European Journal of Neuroscience
November 16, 2007
Susan Schenk, Lincoln S. Hely, Barbara Lake et al.
113 citations
Abstract 3,4‐Methylenedioxymethamphetamine (MDMA) self‐administration has been shown in animals with extensive drug histories, but only a small number of studies have examined high rates of responding maintained by MDMA in previously drug‐naïve animals. In the present study, influence of dose (0.25 or 1.0 mg/kg/infusion) on the acquisition of MDMA self‐administration was measured during daily...
Molecular Pharmacology
November 2007
Michael R Braden, David E Nichols
We assessed the relative importance of two serine residues located near the top of transmembrane helix 5 of the human 5-HT(2A) receptor, comparing the wild type with S5.43(239)A or S5.46(242)A mutations. Using the ergoline lysergic acid diethylamide (LSD), and a series of substituted tryptamine and phenethylamine 5-HT(2A) receptor agonists, we found that Ser5.43(239) is more critical for...
Journal of Neuroscience
October 24, 2007
Francis Rodriguez Bambico, Noam Katz, Guy Debonnel et al.
325 citations
Preclinical and clinical studies show that cannabis modulates mood and possesses antidepressant-like properties, mediated by the agonistic activity of cannabinoids on central CB1 receptors (CB1Rs). The action of CB1R agonists on the serotonin (5-HT) system, the major transmitter system involved in mood control and implicated in the mechanism of action of antidepressants, remains however poorly...
Proceedings of the National Academy of Sciences
October 9, 2007
Alexandra Jean, Grégory Conductier, Christine Manrique et al.
Anorexia nervosa is a growing concern in mental health, often inducing death. The potential neuronal deficits that may underlie abnormal inhibitions of food intake, however, remain largely unexplored. We hypothesized that anorexia may involve altered signaling events within the nucleus accumbens (NAc), a brain structure involved in reward. We show here that direct stimulation of serotonin...
Journal of Biological Chemistry
October 5, 2007
Miriam T Jacobs, Yuan-Wei Zhang, Scott D Campbell et al.
149 citations
Ibogaine, a hallucinogenic alkaloid with purported anti-addiction properties, inhibited serotonin transporter (SERT) noncompetitively by decreasing V(max) with little change in the K(m) for serotonin (5-HT). Ibogaine also inhibited binding to SERT of the cocaine analog 2beta-2-carbomethoxy-3-(4-[(125)I]iodophenyl)tropane. However, inhibition of binding was competitive, increasing the apparent...
Journal of Pharmacology and Experimental Therapeutics
October 2007
Ju Shi, Katerina J Damjanoska, Rakesh K Singh et al.
We previously demonstrated that 24-h treatment with (-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane HCl (DOI) causes phosphorylation of Galpha11 protein at serine 154 and that this phosphorylation causes desensitization of serotonin (5-HT) 2A receptor signaling in A1A1v cells (Shi et al., 2007). We now report that treatment of A1A1v cells with DOI for 24 h produces a greater reduction in the...
Pharmacology, Biochemistry, and Behavior
October 1, 2007
Jerrold C Winter, K C Rice, D J Amorosi et al.
73 citations
Although psilocybin has been trained in the rat as a discriminative stimulus, little is known of the pharmacological receptors essential for stimulus control. In the present investigation rats were trained with psilocybin and tests were then conducted employing a series of other hallucinogens and presumed antagonists. An intermediate degree of antagonism of psilocybin was observed following...
British Journal of Pharmacology
September 24, 2007
Therese Montgomery, Christophe Buon, S Eibauer et al.
33 citations
Background and purpose: Illegal ‘ecstasy’ tablets frequently contain 3,4‐methylenedioxymethamphetamine (MDMA)‐like compounds of unknown pharmacological activity. Since monoamine transporters are one of the primary targets of MDMA action in the brain, a number of MDMA analogues have been tested for their ability to inhibit [ 3 H]noradrenaline uptake into rat PC12 cells expressing the...
Pharmacology, Biochemistry, and Behavior
September 19, 2007
Chad J Reissig, Justin R Eckler, R A Rabin et al.
A previous investigation in our laboratory found that the stimulus effects of the 5-HT2A agonist, LSD, are potentiated by 5-HT1A receptor agonists including the prototypic agonist, 8-OH-DPAT. Also suggestive of behaviorally relevant interactions between 5-HT1A and 5-HT2A receptors are behavioral analyses of locomotor activity, head-twitch response, forepaw treading and production of the...
Psychopharmacology
September 13, 2007
Olivia Carter, Felix Hasler, John D. Pettigrew et al.
150 citations
RationaleBinocular rivalry occurs when different images are simultaneously presented to each eye. During continual viewing of this stimulus, the observer will experience repeated switches between visual awareness of the two images. Previous studies have suggested that a slow rate of perceptual switching may be associated with clinical and drug-induced psychosis.ObjectivesThe objective of the...
