Research published in British Journal of Pharmacology

Methylenedioxymethamphetamine (‘Ecstasy’)‐induced immunosuppression: a cause for concern?

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...

DOI: 10.1111/j.1476-5381.2010.00899.x

Mechanisms mediating the ability of caffeine to influence MDMA (‘Ecstasy’)‐induced hyperthermia in rats

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...

DOI: 10.1111/j.1476-5381.2010.00660.x MDMA Sch-23390 Pharmacology Receptor antagonist +4

The role of monoamines in the changes in body temperature induced by 3,4‐methylenedioxymethamphetamine (MDMA, ecstasy) and its derivatives

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...

DOI: 10.1111/j.1476-5381.2010.00722.x MDMA Ecstasy Hyperthermia Hypothermia +6

Potential anxiolytic‐ and antidepressant‐like effects of salvinorin A, the main active ingredient of Salvia divinorum, in rodents

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...

DOI: 10.1111/j.1476-5381.2009.00230.x Pharmacology Κ-opioid receptor Am251 Anxiolytic +2

Role of α1‐ and β3‐adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse

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...

DOI: 10.1111/j.1476-5381.2009.00186.x MDMA Antagonist Hyperthermia Prazosin +1

Inhibitory effect of salvinorin A, from Salvia divinorum, on ileitis-induced hypermotility: cross-talk between kappa-opioid and cannabinoid CB(1) receptors.

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...

DOI: 10.1038/bjp.2008.294 Full text Salvinorin a Natural compound Gastrointestinal health Gut health +13

Gaddum and LSD: the birth and growth of experimental and clinical neuropharmacology research on 5‐HT in the UK

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....

DOI: 10.1038/bjp.2008.207 Lysergic acid diethylamide Serotonin Neuropharmacology 5-HT Receptor +2

Comparative potencies of 3,4‐methylenedioxymethamphetamine (MDMA) analogues as inhibitors of [3H]noradrenaline and [3H]5‐HT transport in mammalian cell lines

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...

DOI: 10.1038/sj.bjp.0707473 MDMA Ecstasy Serotonin Pharmacology +4

MDMA‐induced neurotoxicity: long‐term effects on 5‐HT biosynthesis and the influence of ambient temperature

British Journal of Pharmacology June 12, 2006 Esther O’shea, Laura Orío, Isabel Escobedo et al. 57 citations

3,4‐Methylenedioxymethamphetamine (MDMA or ‘ecstasy’) decreases the 5‐HT concentration, [ 3 H]‐paroxetine binding and tryptophan hydroxylase activity in rat forebrain, which has been interpreted as indicating 5‐HT neurodegeneration. This has been questioned, particularly the 5‐HT loss, as MDMA can also inhibit tryptophan hydroxylase. We have now evaluated the validity of these parameters as a...

DOI: 10.1038/sj.bjp.0706783 MDMA Serotonin Neurotoxicity Term time +3

Effects of MDMA, MDA and MDEA on blood pressure, heart rate, locomotor activity and body temperature in the rat involveα‐adrenoceptors

British Journal of Pharmacology February 20, 2006 Sotiria Bexis, James R. Docherty 62 citations

The effects of injection of 3,4‐methylenedioxymethamphetamine (MDMA), 3,4‐methylenedioxyamphetamine (MDA) and N ‐ethyl‐3,4‐methylenedioxyamphetamine (MDEA) (all 20 mg kg −1 ) on blood pressure, heart rate, core body temperature and locomotor activity in conscious rats were investigated using radiotelemetry. MDMA and MDA produced a prolonged increase in both systolic and diastolic pressures,...

