S. R. Nahorski, K.J. Rogers, C. Edwards,
The acute administration of MDMA has been shown to promote glycogenolysis and increase the extracellular concentration of glucose in the striatum. In the present study ... of serotonergic and/or noradrenergic mechanisms in the MDMA-induced increase in extracellular glucose and glycogenolysis was ... of these responses to the hyperthermia produced by MDMA also was examined. The administration of MDMA (10 mg/kg, i.p.) resulted in a ... blood glucose was modestly increased by 32% after MDMA treatment. Treatment of rats with fluoxetine (10 mg/ ...
Tópico(s): Forensic Toxicology and Drug Analysis
1975 - Elsevier BV | Brain Research
Donald R. Gehlert, C.J. Schmidt, Le-yu Wu, Walter Lovenberg,
(±)3,4-Methylenedioxymethamphetamine (MDMA, Ecstasy) is a synthetic ring-substituted amphetamine analog that produces a unique blend of stimulant and psychedelic effects. Considerable research demonstrates that MDMA has the potential to damage brain serotonin (5- ... and a growing body of data indicates that MDMA is also a 5-HT neurotoxin in humans. ... begins with a review of the history of MDMA's origins and early use practices, its emergence ... therapy. The major focus of this chapter addresses MDMA's effects on the human nervous system. To ...
Tópico(s): Neurotransmitter Receptor Influence on Behavior
1985 - Elsevier BV | European Journal of Pharmacology
Efrain C. Azmitia, Randall B. Murphy, Patricia M. Whitaker‐Azmitia,
... of 5-HT (toxicity) by 3, 4-methylenedioxymethamphetamine (MDMA) with the S(+) enantiomer being more active than ... system of fetal raphe neurons, the enantiomers of MDMA were tested to determine if a similar difference ... of plating of 5 × 10−6 M S(+)-MDMA and 5 × 10−5 M R(−)-MDMA. In order to determine if the Ca2+-independent ... 3H]5-HT uptake capacity, with the direct MDMA-induced Ca2+-independent (fluoxetine-sensitive) release being the first step. Evidence from binding studies indicates that MDMA has a micromolar affinity for the 5-HT2 ...
Tópico(s): Forensic Toxicology and Drug Analysis
1990 - Elsevier BV | Brain Research
G.A. Ricaurte, Kevin T. Finnegan, Ian Irwin, J. William Langston,
... in Cerebrospinal Fluid of Humans Previously Exposed to MDMA: Preliminary Observationsa G. A. RICAURTE, Corresponding Author G. ... a preprint to the Drug Enforcement Agency for MDMA hearings. 3 Doblin, R. 1989. Risk Assessment, the FDA and MDMA Research. In Ecstasy: The MDMA Story. B. Eisner, Ed. Ronin Publishing, Inc., Berkeley , ... Seiden 1987. Biochemical and histological evidence that methylenedioxymethylamphetamine (MDMA) is toxic to neurons in the rat brain. ... Gibb 1986. The effects of 3,4-methylenedioxymethamphetamine (MDMA) and 3,4-methylenedioxyamphetamine on monoaminergic systems in ...
Tópico(s): Neurotransmitter Receptor Influence on Behavior
1990 - Wiley | Annals of the New York Academy of Sciences
3,4-Methylenedioxymethamphetamine (MDMA) and 3,4- Methylenedioxyethamphetamine (MDEA) are synthetic amphetamine analogues that have received considerable media attention as recreational drugs popular among college students and young professionals. MDMA, more commonly known as "Ecstasy," has been available ... started to gain prominence since the placement of MDMA on Schedule I of the Controlled Substance Act ... Drug Enforcement Administration (DEA) on July 1, 1985. MDMA has been investigated by a small number of ...
