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...
The FASEB Journal
April 1, 2012
Ilana Emert, Katarzyna M Targowska-Duda, Dominik Feuerbach et al.
The interaction of ibogaine and phencyclidine (PCP) with human (h) α3β4 nicotinic acetylcholine receptors (AChRs) in different conformational states was determined using radioligand binding assays, Ca 2+ influx detections, thermodynamic and kinetic measurements. The results show that ibogaine inhibits (±)‐epibatidine‐induced Ca 2+ influx in hα3β4 AChRs with ~9‐fold higher potency than PCP, [ 3...
The FASEB Journal
April 1, 2012
David Martin, David E. Nichols, Charles D. Nichols
The objective of this work is to characterize genetic and proteomic changes in a novel rat model of schizophrenia. Three‐month treatment with low doses of the hallucinogenic drug, LSD, induces a range of abnormal behaviors including social deficits, hyperactivity, and anhedonia. These behavioral changes persist in the absence of drug , and likely result from neuroadaptive changes in the medial...
The FASEB Journal
April 1, 2012
Luli R Akinfiresoye, D. M. Lovinger, Y. Tizabi
Studies have shown that therapeutics that act on the glutamatergic system could provide a novel mechanistic approach for the treatment of depression. We previously reported that ketamine, an NMDA antagonist, has a rapid and lasting antidepressant effect both acutely and chronically on depressive‐like behavior in Wistar‐Kyoto (WKY) rats ( Soc Neurosci Abst 2008) . Other studies had suggested...
The FASEB Journal
April 1, 2011
Kevin S. Murnane, Leonard L. Howell
3,4-methylenedioxymethamphetamine (MDMA) is a substituted amphetamine derivative that is widely abused as the street drug “ecstasy”. Despite its high abuse liability, the neuropharmacology of MDMA remains poorly understood. In the present study, functional magnetic resonance imaging (fMRI) was used in fully conscious rhesus monkeys to characterize the neuroactivational effects of MDMA and its...
The FASEB Journal
April 1, 2010
Cullen L. Schmid, Laura Bohn
Serotonin and the hallucinogenic metabolites of tryptamines, dimethylated tryptamines, activate the serotonin 2A receptor (5‐HT2AR), which is implicated in numerous mental health disorders. We have previously demonstrated that the 5‐HT2AR is differentially regulated by βarrestin2 (βarr2) depending upon the agonist; here we utilized βarr2 knockout mice to compare signaling profiles in vivo, by...
The FASEB Journal
April 1, 2010
Kevin T. Ball
MDMA is a widely used amphetamine derivative that increases dopamine and serotonin transmission via its interaction with monoamine transporters. Compared to other psychostimulants, little is known about the long‐term neurobehavioral effects of MDMA. We conducted a series of studies aimed at elucidating the effects of MDMA administration on behavior, limbic cortico‐striatal neuronal structure,...
The FASEB Journal
April 1, 2009
Sandy Ghozland, Srihari R. Tella, Michelle D. Walker et al.
Pursuant to the Controlled Substances Act (CSA), DEA collects and reviews scientific, medical and other data for substances with abuse potential for possible placement under the CSA. The administrative process for scheduling is ongoing for indiplon, carisoprodol, dextromethorphan, salvinorin A and several petitions requesting a change in the control status of nabilone, methylphenidate product,...
The FASEB Journal
April 1, 2008
Krzysztof Jozwiak, Ruin Moaddel, Irving W. Wainer et al.
2 citations
PURPOSE: Characterization of the binding sites for ibogaine analogs on the nicotinic acetylcholine receptor (AChR) in the resting and desensitized states. METHODS: [ 3 H]18‐methoxycoronaridine ([ 3 H]18‐MC) Scatchard‐plots using Torpedo AChR membranes, [ 3 H]TCP (a well characterized noncompetitive antagonist) competition binding experiments and Schild‐type analysis, analog‐induced binding...
The FASEB Journal
March 1, 2008
Nicholas V. Cozzi, Anupama Gopalakrishnan, Lyndsey L. Anderson et al.
The plant hallucinogen N,N ‐dimethyltryptamine (DMT) has been used for religious and other purposes for many centuries. Over the past few decades, DMT has been reported in human brain, and pharmacological studies have shown that DMT binds to monoamine receptors. Recently, several N,N ‐dialkyltryptamines were reported to modify monoamine uptake and release in rat brain synaptosomes, indicating...
The FASEB Journal
March 1, 2008
Kevin Sean Murnane, Leonard L. Howell, William E Fantegrossi
3,4‐Methylenedioxymethamphetamine (MDMA) is an amphetamine derivative with increasingly widespread abuse. MDMA has been difficult to classify as a stimulant or hallucinogen because it shares effects with both drug classes. Furthermore, racemic MDMA is composed of two isomers that vary in terms of behavioral effects rather than simple potency differences. Specifically, the R(−) isomer of MDMA...
The FASEB Journal
March 1, 2006
M. Braden, James J. Chambers, David E. Nichols
The human serotonin 2A receptor (h5‐HT 2A R) plays an essential role in cognition, and is the principal target for serotonergic hallucinogens as well as atypical antipsychotics. Utilizing our in silico ‐activated h5‐HT 2A R homology model, an interaction was predicted between Asn343(6.55) in TM6 and the carbonyl of LSD. Virtual docking simulations of a new class of 5‐HT2 agonists, substituted N...
The FASEB Journal
December 1, 2002
Bruce Ladenheim, Michael Mccoy, Jean Lud Cadet et al.
34 citations
ABSTRACT 3,4‐Methylenedioxymethamphetamine (MDMA, ecstasy) is a popular drug of abuse. MDMA is pharmacologically classified as an entactogen because of its affinities to classical hallucinogens and stimulants. Oral ingestion of a single dose of the drug is associated with euphoria, elevated self‐confidence, and heightened sensory awareness in humans. Evidence for neurotoxicity in the human...
The FASEB Journal
February 1, 1997
Rabi Simantov, M Tauber
89 citations
The widely abused amphetamine analog 3,4‐methylenecdioxymethamphetamine (MDMA, also called “ecstasy”) induces hallucination and psychostimulation, as well as long‐term neuropsychiatric behaviors such as panic and psychosis. In rodents and monkeys, MDMA is cytotoxic to serotonergic neurons, but this is less clear with humans. Herein, MDMA was cytotoxic to human serotonergic JAR cells; it altered...