British Journal of Pharmacology
July 1, 2012
Ar Green, MV King, SE Shortall et al.
3,4‐Methylenedioxymethamphetamine (MDMA) induces both acute adverse effects and long‐term neurotoxic loss of brain 5‐HT neurones in laboratory animals. However, when choosing doses, most preclinical studies have paid little attention to the pharmacokinetics of the drug in humans or animals. The recreational use of MDMA and current clinical investigations of the drug for therapeutic purposes...
British Journal of Pharmacology
June 1, 2012
Natacha Vanattou‐saïfoudine, Ruth Mcnamara, Andrew Harkin
60 citations
Concomitant consumption of caffeine with recreational psychostimulant drugs of abuse can provoke severe acute adverse reactions in addition to longer term consequences. The mechanisms by which caffeine increases the toxicity of psychostimulants include changes in body temperature regulation, cardiotoxicity and lowering of the seizure threshold. Caffeine also influences the stimulatory,...
British Journal of Pharmacology
April 2012
Leigh V Panlilio, Sergi Ferré, Sevil Yasar et al.
Cannabis and caffeine are two of the most widely used psychoactive substances. Δ(9) -Tetrahydrocannabinol (THC), the main psychoactive constituent of cannabis, induces deficits in short-term memory. Caffeine, a non-selective adenosine receptor antagonist, attenuates some memory deficits, but there have been few studies addressing the effects of caffeine and THC in combination. Here, we evaluate...
British Journal of Pharmacology
March 9, 2012
A. C. Parrott
50 citations
In this issue of the BJP , Green et al . suggest that animal data could not be used to predict the adverse effects of 3,4‐methylenedioxymethamphetamine (MDMA) in humans and that MDMA did not produce 5‐HT neurotoxicity in the human brain. This proposal was, however, not accompanied by a review of the empirical evidence in humans. The neuroimaging data on 5‐HT markers in abstinent recreational...
British Journal of Pharmacology
March 8, 2012
Cédric M. Hysek, Yasmin Schmid, Anna Rickli et al.
81 citations
BACKGROUND AND PURPOSE The use of ±3,4‐methylenedioxymethamphetamine (MDMA, ‘ecstasy’) is associated with cardiovascular complications and hyperthermia. EXPERIMENTAL APPROACH We assessed the effects of the α 1 ‐ and β‐adrenoceptor antagonist carvedilol on the cardiostimulant, thermogenic and subjective responses to MDMA in 16 healthy subjects. Carvedilol (50 mg) or placebo was administered 1 h...
British Journal of Pharmacology
September 2011
Jennifer L. Stewart, Lance R Mcmahon
The fatty acid amide hydrolase inhibitor URB 597 increases brain anandamide levels, suggesting that URB 597 could enhance the behavioural effects of anandamide. The goal of the current study was to examine and characterize the in vivo pharmacology of URB 597 alone and in combination with anandamide and Δ⁹-tetrahydrocannabinol (Δ⁹ -THC) in two drug discrimination assays in rhesus monkeys. The...
British Journal of Pharmacology
May 26, 2011
Ján Kehr, Fumio Ichinose, Shimako Yoshitake et al.
BACKGROUND AND PURPOSE: The designer drug 1-(4-methylphenyl)-2-methylaminopropan-1-one (4-methylmethcathinone, mephedrone) is reported to possess psychostimulant, entactogenic and hallucinogenic effects. The purpose of this study was to examine the effects of acute administration of mephedrone on extracellular levels of dopamine (DA) and 5-HT in the nucleus accumbens of awake rats and compare...
British Journal of Pharmacology
April 21, 2011
Daniel José Barbosa, João Paulo Capela, Jorge M.A. Oliveira et al.
60 citations
BACKGROUND AND PURPOSE: 3,4-Methylenedioxymethamphetamine (MDMA or 'Ecstasy') is a worldwide major drug of abuse known to elicit neurotoxic effects. The mechanisms underlying the neurotoxic effects of MDMA are not clear at present, but the metabolism of dopamine and 5-HT by monoamine oxidase (MAO), as well as the hepatic biotransformation of MDMA into pro-oxidant reactive metabolites is thought...