Tópico(s): GABA and Rice Research
1990 - Springer Nature | Topics in the neurosciences
Robert L. Fitzgerald, Robert V. Blanke, Alphonse Poklis,
... to characterize the pharmacokinetics of the enantiomers of MDMA were conducted in rats using the iliac arterial ... for each route [20 and 40 mg/kg (±)‐MDMA for subcutaneous, 10 and 20 mg/kg (±)‐MDMA for intravenous administrations]. The average half‐life (±SD) ... was 2.5 ± 0.8 h for (−)‐(R)‐MDMA and 2.2 ±0.8 h for (+)‐(S)‐MDMA. The more rapid clearnace of (+)‐(S)‐MDMA compared with (−)‐(R)‐MDMA is consistent with the area under the curve ( ... The mean (±SD) AUC S/R ratios of MDMA and MDA were 0.70 ± 0.05 and ... Following a 20 mg/kg dose of racemic MDMA iv the mean (±SD) of the percent dose ...
Tópico(s): Cannabis and Cannabinoid Research
1990 - Wiley | Chirality
Dennis J. McKenna, Stephen J. Peroutka,
... 22 Neurochemistry and Neurotoxicity of 3,4-Methylenedioxymethamphetamine (MDMA, "Ecstasy") Dennis J. McKenna, Dennis J. McKenna Department ... De Souza E. B. (1988a) Pharmacologic profile of MDMA (3,4-methylenedioxy-methamphetamine) at various brain recognition ... S. Y., and De Souza E. B. (1988b) MDMA-induced neurotoxicity: parameters of degeneration and recovery of ... Zaczek R., and De Souza E. B. (1989) MDMA effects in brain: pharmacologic profile and evidence of neurotoxicity from neurochemical and autoradiographic studies, in MDMA: "Ecstasy" and/or Human Neurotoxin ( S. J. Peroutka, ...
Tópico(s): Neuroscience and Neuropharmacology Research
1990 - Wiley | Journal of Neurochemistry
3,4-Methylenedioxymethamphetamine (MDMA) has previously been shown to destroy serotonin terminals in the rat brain. Despite profound and prolonged loss of serotonin innervation, long-term behavioral effects of MDMA have not previously been reported. In this study, ... monitored the short- and long-term effects of MDMA administration on the ultrasonic isolation call of the ... to 60 min after a single dose of MDMA (0.5-10.0 mg/kg), isolation calls ... highest dose. Repeated administration of 10 mg/kg MDMA (once or twice daily on postnatal days 1- ...
Tópico(s): Neuroscience and Music Perception
1990 - American Society for Pharmacology and Experimental Therapeutics | Journal of Pharmacology and Experimental Therapeutics
Clifton W. Callaway, Laura Wing, Mark A. Geyer,
Methylenedioxymethamphetamine (MDMA) is a phenylethylamine with novel mood-altering properties in humans. MDMA shares the dopamine-releasing properties of amphetamine but ... roles of dopamine and 5-HT release in MDMA-induced locomotor hyperactivity. S-(+)MDMA produced dose-dependent increases of rat locomotion. Investigatory ... such as holepokes and rearings were suppressed by (+)MDMA. Pretreatment with the selective 5-HT uptake inhibitors fluoxetine, sertraline and zimelidine inhibited (+)MDMA-induced locomotor hyperactivity but failed to antagonize the ...
Tópico(s): Zebrafish Biomedical Research Applications
1990 - American Society for Pharmacology and Experimental Therapeutics | Journal of Pharmacology and Experimental Therapeutics
Samuel S.‐H. Wang, George A. Ricaurte, Stephen J. Peroutka,
The binding of [3H]3,4-methylenedioxymethamphetamine ([3H]MDMA) to both rat brain membrane preparations and glass ... the present study. Saturation studies indicate that [3H]MDMA binding is saturable and monophasic in both the ... brain membranes. This apparent ‘specific’ binding of [3H]MDMA in both the presence and absence of brain ... with polyethylenimine. Drug competition studies demonstrated that [3H]MDMA binding displays a distinct ‘pharmacological’ profile in the ... brain tissue. These data indicate that apparent [3H]MDMA binding to rat brain homogenates results from artifactual ...
