Acta Pharmaceutica Sinica B
August 6, 2016
Xi-Ling Jiang, Hong-Wu Shen, Donald E. Mager et al.
4 citations
We have shown recently that concurrent harmaline, a monoamine oxidase-A inhibitor (MAOI), potentiates serotonin (5-HT) receptor agonist 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT)-induced hyperthermia. The objective of this study was to develop an integrated pharmacokinetic/pharmacodynamic (PK/PD) model to characterize and predict the thermoregulatory effects of such serotonergic drugs in...
Pharmacological reports : PR
June 1, 2016
Xi-Ling Jiang, Hong-Wu Shen, Ai-Ming Yu
13 citations
5-Methoxy-N,N-dimethyltryptamine (5-MeO-DMT) and harmaline are indolealkylamine (IAA) drugs often abused together. Our recent studies have revealed the significant effects of co-administered harmaline, a monoamine oxidase inhibitor (MAOI), on 5-MeO-DMT pharmacokinetics and thermoregulation. This study was to delineate the impact of harmaline and 5-MeO-DMT on home-cage activity in mouse models,...
Neuropharmacology
February 1, 2015
Xi-Ling Jiang, Hong-Wu Shen, Ai-Ming Yu
26 citations
5-Methoxy-N,N-dimethyltryptamine (5-MeO-DMT) and harmaline are serotonin (5-HT) analogs often abused together, which alters thermoregulation that may indicate the severity of serotonin toxicity. Our recent studies have revealed that co-administration of monoamine oxidase inhibitor harmaline leads to greater and prolonged exposure to 5-HT agonist 5-MeO-DMT that might be influenced by cytochrome...
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...
The FASEB Journal
April 1, 2012
Ai-Ming Yu
Indolealkylamine (IAA) drugs are a major class of serotonin analogs that have high impact as substances of abuse. Among them, 5‐methoxy‐ N,N ‐dimethyltryptamine (5‐MeO‐DMT) was placed into Schedule I controlled substance status in the United States as of January 19, 2011, which is often co‐abused with harmaline. IAA drugs acts mainly on the serotonin neurotransmission system. Overdose of one...
Pharmacology, biochemistry, and behavior
September 1, 2011
Jerrold C Winter, D J Amorosi, Kenner C Rice et al.
10 citations
In previous studies we have observed that, in comparison with wild type mice, Tg-CYP2D6 mice have increased serum levels of bufotenine [5-hydroxy-N,N-dimethyltryptamine] following the administration of 5-MeO-DMT. Furthermore, following the injection of 5-MeO-DMT, harmaline was observed to increase serum levels of bufotenine and 5-MeO-DMT in both wild-type and Tg-CYP2D6 mice. In the present...
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...
Current Drug Metabolism
October 1, 2010
Hong-Wu Shen, Xi-Ling Jiang, Jerrold C Winter et al.
171 citations
5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) belongs to a group of naturally-occurring psychoactive indolealkylamine drugs. It acts as a nonselective serotonin (5-HT) agonist and causes many physiological and behavioral changes. 5-MeO-DMT is O-demethylated by polymorphic cytochrome P450 2D6 (CYP2D6) to an active metabolite, bufotenine, while it is mainly inactivated through the deamination...
Biochemical Pharmacology
July 1, 2010
Hong-Wu Shen, Chao Wu, Xi-Ling Jiang et al.
40 citations
5-Methoxy-N,N-dimethyltryptamine (5-MeO-DMT) is a natural psychoactive indolealkylamine drug that has been used for recreational purpose. Our previous study revealed that polymorphic cytochrome P450 2D6 (CYP2D6) catalyzed 5-MeO-DMT O-demethylation to produce active metabolite bufotenine, while 5-MeO-DMT is mainly inactivated through deamination pathway mediated by monoamine oxidase (MAO). This...
Bioanalysis
March 27, 2009
Hong-Wu Shen, Xi-Ling Jiang, Ai-Ming Yu
26 citations
INTRODUCTION: 5-Methoxy-N,N-dimethyltryptamine (5-MeO-DMT) is a psychoactive indolealkylamine substance that has been used for recreational purpose and may lead to fatal toxicity. While 5-MeO-DMT is mainly inactivated via deamination, it is O-demethylated to an active metabolite, bufotenine. Quantitation of 5-MeO-DMT and bufotenine is essential to understand the exposure to and the effects of...
The AAPS Journal
May 3, 2008
Ai-Ming Yu
60 citations
Indolealkylamine (IAA) drugs are 5-hydroxytryptamine (5-HT or serotonin) analogs that mainly act on the serotonin system. Some IAAs are clinically utilized for antimigraine therapy, whereas other substances are notable as drugs of abuse. In the clinical evaluation of antimigraine triptan drugs, studies on their biotransformations and pharmacokinetics would facilitate the understanding and...