International Journal of Molecular Sciences
December 4, 2020
Sara Malaca, Alfredo Fabrizio Lo Faro, Alice Tamborra et al.
48 citations
Tryptamines are 5-HT2A receptor agonists that alter perceptions of reality. Their prevalence in drug overdoses is low but increasing, yet they are not part of typical toxicology testing, so their contribution may be underestimated. From 2015 to 2020, 22 new analytical methods, primarily liquid chromatography tandem mass spectrometry, were developed to identify tryptamines and metabolites in biological samples. The most prevalent tryptamines are 5-MeO-DiPT, 5-MeO-DALT, and DMT. Morbidity from tryptamine intake is considerable, and clinicians and laboratorians need updated data on this public health threat.
International Journal of Molecular Sciences
November 23, 2022
Lourdes Poyatos, Alfredo Fabrizio Lo Faro, Diletta Berardinelli et al.
22 citations
After controlled oral doses of 50–200 mg methylone given to 12 male volunteers, plasma concentrations increased in proportion to dose. Maximum concentrations ranged from 153 ng/mL at the lowest dose to 604 ng/mL at the highest dose. The drug was absorbed rapidly, reaching peak levels in 1.5–2 hours, and had a half-life of about 6 hours. Its metabolite HMMC reached peak concentrations 10–14 times lower than methylone. Unlike MDMA, methylone showed linear pharmacokinetics across the dose range. A validated LC-MS/MS method was used to measure methylone, MDMA, and their metabolites in plasma.
Metabolites
July 29, 2022
Sara Malaca, Marilyn A. Huestis, Leonardo Lattanzio et al.
8 citations
Synthetic tryptamines like 4-AcO-DiPT are increasingly involved in intoxications and fatalities yet remain unregulated in many countries, with little known about how the body processes them. Using human liver cells and high-resolution mass spectrometry, researchers identified six metabolites formed after three hours of incubation. The main transformation was ester hydrolysis to 4-OH-DiPT, followed by glucuronidation, sulfation, N-oxidation, and N-dealkylation. The most abundant second-generation metabolites were 4-OH-iPT-sulfate and 4-OH-DiPT-glucuronide. The authors suggest that 4-OH-DiPT, 4-OH-iPT, and 4-OH-DiPT-N-oxide are the best biomarkers to detect 4-AcO-DiPT consumption.