Tópico(s): Neurotransmitter Receptor Influence on Behavior
1987 - Elsevier BV | European Journal of Pharmacology
Thomas Steele, David E. Nichols, G.K.W. Yim,
3,4-Methylenedioxymethamphetamine (MDMA) is a recently popularized recreational drug, although some have advocated its psychotherapeutic potential. Since the pharmacology of MDMA is largely uncharacterized, the stereochemical profiles of MDMA and some of its homologs were derived on ... observed with amphetamine, only the S-(+) enantiomer of MDMA and 3,4-methylenedioxyamphetamine (MDA) inhibited [3H]dopamine ... Neither stereoisomer of the alpha-ethyl homolog of MDMA, N-methyl-1-(1,3-benzodioxol-5-yl)- ... uptake. The two stereoisomers of amphetamine and the MDMA-related compounds were equipotent in inhibiting [3H]norepinephrine ...
Tópico(s): Chemical synthesis and alkaloids
1987 - Elsevier BV | Biochemical Pharmacology
Deborah Commins, Georgetta Vosmer, Robert M. Virus, W. L. Woolverton, Charles R. Schuster, Lewis S. Seiden,
(+/-)-3,4-Methylenedioxymethylamphetamine (MDMA) was administered s.c. to rats (10, 20 or 40 mg/kg b. wt.) and guinea pigs (20 mg/ ... the hippocampus, hypothalamus, striatum and neocortex. In rats, MDMA produced dose-dependent reductions in 5-HT in ... some regions. The 20-mg/kg dose of MDMA depleted 5-HT in all regions of the ... species, repeated administration of 20 mg/kg of MDMA reduced the Vmax but not the Km of ... administration. A single 40-mg/kg injection of MDMA depleted 5-HT 2 and 8 weeks after ... the hypothalamus. Administration of 80 mg/kg of MDMA twice a day for 2 days to rats ...
Tópico(s): Neuroscience and Neuropharmacology Research
1987 - American Society for Pharmacology and Experimental Therapeutics | Journal of Pharmacology and Experimental Therapeutics
Thomas Steele, David E. Nichols, G.K.W. Yim,
(±)-3,4-Methylenedioxymethamphetamine (MDMA) (10, 20, and 40 mg/kg) was administered to male CF-1 mice which were sacrificed 3, 6 or ... and metabolites. In contrast to reported effects of MDMA in the rat, the highest dose of MDMA transiently elevated mouse brain 5-hydroxytryptamine (5-HT) ... acid and dihydroxyphenylacetic acid were significantly lowered by MDMA at the two early time points. The highest dose of MDMA produced a transient depletion of norepinephrine in mouse brain and heart tissue. Only the effects of MDMA on cardiac norepinephrine were prevented by pretreatment of ...
Tópico(s): Psychedelics and Drug Studies
1989 - Elsevier BV | Pharmacology Biochemistry and Behavior
Thomas R. Insel, Giuseppe Battaglia, Jan N. Johannessen, Sergio Marra, E B De Souza,
3,4-Methylenedioxymethamphetamine (MDMA, "Ecstasy"), an amphetamine analog, is a "designer drug" which is being increasingly abused. The potential neurotoxic hazard of MDMA in humans was assessed by examining the effects of repeated systemic administration of MDMA on selected neurochemical and behavioral measures in rhesus monkeys. In the first study, MDMA (2.5 or 10 mg/kg twice daily ... and 5-HIAA. At the high dose of MDMA, a selective decrease in serotonin uptake sites (reflecting ... To determine if these changes after high dose MDMA were pharmacologic or truly neurotoxic, in a subsequent ...
Tópico(s): Cannabis and Cannabinoid Research
1989 - American Society for Pharmacology and Experimental Therapeutics | Journal of Pharmacology and Experimental Therapeutics
Richard A. Glennon, Bryan R. Misenheimer,
... monomethyl-1-(3,4-methylenedioxyphenyl)-2-aminopropane HCl (MDMA) from saline in order to determine if two ... OH MDA) would produce similar stimulus effects. The MDMA-stimulus (MDMA, ED50 value = 0.76 mg/kg) generalized both ... amphetamine resulted in partial generalization (maximum of 49% MDMA-appropriate responding) in the MDMA-trained animals. Taken together with our previous studies showing that MDMA substitutes for the phenylisopropylamine stimulant (+)amphetamine, but that ... 2-aminopropane (DOM), the present results [i.e., MDMA-stimulus generalization to MDE, N-OH MDA, but ...
