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British Journal of Pharmacology

ISSN 0007-1188

108 papers in the library · 6,557 citations · publishing 1968-2026

Papers

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Pharmacokinetic, pharmacodynamic, and behavioural studies of deschloroketamine in Wistar rats.

British Journal of Pharmacology 2022 Kristýna Štefková-mazochová, Hynek Danda, Wim Dehaen et al. 13 citations

Deschloroketamine (DCK), a structural analogue of ketamine, has recently emerged on the illicit drug market as a recreational drug with a modestly long duration of action. Despite it being widely used by recreational users, no systematic research on its effects has been performed to date. Pharmacokinetics, acute effects, and addictive potential in a series of behavioural tests in Wistar rats...

Novel drug developmental strategies for treatment‐resistant depression

British Journal of Pharmacology November 25, 2021 Éva Borbély, Mária Simon, Eberhard Fuchs et al. 103 citations

Major depressive disorder is a leading cause of disability worldwide. Because conventional therapies are ineffective in many patients, novel strategies are needed to overcome treatment‐resistant depression (TRD). Limiting factors of successful drug development in the last decades were the lack of (1) knowledge of pathophysiology, (2) translational animal models and (3) objective diagnostic...

Methoxphenidine (MXP) induced abnormalities: Addictive and schizophrenia-related behaviours based on an imbalance of neurochemicals in the brain.

British Journal of Pharmacology October 1, 2021 Kwang-Hyun Hur, Seong-Eon Kim, Shi-Xun Ma et al.

Methoxphenidine is a dissociative-based novel psychoactive designer drug. Although fatal accidents from methoxphenidine abuse have been reported, recreational use of the drug continues. We aim to provide scientific supportfor legal regulation of recreational abuse of methoxphenidine by demonstrating its the pharmacological action. Addictive potential of methoxphenidine was examined using...

Lasting effects of repeated ∆9 -tetrahydrocannabinol vapour inhalation during adolescence in male and female rats.

British Journal of Pharmacology 2020 Jacques D. Nguyen, Kevin M Creehan, Tony M Kerr et al.

Adolescents are regularly exposed to ∆9 -tetrahydrocannabinol (THC) via smoking and, more recently, vaping cannabis extracts. Growing legalization of cannabis for medical and recreational purposes, combined with decreasing perceptions of harm, makes it increasingly important to determine the consequences of frequent adolescent exposure for motivated behaviour and lasting tolerance in response...

(R)-Ketamine exerts antidepressant actions partly via conversion to (2R,6R)-hydroxynorketamine, while causing adverse effects at sub-anaesthetic doses.

British Journal of Pharmacology July 1, 2019 Panos Zanos, Jaclyn N. Highland, Xin Liu et al.

(R)-Ketamine (arketamine) may have utility as a rapidly acting antidepressant. While (R)-ketamine has lower potency than (R,S)-ketamine to inhibit NMDA receptors in vitro, the extent to which (R)-ketamine shares the NMDA receptor-mediated adverse effects of (R,S)-ketamine in vivo has not been fully characterised. Furthermore, (R)-ketamine is metabolised to (2R,6R)-hydroxynorketamine (HNK),...

Neurocognition and subjective experience following acute doses of the synthetic cannabinoid JWH‐018: a phase 1, placebo‐controlled, pilot study

British Journal of Pharmacology November 22, 2017 Eef L. Theunissen, Nadia R. P. W. Hutten, Natasha L. Mason et al. 38 citations

BACKGROUND AND PURPOSE: Synthetic cannabinoids (often sold as Spice or K2) have become a very popular alternative to cannabis due to their easy access and portrayed safety. Controlled studies on the behavioural effects of synthetic cannabinoids are currently lacking, which hampers risk assessments of these compounds. EXPERIMENTAL APPROACH: This is a first attempt to assess the influence of a...

Methoxetamine affects brain processing involved in emotional response in rats.

British Journal of Pharmacology October 1, 2017 Mary T. Zanda, Paola Fadda, S Antinori et al.

Methoxetamine (MXE) is a novel psychoactive substance that is emerging on the Internet and induces dissociative effects and acute toxicity. Its pharmacological effects have not yet been adequately investigated. We examined a range of behavioural effects induced by acute administration of MXE (0.5-5 mg·kg-1 ; i.p.) in rats and whether it causes rapid neuroadaptive molecular changes. MXE (0.5-5...

Pharmacological profile of novel psychoactive benzofurans

British Journal of Pharmacology March 13, 2015 Anna Rickli, Simone Kopf, Marius C. Hoener et al. 115 citations

Background and Purpose Benzofurans are newly used psychoactive substances, but their pharmacology is unknown. The aim of the present study was to pharmacologically characterize benzofurans in vitro . Experimental Approach We assessed the effects of the benzofurans 5‐ APB , 5‐ APDB , 6‐ APB , 6‐ APDB , 4‐ APB , 7‐ APB , 5‐ EAPB and 5‐ MAPDB and benzodifuran 2 C ‐ B ‐ FLY on the human...

Pharmacology and anti-addiction effects of the novel κ opioid receptor agonist Mesyl Sal B, a potent and long-acting analogue of salvinorin A.

British Journal of Pharmacology 2015 Bridget Simonson, Aashish S Morani, Amy W M Ewald et al.

Acute activation of κ opioid (KOP) receptors results in anticocaine-like effects, but adverse effects, such as dysphoria, aversion, sedation and depression, limit their clinical development. Salvinorin A, isolated from the plant Salvia divinorum, and its semi-synthetic analogues have been shown to have potent KOP receptor agonist activity and may induce a unique response with similar...

