Drug metabolism and disposition: the biological fate of chemicals
July 1, 2025
Severin Mairinger, Mihye Kwon, Martin Bauer et al.
An important safety consideration for topically administered drugs is the extent of systemic exposure they achieve. The aim of this study was to evaluate whether a topically administered microdose of the model drug diclofenac can predict the systemic availability, plasma, and tissue pharmacokinetics of a topical therapeutic dose. Eight healthy participants (6 men and 2 women) participated in a...
Drug metabolism and disposition: the biological fate of chemicals
April 28, 2025
Jan Thomann, Deborah Rudin, Selina Kraus et al.
4 citations
4-Bromo-2,5-dimethoxyphenethylamine (2C-B) is widely used recreationally and has recently gained interest as a treatment for mental health disorders. In this study, a liquid chromatography-tandem mass spectrometry method to quantify 2C-B and its metabolites 4-bromo-2,5-dimethoxyphenylacetic acid (BDMPAA) and 4-bromo-2-hydroxy-5-methoxyphenylacetic acid (B-2-HMPAA) in human plasma was developed...
Drug metabolism and disposition: the biological fate of chemicals
May 1, 2013
Xi-Ling Jiang, Hong-Wu Shen, Donald E. Mager et al.
29 citations
5-Methoxy-N,N-dimethyltryptamine (5-MeO-DMT or street name "5-MEO") is a newer designer drug belonging to a group of naturally occurring indolealkylamines. Our recent study has demonstrated that coadministration of monoamine oxidase A (MAO-A) inhibitor harmaline (5 mg/kg) increases systemic exposure to 5-MeO-DMT (2 mg/kg) and active metabolite bufotenine. This study is aimed at delineating...
Drug metabolism and disposition: the biological fate of chemicals
July 1, 2011
Hong-Wu Shen, Xi-Ling Jiang, Ai-Ming Yu
29 citations
5-Methoxy-N,N,-dimethyltryptamine (5-MeO-DMT), an abused serotonergic indolealkylamine drug, was placed into Schedule I controlled substance status in the United States as of January 19, 2011. In previous studies, we have shown the impact of monoamine oxidase A and cytochrome P450 2D6 enzymes on 5-MeO-DMT metabolism and pharmacokinetics. The aim of this study was to investigate 5-MeO-DMT...
Drug metabolism and disposition: the biological fate of chemicals
July 2010
Irene Antolino-Lobo, Jan Meulenbelt, Sandra M Nijmeijer et al.
Metabolism plays an important role in the toxic effects caused by 3,4-methylenedioxymethamphetamine (MDMA). Most research has focused on the involvement of CYP2D6 enzyme in MDMA bioactivation, and less is known about the contribution of other cytochrome P450 (P450) and phase II metabolism. In this study, we researched the differential roles of phase I P450 enzymes CYP1A2, CYP3A4, and CYP2D6 and...
Drug metabolism and disposition: the biological fate of chemicals
March 2010
Nenad Manevski, Mika Kurkela, Camilla Höglund et al.
We have examined the glucuronidation of psilocin, a hallucinogenic indole alkaloid, by the 19 recombinant human UDP-glucuronosyltransferases (UGTs) of subfamilies 1A, 2A, and 2B. The glucuronidation of 4-hydroxyindole, a related indole that lacks the N,N-dimethylaminoethyl side chain, was studied as well. UGT1A10 exhibited the highest psilocin glucuronidation activity, whereas the activities of...
Drug metabolism and disposition: the biological fate of chemicals
November 2009
Michael H. Baumann, Dorota Zolkowska, Insook Kim et al.
Based on animal data, there is speculation that (+ or -)-3,4-methylenedioxymethamphetamine (MDMA) is neurotoxic to humans. Extrapolation of MDMA findings from animals to humans requires assessment of pharmacokinetics in various species, and low-dose administration data from rats are lacking. In this study, we examine MDMA pharmacokinetics in rats given low (2 mg/kg) and high (10 mg/kg) doses of...
Drug metabolism and disposition: the biological fate of chemicals
October 2009
Melanie Mueller, Jie Yuan, Anne Felim et al.
The mechanism by which the recreational drug (+/-)-3,4-methylenedioxymethamphetamine (MDMA) destroys brain serotonin (5-HT) axon terminals is not understood. Recent studies have implicated MDMA metabolites, but their precise role remains unclear. To further evaluate the relative importance of metabolites versus the parent compound in neurotoxicity, we explored the relationship between...
Drug metabolism and disposition: the biological fate of chemicals
October 2007
Matthew L Banks, Jon E. Sprague, David F Kisor et al.
Changes in ambient temperature are known to alter both the hyperthermic and the serotonergic consequences of 3,4-methylenedioxymethamphetamine (MDMA). Metabolism of MDMA has been suggested to be a requisite for these neurotoxic effects, whereas the hyperthermic response is an important contributing variable. The aim of the present study was to investigate the interaction between ambient...
Drug metabolism and disposition: the biological fate of chemicals
June 1, 2002
Wenjiang Zhang, Yamini Ramamoorthy, Rachel F. Tyndale et al.
17 citations
18-Methoxycoronaridine, a newly developed ibogaine analog, has been reported to decrease the self-administration of morphine, cocaine, ethanol, and nicotine. It has also been reported to attenuate naltrexone-precipitated signs of morphine withdrawal. In this study, three metabolites of 18-methoxycoronaridine (18-MC) were separated and identified by high-performance liquid...