DOI: 10.1038/sj.bjp.0706688 MDMA Heart rate Blood pressure Pharmacology +1

Role of α2A‐adrenoceptors in the effects of MDMA on body temperature in the mouse

British Journal of Pharmacology July 18, 2005 Sotiria Bexis, James R. Docherty 43 citations

3,4‐Methylenedioxymetamphetamine (MDMA) produces complex effects on body temperature, including hypo‐ and hyperthermic components that vary with ambient temperature and strain of rat. We have previously reported that MDMA is an α 2 ‐adrenoceptor agonist, and α 2 ‐adrenoceptor agonists such as clonidine produce hypothermia. The purpose of this study was to investigate the effects of MDMA on core...

DOI: 10.1038/sj.bjp.0706320 MDMA Hypothermia Hyperthermia Clonidine +4

Studies on the effect of MDMA (‘ecstasy’) on the body temperature of rats housed at different ambient room temperatures

British Journal of Pharmacology July 4, 2005 Alfred Richard Green, Esther O’shea, Kathryn S. Saadat et al. 70 citations

3,4‐Methylenedioxymethamphetamine (MDMA, ‘ecstasy’) administration to rats produces hyperthermia if they are housed in normal or warm ambient room temperature ( T a ) conditions (20°C), but hypothermia when in cool conditions ( T a 17°C). We have now investigated some of the mechanisms involved. MDMA (5 mg kg −1 i.p.) produced a rapid decrease in rectal temperature in rats at T a 15°C. This...

DOI: 10.1038/sj.bjp.0706318 MDMA Ecstasy Hypothermia Hyperthermia +6

A comparative study on the acute and long‐term effects of MDMA and 3,4‐dihydroxymethamphetamine (HHMA) on brain monoamine levels after i.p. or striatal administration in mice

British Journal of Pharmacology 2005 Isabel Escobedo, Esther O’shea, Laura Orío et al. 68 citations

This study investigated whether the immediate and long‐term effects of 3,4‐methylenedioxymethamphetamine (MDMA) on monoamines in mouse brain are due to the parent compound and the possible contribution of a major reactive metabolite, 3,4‐dihydroxymethamphetamine (HHMA), to these changes. The acute effect of each compound on rectal temperature was also determined. MDMA given i.p. (30 mg kg −1 ,...

DOI: 10.1038/sj.bjp.0706071 MDMA Serotonin Dopamine Monoamine neurotransmitter +5

Attenuation of 3,4‐methylenedioxymethamphetamine (MDMA, Ecstasy)‐induced rhabdomyolysis with α1‐ plus β3‐adrenoreceptor antagonists

British Journal of Pharmacology June 1, 2004 Jon E. Sprague, Robert E. Brutcher, Edward Mills et al. 53 citations

Studies were designed to examine the effects of α 1 ( α 1 AR)‐ plus β 3 ‐adrenoreceptor ( β 3 AR) antagonists on 3,4‐methylenedioxymethamphetamine (MDMA, Ecstasy)‐induced hyperthermia and measures of rhabdomyolysis (creatine kinase (CK)) and renal function (blood urea nitrogen (BUN) and serum creatinine (sCr)) in male Sprague–Dawley rats. MDMA (40 mg kg −1 , s.c.) induced a rapid and robust...

DOI: 10.1038/sj.bjp.0705823 MDMA Ecstasy Rhabdomyolysis Prazosin +7

4-Bromo-2,5-dimethoxyphenethylamine (2C-B) and structurally related phenylethylamines are potent 5-HT2A receptor antagonists in Xenopus laevis oocytes.

British Journal of Pharmacology April 1, 2004 Claudio A Villalobos, Paulina Bull, Patricio Sáez et al. 50 citations

1. We recently described that several 2-(2,5-dimethoxy-4-substituted phenyl)ethylamines (PEAs), including 4-I=2C-I, 4-Br=2C-B, and 4-CH(3)=2C-D analogs, are partial agonists at 5-HT(2C) receptors, and show low or even negligible intrinsic efficacy at 5-HT(2A) receptors. These results raised the proposal that these drugs may act as 5-HT(2) antagonists. 2. To test this hypothesis, Xenopus laevis...