British Journal of Pharmacology
December 30, 2010
Susan Schenk, David Gittings, Joyce Colussi‐mas
61 citations
BACKGROUND AND PURPOSE Animal models of drug‐seeking suggest that exposure to cues associated with self‐administered drugs and drug primes might precipitate relapse via activation of central dopaminergic substrates. EXPERIMENTAL APPROACH The effects of priming injections of dopamine and 5‐HT agonists on drug‐seeking and effects of dopamine antagonists on methylenedioxymethamphetamine...
British Journal of Pharmacology
June 1, 2010
Jürg Gertsch, Roger G Pertwee, Vincenzo Di Marzo
It is intriguing that during human cultural evolution man has detected plant natural products that appear to target key protein receptors of important physiological systems rather selectively. Plants containing such secondary metabolites usually belong to unique chemotaxa, induce potent pharmacological effects and have typically been used for recreational and medicinal purposes or as poisons....
British Journal of Pharmacology
June 1, 2010
Daniel T Malone, Matthew N Hill, Tiziana Rubino
Cannabis is one of the most widely used illicit drugs among adolescents, and most users first experiment with it in adolescence. Adolescence is a critical phase for brain development, characterized by neuronal maturation and rearrangement processes, such as myelination, synaptic pruning and dendritic plasticity. The endocannabinoid system plays an important role in fundamental brain...
British Journal of Pharmacology
June 2010
Brady K Atwood, John W Huffman, Alex Straiker et al.
'Spice' is an herbal blend primarily marketed in Europe as a mild hallucinogen with prominent cannabis-like effects and as a legal alternative to cannabis. However, a recent report identified a number of synthetic additives in samples of 'Spice'. One of these, the indole derivative JWH018, is a ligand for the cannabinoid receptor 1 (CB(1)) cannabinoid receptor and inhibits cAMP production in...
British Journal of Pharmacology
May 27, 2010
Noreen T. Boyle, Thomas J. Connor
42 citations
Methylenedioxymethamphetamine (MDMA; 'Ecstasy') is a ring-substituted amphetamine and a popular drug of abuse. In addition to ability to induce euphoria, MDMA abuse is associated with a range of acute and long-term hazardous effects. This paper is focused on once such adverse effect: its ability to negatively impact on functioning of the immune system. Research demonstrates that MDMA has...
British Journal of Pharmacology
May 24, 2010
Natacha Vanattou‐saïfoudine, Ruth Mcnamara, Andrew Harkin
39 citations
Background and purpose: Caffeine exacerbates the hyperthermia associated with an acute exposure to 3,4 methylenedioxymethamphetamine (MDMA, ‘Ecstasy’) in rats. The present study investigated the mechanisms mediating this interaction. Experimental approach: Adult male Sprague‐Dawley rats were treated with caffeine (10 mg·kg −1 ; i.p.) and MDMA (15 mg·kg −1 ; i.p.) alone and in combination. Core...
British Journal of Pharmacology
May 1, 2010
Methylenedioxymethamphetamine inhibits mitochondrial complex I activity in mice: a possible mechanism underlying neurotoxicity.
British Journal of Pharmacology
March 3, 2010
James R. Docherty, Ar Green
88 citations
Hyperthermia is probably the most widely known acute adverse event that can follow ingestion of 3,4‐methylenedioxymethamphetamine (MDMA, ecstasy) by recreational users. The effect of MDMA on body temperature is complex because the drug has actions on all three major monoamine neurotransmitters [5‐hydroxytryptamine (5‐HT), dopamine and noradrenaline], both by amine release and by direct receptor...
British Journal of Pharmacology
December 10, 2009
Inés Peraile, Elisa Torres, Andrea Mayado et al.
Background and purpose: 3,4-Methylenedioxymethamphetamine (MDMA) and cocaine are two widely abused psychostimulant drugs targeting the dopamine transporter (DAT). DAT availability regulates dopamine neurotransmission and uptake of MDMA-derived neurotoxic metabolites. We aimed to determine the effect of cocaine pre-exposure on the acute and long-term effects of MDMA in mice. Experimental...