Tópico(s): Psychedelics and Drug Studies
1989 - Elsevier BV | Pharmacology Biochemistry and Behavior
Jeffrey Sprouse, Charles W. Bradberry, Robert H. Roth, George K. Aghajanian,
The effects of MDMA (3,4-methylenedioxymethamphetamine) on the activity of serotonin (5-HT)-containing dorsal raphe neurons were characterized using extracellular single- ... the in vitro midbrain slice preparation. Addition of (+)-MDMA, (−)-MDMA or p-chloroamphetamine (PCA) to the superfusate (final ... was reversible and reproducible. Based upon IC50 values, (+)-MDMA was 2- to 3-fold more potent than (−)-MDMA. Pretreatment with the selective 5-HT uptake inhibitor ... firing (20 μM), blocked the inhibitory effect of (+)-MDMA and PCA on dorsal raphe neurons. The selective ...
Tópico(s): Psychedelics and Drug Studies
1989 - Elsevier BV | European Journal of Pharmacology
Robert T. Matthews, Thomas H. Champney, Gerald D. Frye,
Acute treatment with (±)3,4-methylenedioxymethamphetamine (MDMA) at high doses (10 and 30 mg/kg, IP), but not lower doses increased locomotor activity in male rats. MDMA did not consistently produce any other stereotyped behaviors ... after acute treatment with 10 mg/kg of MDMA. DA turnover rate was inconsistently decreased in the ... hours after a 30 mg/kg injection of MDMA, DA turnover rate was decreased in all brain areas tested. MDMA and d-amphetamine partially reversed a haloperidol-induced ... haloperidol's effect. In chloral hydrate-anesthesized rats, MDMA injected IV partially inhibited spontaneous firing rate of ...
Tópico(s): Psychedelics and Drug Studies
1989 - Elsevier BV | Pharmacology Biochemistry and Behavior
... stimulation and perceptual alterations, the psychoactive qualities of MDMA are less distinctive. MDMA binds to serotonergic receptors and has been shown ... serotonin concentrations. Biochemical and behavioral evidence suggests that MDMA may also act on the dopamine system. The ... explored the effects of blocking serotonin receptors on MDMA and amphetamine induced locomotor hyperactivity in rats. Locomotor ... combination with amphetamine (0.5 mg/kg) or MDMA (10 mg/kg). Methysergide, which had no effect ... own, significantly potentiated the locomotor hyperactivity produced by MDMA but not amphetamine. Thus, the intrinsic serotonergic agonist ...
Tópico(s): Forensic Toxicology and Drug Analysis
1988 - Elsevier BV | Pharmacology Biochemistry and Behavior
... the discriminative stimulus properties of the “designer” drug MDMA. In Experiment 1, rats trained to discriminate 1.5 mg/kg (±)-MDMA from its vehicle at 20 min postadministration were ... various dopaminergically-active agonists did not result in MDMA-like responding. In Experiment 2, dopaminergic and serotonergic antagonists were employed to observe their effect upon MDMA discrimination at 20 min postinjection. The serotonin antagonist pirenperone significantly decreased MDMA discrimination, whereas the dopamine decreasing drugs CGS 10746B ...
Tópico(s): Cannabis and Cannabinoid Research
1988 - Elsevier BV | Pharmacology Biochemistry and Behavior
William Slikker, Syed F. Ali, Andrew C. Scallet, Chris Frith, Glenn D. Newport, J R Bailey,
MDMA is an amphetamine analog prescribed by some health professionals in the field of psychotherapy and used ... public. In recent reports, investigators have suggested that MDMA produces acute neurotoxicity when administered by subcutaneous injection. In order to determine if MDMA produces lasting neurochemical alterations after oral administration, groups ... with either 40 or 80 mg/kg of MDMA or saline vehicle once every 12 hr for ... norepinephrine (NE). In the CN, 40 mg/kg MDMA produced no change in DA, DOPAC, or HVA, ...