DOI: 10.1038/sj.bjp.0705722 Full text 5-ht2a receptor Psychoactive compounds Psychoactive effects Phenylethylamines +5

Importance of ERK activation in behavioral and biochemical effects induced by MDMA in mice

British Journal of Pharmacology October 29, 2003 Julie Salzmann, Cynthia Marie‐claire, Stéphanie Le Guen et al. 120 citations

Little is known about the cellular effects induced by 3,4‐methylenedioxymethamphetamine (MDMA, ecstasy), although changes in gene expression have been observed following treatments with other psychostimulants. Thus, the aim of this study was to investigate in mice, the relationships between the ras‐dependent protein kinase ERK and MDMA‐induced reinforcement using the conditioned place...

DOI: 10.1038/sj.bjp.0705506 MDMA Nucleus accumbens Mapk/erk pathway Caudate nucleus +7

Role of the endocannabinoid system in MDMA intracerebral self‐administration in rats

British Journal of Pharmacology August 1, 2002 Daniela Braida, Mariaelvina Sala 64 citations

I.c.v. self‐administration of MDMA (0.01–2 μg per infusion), alone and in combination with CP 55,940 (0.4 μg infusion −1 ), was studied on an operant responding procedure. On the basis of individual preference for one of two levers, developed during training, rats were allowed to self‐administer vehicle from the preferred lever and MDMA from the other. Pressings on the MDMA associated‐lever,...

DOI: 10.1038/sj.bjp.0704825 MDMA Self-administration Pharmacology Anesthesia

Differences in potency and efficacy of a series of phenylisopropylamine/phenylethylamine pairs at 5-HT(2A) and 5-HT(2C) receptors.

British Journal of Pharmacology June 1, 2002 Claudio Acuña-Castillo, Claudio A Villalobos, Pablo R Moya et al.

The pharmacological profile of a series of (+/-)-2,5-dimethoxy-4-(X)-phenylisopropylamines (X=I, Br, NO(2), CH(3), or H) and corresponding phenylethylamines, was determined in Xenopus laevis oocytes injected with cRNA coding for rat 5-HT(2A) or 5-HT(2C) receptors. The efficacy and relative potency of these drugs were determined and compared to classical 5-HT(2) receptor agonists and...

DOI: 10.1038/sj.bjp.0704747 Full text

Characterization of the discriminable stimulus produced by 2-BFI: effects of imidazoline I(2)-site ligands, MAOIs, beta-carbolines, agmatine and ibogaine.

British Journal of Pharmacology March 1, 2002 Nicholas Macinnes, Sheila L. Handley 30 citations

1. The molecular nature and functions of the I(2) subtype of imidazoline binding sites are unknown but evidence suggests an association with monoamine oxidase (MAO). Rats can distinguish the selective imidazoline I(2)-site ligand 2-BFI from vehicle in drug discrimination, indicating functional consequences of occupation of these sites. We have used drug discrimination to investigate the nature...

DOI: 10.1038/sj.bjp.0704579 Full text Ibogaine I2 sites Neurochemistry Drug effects

The effect of 3,4‐methylenedioxymethamphetamine (MDMA, ?ecstasy?) and its metabolites on neurohypophysial hormone release from the isolated rat hypothalamus

British Journal of Pharmacology February 1, 2002 Mary L. Forsling, John K. Fallon, Darshna Shah et al. 77 citations

Methylenedioxymethamphetamine (MDMA, “ecstasy”), widely used as a recreational drug, can produce hyponatraemia. The possibility that this could result from stimulation of vasopressin by MDMA or one of its metabolites has been investigated in vitro . Release of both oxytocin and vasopressin from isolated hypothalami obtained from male Wistar rats was determined under basal conditions and...