Australian & New Zealand Journal of Psychiatry
July 25, 2007
Edmund Silins, Jan Copeland, Paul Dillon
76 citations
Growth of the antidepressant market and widespread use of the illicit drug ecstasy (methylenedioxymethamphetamine; MDMA) creates a need to delineate the potential harms associated with the concomitant use of ecstasy and serotonergic pharmaceutical drugs. One such harm is serotonin syndrome. The study aimed to synthesize the risk of serotonin syndrome associated with the concomitant use of...
Neurotoxicology
July 2007
João Paulo Capela, Eduarda Fernandes, Fernando Remião et al.
3,4-Methylenedioxymethamphetamine (MDMA or "Ecstasy") is a psychoactive and hallucinogenic drug of abuse. MDMA has been shown to produce neurotoxicity both in animals and humans. MDMA and other amphetamines induce serotonergic and dopaminergic terminal neurotoxicity and also neurodegeneration in areas including the cortex, hippocampus, striatum and thalamus. Herein, we investigated the...
European Journal of Neuroscience
July 1, 2007
Sameera Dasari, Kert Viele, Amy Turner et al.
40 citations
Abstract The effects of para‐chlorophenylalanine (PCPA) and 3,4 methylenedioxy‐methamphetamine (MDMA, ‘ecstasy’) were investigated in relation to development, behavior and physiology in larval Drosophila . PCPA blocks the synthesis of serotonin (5‐HT) and MDMA is known to deplete 5‐HT in mammalian neurons; thus these studies were conducted primarily to target the serotonergic system. Treatment...
Journal of Pharmacology and Experimental Therapeutics
June 2007
Pablo R Moya, Kelly A Berg, Manuel A Gutiérrez-Hernandez et al.
2,5-Dimethoxy-4-substituted phenylisopropylamines and phenethylamines are 5-hydroxytryptamine (serotonin) (5-HT)(2A/2C) agonists. The former are partial to full agonists, whereas the latter are partial to weak agonists. However, most data come from studies analyzing phospholipase C (PLC)-mediated responses, although additional effectors [e.g., phospholipase A(2) (PLA(2))] are associated with...
European Journal of Pharmacology
May 21, 2007
Beatriz Goñi-allo, Elena Puerta, Isabel Hervias et al.
13 citations
Amiloride and several of its congeners known to block the Na(+)/Ca(2+) and/or Na(+)/H(+) antiporters potentiate methamphetamine-induced neurotoxicity without altering methamphetamine-induced hyperthermia. We now examine whether amiloride also exacerbates 3,4-methylenedioxymethamphetamine (MDMA)-induced long-term serotonin (5-HT) loss in rats. Amiloride (2.5 mg/kg, every 2 h x 3, i.p.) given at...
Journal of Psychopharmacology
May 1, 2007
Karsten Heekeren, Anna Neukirch, Jörg Daumann et al.
49 citations
Patients with schizophrenia exhibit diminished prepuLse inhibition (PPI) of the acoustic startle reflex and deficits in the attentional moduLation of PPI. Pharmacological challenges with hallucinogens are used as models for psychosis in both humans and animals. RemarkabLy, in contrast to the findings in schizophrenic patients and in animal hallucinogen modeLs of psychosis, previous studies with...
Toxicology Letters
April 5, 2007
Chiharu Sogawa, Norio Sogawa, J Tagawa et al.
47 citations
5-Methoxy-N,N-diisopropyltryptamine (5-MeO-DIPT) is a synthetic orally active hallucinogenic tryptamine derivative, known also as Foxy or Foxy methoxy. However, few studies have examined its effects in vitro. In the present study, we investigated the actions of 5-MeO-DIPT against monoamine neurotransmitter transporters, including the transporters for dopamine (DAT), norepinephrine (NET), and...
Synapse
April 5, 2007
Paul Cumming, Mette Møller, Kjeld Benda et al.
28 citations
Abstract The psychostimulant 3,4‐methylendioxymethamphetamine (MDMA, “ecstasy”) evokes degeneration of telencephalic serotonin innervations in rodents, nonhuman primates, and human recreational drug users. However, there has been no alternative to nonhuman primates for studies of the cognitive and neurochemical consequences of serotonin depletion in a large‐bodied animal. Therefore, we used...
European Journal of Pharmacology
March 22, 2007
Fumiko Nagai, Ryouichi Nonaka, Kanako Satoh Hisashi Kamimura
277 citations
We developed a reproducible, simple, and small-scale method for determining the re-uptake and release of monoamines (dopamine, serotonin (5-HT) and norepinephrine) using rat brain synaptosomes. These assays were then applied to study the effects of different kinds of non-medically used psychoactive drugs on monoamine re-uptake and release. The phenethylamine derivatives, 4-fluoroamphetamine,...
Journal of Psychoactive Drugs
March 1, 2007
Casey R. Guillot
26 citations
Due to potential serotonergic deficits, 3,4-methylenedioxymethamphetamine (MDMA or Ecstasy) may cause long-term mood disruptions in recreational Ecstasy users. The purpose of this review is to evaluate the evidence for a relationship between recreational Ecstasy use and higher levels of depressive symptoms. Eleven out of 22 studies initially have reported significantly higher depression scores...