Tópico(s): Forensic Toxicology and Drug Analysis
1988 - Elsevier BV | Toxicology and Applied Pharmacology
J. Frank Nash, Hy Meltzer, G A Gudelsky,
The racemic mixture of 3,4-methylenedioxymethamphetamine (MDMA), which has been reported to produce selective destruction of serotonergic neurons in the central nervous system, was studied to determine its neuroendocrine and temperature effects and mechanism of action. MDMA elevated serum concentrations of corticosterone in doses ranging ... were elevated 30 min after the administration of MDMA (10 mg/kg i.p.) and remained elevated ... prolactin (PRL) concentrations were elevated by administration of MDMA in doses ranging from 1 to 20 mg/ ...
Tópico(s): Psychedelics and Drug Studies
1988 - American Society for Pharmacology and Experimental Therapeutics | Journal of Pharmacology and Experimental Therapeutics
Manuel Daza‐Losada, Marta Rodríguez‐Arias, M.A. Aguilar, José Miñarro,
... reported by 75.5% of high school student MDMA (± 3,4‐methylenedioxymetamphetamine hydrochloride) users. The aim of ... evaluate the effects of exposure during adolescence to MDMA, cocaine or to both drugs on the MDMA‐induced conditioned place preference (CPP) in adult mice. ... daily administrations of saline, 10 mg/kg of MDMA, 25 mg/kg of cocaine or 10 mg/kg of MDMA plus 25 mg/kg of cocaine over 3 ... to 30). Three weeks after pre‐treatment, the MDMA‐induced CPP procedure was initiated (PD52). Acquisition of ... was induced with a sub‐threshold dose of MDMA (1.25 mg/kg) only in animals treated ...
Tópico(s): Cannabis and Cannabinoid Research
2009 - Wiley | Addiction Biology
Jacobi I. Cunningham, Jamie Raudensky, John Tonkiss, Bryan K. Yamamoto,
3,4-Methylenedioxymethamphetamine (MDMA) is a drug of abuse worldwide and a selective serotonin (5-HT) neurotoxin. An important factor in the risk ... relapse is stress. Although multiple parallels exist between MDMA abuse and stress, including effects on 5-HTergic ... have investigated the consequences of combined exposure to MDMA and chronic stress. Therefore, rats were pretreated with MDMA and exposed 7 days later to 10 days of mild chronic unpredictable stress (CUS). MDMA pretreatment was hypothesized to enhance the effects of ...
Tópico(s): Neurotransmitter Receptor Influence on Behavior
2009 - American Psychological Association | Behavioral Neuroscience
Melanie Mueller, Jie Yuan, Anne Felim, Anne Neudörffer, Frank T. Peters, Hans H. Maurer, Una D. McCann, Martine Largeron, George A. Ricaurte,
... 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 ... we explored the relationship between pharmacokinetic parameters of MDMA, 3,4-methylenedioxyamphetamine (MDA), 3,4-dihydroxymethamphetamine (HHMA), ... acetylcystein- S -yl)-HHMA (5-NAC-HHMA), an MDMA metabolite recently implicated in 5-HT neurotoxicity. Lasting serotonergic deficits correlated strongly with pharmacokinetic parameters of MDMA ( C max and area under the concentration-time ...