DOI: 10.1038/sj.bjp.0704502 Full text MDMA Ecstasy Vasopressin Oxytocin +5

The pharmacology of the acute hyperthermic response that follows administration of 3,4‐methylenedioxymethamphetamine (MDMA, ‘ecstasy’) to rats

British Journal of Pharmacology 2002 Annis O. Mechan, B. Moreno Esteban, Esther O’shea et al. 219 citations

The pharmacology of the acute hyperthermia that follows 3,4‐methylenedioxymethamphetamine (MDMA, ‘ecstasy’) administration to rats has been investigated. MDMA (12.5 mg kg −1 i.p.) produced acute hyperthermia (measured rectally). The tail skin temperature did not increase, suggesting that MDMA may impair heat dissipation. Pretreatment with the 5‐HT 1/2 antagonist methysergide (10 mg kg −1 ), the...

DOI: 10.1038/sj.bjp.0704442 MDMA Ecstasy Serotonin Serotonergic +8

A study of the mechanisms involved in the neurotoxic action of 3,4‐methylenedioxymethamphetamine (MDMA, ‘ecstasy’) on dopamine neurones in mouse brain

British Journal of Pharmacology December 1, 2001 María Isabel Colado, Jorge Camarero, Annis O. Mechan et al. 122 citations

Administration of 3,4‐methylenedioxymethamphetamine (MDMA, ‘ecstasy’) to mice produces acute hyperthermia and long‐term degeneration of striatal dopamine nerve terminals. Attenuation of the hyperthermia decreases the neurodegeneration. We have investigated the mechanisms involved in producing the neurotoxic loss of striatal dopamine. MDMA produced a dose‐dependent loss in striatal dopamine...

DOI: 10.1038/sj.bjp.0704435 MDMA Neuroprotection Dopamine Pharmacology +6

The mechanisms involved in the long‐lasting neuroprotective effect of fluoxetine against MDMA (‘ecstasy’)‐induced degeneration of 5‐HT nerve endings in rat brain

British Journal of Pharmacology September 1, 2001 Violeta Sánchez Sánchez, Jorge Camarero, B. Moreno Esteban et al. 103 citations

It has been reported that co‐administration of fluoxetine with 3,4‐methylenedioxymethamphetamine (MDMA, ‘ecstasy’) prevents MDMA‐induced degeneration of 5‐HT nerve endings in rat brain. The mechanisms involved have now been investigated. MDMA (15 mg kg −1 , i.p.) administration produced a neurotoxic loss of 5‐HT and 5‐hydroxyindoleacetic acid (5‐HIAA) in cortex, hippocampus and striatum and a...

DOI: 10.1038/sj.bjp.0704230 MDMA Serotonin Fluoxetine Paroxetine +8

Vascular actions of MDMA involve α1 and α2‐adrenoceptors in the anaesthetized rat

British Journal of Pharmacology June 1, 2001 John Mcdaid, James R. Docherty 46 citations

We have investigated the effects of methylenedioxymethamphetamine (MDMA, ‘ecstasy’), i.v., on diastolic blood pressure (DBP) in pithed and pentobarbitone anaesthetized rats. In pithed rats, the non‐selective 5‐HT receptor antagonist methiothepin (0.1 mg kg −1 ) and the α 2 ‐adrenoceptor antagonists methoxyidazoxan and yohimbine (1 mg kg −1 ) showed significant α 1 ‐adrenoceptor antagonist...

DOI: 10.1038/sj.bjp.0704094 Ritanserin Prazosin Yohimbine Endocrinology +4

Blockade of phencyclidine-induced effects by a nitric oxide donor.

British Journal of Pharmacology July 1, 2000 M Bujas-Bobanovic, D C Bird, H A Robertson et al.

1. Phencyclidine (PCP) is widely used as an animal model of schizophrenia. The aim of this study was to better understand the role of nitric oxide (NO) in the mechanism of action of PCP and to determine whether positive NO modulators may provide a new approach to the treatment of schizophrenia. 2. The effects of the NO donor, sodium nitroprusside (SNP), were studied in PCP-treated rats....

DOI: 10.1038/sj.bjp.0703406 Full text

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