British Journal of Pharmacology
November 2009
P Quérée, S Peters, T Sharp
Recent experiments using non-selective 5-hydroxytryptamine (5-HT)(2C) receptor agonists including WAY 161503 suggested that midbrain 5-HT neurones are under the inhibitory control of 5-HT(2C) receptors, acting via neighbouring gamma-aminobutyric acid (GABA) neurones. The present study extended this pharmacological characterization by comparing the actions of WAY 161503 with the 5-HT(2C)...
British Journal of Pharmacology
November 2009
Nathan Gunasekaran, L E Long, B L Dawson et al.
Delta(9)-tetrahydrocannabinol (THC), the main psychoactive constituent of cannabis, accumulates in adipose tissue where it is stored for long periods of time. Here we investigated whether conditions that promote lipolysis can liberate THC from adipocytes to yield increased blood levels of THC. In vitro studies involved freshly isolated rat adipocytes that were incubated with THC before exposure...
British Journal of Pharmacology
May 5, 2009
Daniela Braida, Valeria Capurro, Alessia Zani et al.
145 citations
BACKGROUND AND PURPOSE: Drugs targeting brain kappa-opioid receptors produce profound alterations in mood. In the present study we investigated the possible anxiolytic- and antidepressant-like effects of the kappa-opioid receptor agonist salvinorin A, the main active ingredient of Salvia divinorum, in rats and mice. EXPERIMENTAL APPROACH: Experiments were performed on male Sprague-Dawley rats...
British Journal of Pharmacology
April 30, 2009
Sotiria Bexis, James R. Docherty
36 citations
Background and purpose: We have investigated the ability of the β 3 ‐adrenoceptor antagonist 1‐(2‐ethylphenoxy)‐3‐[[(1S)‐1,2,3,4,‐tetrahydro‐1‐naphthalenyl]amino]‐(2S)‐2‐propanol hydrochloride (SR59230A) to affect the hyperthermia produced by methylenedioxymethamphetamine (MDMA) in conscious mice and whether α 1 ‐adrenoceptor antagonist actions are involved. Experimental approach: Mice were...
British Journal of Pharmacology
November 1, 2008
Raffaele Capasso, Francesca Borrelli, M G Cascio et al.
82 citations
Salvinorin A, the active component of the hallucinogenic herb Salvia divinorum, inhibits intestinal motility through activation of kappa-opioid receptors (KORs). However, this compound may have target(s) other than the KORs in the inflamed gut. Because intestinal inflammation upregulates cannabinoid receptors and endogenous cannabinoids, in the present study we investigated the possible...
British Journal of Pharmacology
June 2, 2008
Andrew R. Green
30 citations
The vasoconstrictor substance named serotonin was identified as 5‐hydroxytryptamine (5‐HT) by Maurice Rapport in 1949. In 1951, Rapport gave Gaddum samples of 5‐HT substance allowing him to develop a bioassay to both detect and measure the amine. Gaddum and colleagues rapidly identified 5‐HT in brain and showed that lysergic acid diethylamide (LSD) antagonized its action in peripheral tissues....
British Journal of Pharmacology
May 2008
Iain S. Mcgregor, P D Callaghan, G E Hunt
Addictive drugs can profoundly affect social behaviour both acutely and in the long-term. Effects range from the artificial sociability imbued by various intoxicating agents to the depressed and socially withdrawn state frequently observed in chronic drug users. Understanding such effects is of great potential significance in addiction neurobiology. In this review we focus on the 'social...
British Journal of Pharmacology
March 2008
Judith A Pratt, C Winchester, A Egerton et al.
Current treatments of schizophrenia are compromised by their inability to treat all symptoms of the disease and their side-effects. Whilst existing antipsychotic drugs are effective against positive symptoms, they have negligible efficacy against the prefrontal cortex (PFC)-associated cognitive deficits and negative symptoms. New models that reproduce core pathophysiological features of...