Tópico(s): Neurotransmitter Receptor Influence on Behavior
2009 - American Society for Pharmacology and Experimental Therapeutics | Drug Metabolism and Disposition
Déborah Hirt, Julien Fonsart, Marie‐Claude Menet, Marcel Debray, Florence Noble, Xavier Declèves, Jean‐Michel Scherrmann,
... pharmacokinetics of the recreational drug 3,4-methylenedioxymethamphetamine (MDMA) and its mains metabolites have never been modeled ... model with which to analyze the pharmacokinetics of MDMA, 3,4-methylenedioxyamphetamine (MDA), 4-hydroxy-3-methoxymethamphetamine ( ... and 18 females) were given 1 mg/kg MDMA iv, and the concentrations of MDMA, MDA, and HMMA were measured by high-performance ... model was developed to describe the changes in MDMA, HMMA, MDA, and HMA concentrations over time and ... test. Estimated exposures of males and females to MDMA and its metabolites were compared using the Wilcoxon ...
Tópico(s): Cannabis and Cannabinoid Research
2009 - Oxford University Press | Toxicological Sciences
Melanie Mueller, Erin A Kolbrich, Frank T. Peters, Hans H. Maurer, Una D. McCann, Marilyn A. Huestis, George A. Ricaurte,
... metabolism of the recreational drug (±) 3,4-methylenedioxymethamphetamine (MDMA, "ecstasy") in squirrel monkeys and humans because the squirrel monkey has been extensively studied for MDMA neurotoxicity. A newly developed liquid chromatography-mass spectrometric procedure for simultaneous measurement of MDMA, 3,4-dihydroxymethamphetamine, 4-hydroxy-3-methoxymethamphetamine, and ... Humans and squirrel monkeys were found to metabolize MDMA in similar, but not identical, pathways and proportions. ... monkeys than in humans. Both species demonstrated nonlinear MDMA pharmacokinetics at comparable plasma MDMA concentrations (125-150 ...
Tópico(s): Cannabis and Cannabinoid Research
2009 - Lippincott Williams & Wilkins | Therapeutic Drug Monitoring
Nora Von Ameln, Andreas von Ameln-Mayerhofer,
Despite the great popularity of 3,4-methylenedioxymethamphetamine (MDMA, Ecstasy) as a drug of abuse, not much ... of its optical isomers (enantiomers) R- and S-MDMA compared with the racemic RS-MDMA. For this purpose, adolescent rats were repetitively treated ... stage 2: days 15, 17, 19) with RS-MDMA (5 or 10 mg/kg) or each of ... of a photobeam-equipped activity box system. RS-MDMA or S-MDMA administration led acutely to massive hyperlocomotion and subchronically, ... behavioural sensitization after a short habituation period. R-MDMA was free of hyperactivating effects and even decreased ...
Tópico(s): Neurotransmitter Receptor Influence on Behavior
2009 - Wiley | Addiction Biology
The prevalence of 3,4-methylenedioxymethamphetamine (MDMA) use has increased globally and the pattern of consumption has changed considerably. Previously, a subculture of MDMA users was fairly restricted to the dance club ... of this subculture and now many users consume MDMA frequently and in large amounts and some meet ... mixed results with respect to the ability of MDMA to support and maintain self-administration by laboratory animals. This paper reviews the literature on MDMA self-administration in laboratory primates and rodents. Most ...
Tópico(s): Neurotransmitter Receptor Influence on Behavior
2009 - Karger Publishers | Neuropsychobiology
Michael H. Baumann, Dorota Żółkowska, In‐Sook Kim, Karl B. Scheidweiler, Richard B. Rothman, Marilyn A. Huestis,
... data, there is speculation that (±)-3,4-methylenedioxymethamphetamine (MDMA) is neurotoxic to humans. Extrapolation of MDMA findings from animals to humans requires assessment of ... rats are lacking. In this study, we examine MDMA pharmacokinetics in rats given low (2 mg/kg) and high (10 mg/kg) doses of racemic MDMA via intraperitoneal, subcutaneous, and oral routes. Repeated blood ... from venous catheters, and plasma was assayed for MDMA and its metabolites, 4-hydroxy-3-methoxymethamphetamine (HMMA) ... chromatography-mass spectrometry. After 2 mg/kg, maximum MDMA concentrations ( C max ) were ∼200 ng/ml for ...
Tópico(s): Cannabis and Cannabinoid Research
2009 - American Society for Pharmacology and Experimental Therapeutics | Drug Metabolism and Disposition