14C-Psilocin tissue distribution in pregnant rats after intravenous administration

Abstract

Background: Many species of hallucinogenic mushrooms have been found in the genusPsilocybe. The main psychoactive chemicals of Psilocybe mushrooms are psilocin and its phosphoryloxy derivative, psilocybin. In addition to its psychedelic effects, psilocybin is an effective agent to lift the mood of depressed patients with terminal cancers. Objective:To study the dispositional kinetics of 14 C-psilocin in pregnant rats after intravenous injection, to calculate tissue dose surrogates i.e., tissue 14 C concentration and area under the concentration-time curve using the experimental data, to quantify trans-placental passage of psilocin and/or its metabolites, and to identify new psilocin metabolite(s) in rat urine.Methods: A group of 15 pregnant Wistar rats weighing between 0.30-0.36 kg was used in the study. Each rat was given a single dose of 7.5 mg/kg 14 C-psilocin i.v. Three rats were randomly selected and sacrificed at 0.5, 1.0, 2.0, 4.0, and 8.0 hr post-dosing. The maternal and fetal tissues were quickly removed and the radioactivity in these tissues determined by liquid scintillation counting. In a separate study, urine samples were collected from 6 male Wistar rats after administering 15 mg/kg of unlabeled psilocin i.p. The urine samples were collected and extracted by chloroform-methanol (9:1 v/v) and analyzed using a gas chromatograph/mass spectrometer. Results:14 C-Psilocin crossed the placental barrier of pregnant rats readily after i.v.administration; maternal tissue 14 C concentrations were found to be much higher than those in fetal tissues. The areas under the curve for maternal tissues also were much higher than the fetal tissues. In general, maternal tissues could be divided into the fast eliminating organ group, which

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“…However, the concentrations of active principles may va species, origin, size, age, growing, and drying conditions [26]. In an found that after oral administration, 50% of the 14C-labelled psilocin almost evenly distributed throughout the body, including the brain [ studies, after intravenous administration, the 14C-psilocin crossed t reaching fetal tissue concentrations lower than maternal tissue, but w nation half-life [28]. In adult men, following oral administra dephosphorylated to psilocin from the hydrochloric acid made by t Furthermore, psilocybin is dephosphorylated to psilocin in the int blood by the alkaline phosphatase and nonspecific esterases [29,30].…”

“…In animal studies, it was found that after oral administration, 50% of the 14C-labelled psilocin was absorbed and almost evenly distributed throughout the body, including the brain [ 27 ]. In pregnant rat studies, after intravenous administration, the 14C-psilocin crossed the placental barrier reaching fetal tissue concentrations lower than maternal tissue, but with a slower elimination half-life [ 28 ]. In adult men, following oral administration, psilocybin is dephosphorylated to psilocin from the hydrochloric acid made by the stomach [ 29 , 30 ].…”