes, primarily CYP2D6 and CYP2C19. Michaelis-Menten kinetic constants were determined using the substrate depletion approach; Km values ranged from 0.010 μM (CYP2D6, 4-MMA-NBOMe) to 13 μM (CYP2B6, 4-EA-NBOMe). CYP2D6 contributed most to hepatic net clearance for five compounds (61–89%), while CYP2C19 dominated for 4-MMA-NBOMe (64%). Because multiple isoforms are involved, the risk of drug-drug interactions may be low, but inter-individual variation in metabolism is possible for substances highly dependent on polymorphic CYP2C19 or CYP2D6.
Toxicology letters
April 15, 2017
Lea Wagmann, Simon D Brandt, Pierce V Kavanagh et al.
Thirteen analogs of the psychoactive substance alpha-methyltryptamine (AMT) were tested for their ability to inhibit monoamine oxidase (MAO), an enzyme that breaks down neurotransmitters. All analogs inhibited MAO-A, with IC50 values ranging from 0.049 to 166 μM, and four also inhibited MAO-B (IC50 82–376 μM). 7-Me-AMT was the most potent MAO-A inhibitor, comparable to the known inhibitors harmine and harmaline, and acted competitively. Most analogs also inhibited MAO in human liver S9 fractions. These findings suggest that MAO inhibition by these compounds could contribute to dangerous serotonin- and adrenaline-related effects, especially when combined with other drugs that block monoamine reuptake.