Stereochemistry of mephedrone neuropharmacology: enantiomer‐specific behavioural and neurochemical effects in rats

British Journal of Pharmacology September 26, 2014 Ryan A. Gregg, Michael H. Baumann, John S. Partilla et al. 79 citations

BACKGROUND AND PURPOSE: Synthetic cathinones, commonly referred to as 'bath salts', are a group of amphetamine-like drugs gaining popularity worldwide. 4-Methylmethcathinone (mephedrone, MEPH) is the most commonly abused synthetic cathinone in the UK, and exerts its effects by acting as a substrate-type releaser at monoamine transporters. Similar to other cathinone-related compounds, MEPH has a...

A pilot study of plasma metabolomic patterns from patients treated with ketamine for bipolar depression: evidence for a response-related difference in mitochondrial networks.

British Journal of Pharmacology April 1, 2014 A Villaseñor, A Ramamoorthy, M Silva Dos Santos et al. 69 citations

(R,S)-ketamine produces rapid and significant antidepressant effects in approximately 65% of patients suffering from treatment-resistant bipolar depression (BD). The genetic, pharmacological and biochemical differences between ketamine responders and non-responders have not been identified. The purpose of this study was to employ a metabolomics approach, a global, non-targeted determination of...

The preclinical pharmacology of mephedrone; not justMDMAby another name

British Journal of Pharmacology March 24, 2014 Andrew R. Green, Madeleine V. King, S.e. Shortall et al. 70 citations

The substituted β‐keto amphetamine mephedrone (4‐methylmethcathinone) was banned in the UK in A pril 2010 but continues to be used recreationally in the UK and elsewhere. Users have compared its psychoactive effects to those of 3,4‐methylenedioxymethamphetamine ( MDMA , ‘ecstasy’). This review critically examines the preclinical data on mephedrone that have appeared over the last 2–3 years and,...

Sex‐dependent long‐term effects of adolescent exposure to THC and/or MDMA on neuroinflammation and serotoninergic and cannabinoid systems in rats

British Journal of Pharmacology November 15, 2013 Ana Belén López-rodríguez, Alvaro Llorente‐berzal, Luis Miguel García‐segura et al. 50 citations

Background and Purpose Many young people consume ecstasy as a recreational drug and often in combination with cannabis. In this study, we aimed to mimic human consumption patterns and investigated, in male and female animals, the long‐term effects of Δ 9 ‐tetrahydrocannabinol ( THC ) and 3,4‐methylenedioxymethamphetamine ( MDMA ) on diverse neuroinflammation and neurotoxic markers. Experimental...

Effects of 3,4‐methylenedioxymethamphetamine (MDMA) and its main metabolites on cardiovascular function in conscious rats

British Journal of Pharmacology October 12, 2013 Charles W. Schindler, Eric B. Thorndike, Bruce E. Blough et al. 35 citations

Background and Purpose The cardiovascular effects produced by 3,4‐methylenedioxymethamphetamine ( MDMA ; ‘ E cstasy’) contribute to its acute toxicity, but the potential role of its metabolites in these cardiovascular effects is not known. Here we examined the effects of MDMA metabolites on cardiovascular function in rats. Experimental Approach Radiotelemetry was employed to evaluate the...

Single doses of THC and cocaine decrease proficiency of impulse control in heavy cannabis users

British Journal of Pharmacology October 11, 2013 Janelle H. P. van Wel, Kim P. C. Kuypers, Eef L. Theunissen et al. 38 citations

BACKGROUND AND PURPOSE: Cannabis is the most popular drug used in the European Union, closely followed by cocaine. Whereas cannabis impairs neurocognitive function in occasional cannabis users, such impairments appear less prominent in heavy users, possibly as a result of tolerance. The present study was designed to assess whether the impairing effects of Δ(9) -tetrahydrocannabinol (THC) in...

Carvedilol inhibits the cardiostimulant and thermogenic effects of MDMA in humans: Lost in translation

British Journal of Pharmacology September 6, 2013 Cédric M. Hysek, Yasmin Schmid, Anna Rickli et al. 7 citations

We greatly appreciate the comments offered by Drs Rolle, Takematsu and Hoffman and the opportunity to put our work into a wider perspective. We share the view that our work does not reflect the clinical situation but rather provides a proof of mechanism study, which aims to help to translate preclinical findings (Sprague et al., 2005) into the clinic. As we noted in the discussion of our work...

Differential effects of cathinone compounds andMDMAon body temperature in the rat, and pharmacological characterization of mephedrone‐induced hypothermia

British Journal of Pharmacology October 8, 2012 S.e. Shortall, Andrew R. Green, Km Swift et al. 51 citations

Background and Purpose Recreational users report that mephedrone has similar psychoactive effects to 3,4‐methylenedioxymethamphetamine ( MDMA ). MDMA induces well‐characterized changes in body temperature due to complex monoaminergic effects on central thermoregulation, peripheral blood flow and thermogenesis, but there are little preclinical data on the acute effects of mephedrone or other...

Inhibition ofMDMA‐induced increase in cortisol does not prevent acute impairment of verbal memory

British Journal of Pharmacology September 4, 2012 Kim P. C. Kuypers, Rafael de la Torre, Magı́ Farré et al. 23 citations

BACKGROUND: Ecstasy use is commonly linked with memory deficits in abstinent ecstasy users. Similar impairments are being found during ecstasy intoxication after single doses of ± 3,4 metylenedioxymethamphetamine (MDMA). The concordance of memory impairments during intoxication and abstinence suggests a similar neuropharmacological mechanism underlying acute and chronic memory impairments. The...

Caffeine provokes adverse interactions with 3,4‐methylenedioxymethamphetamine (MDMA, ‘ecstasy’) and related psychostimulants: mechanisms and mediators

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,...

MDMA and 5‐HT neurotoxicity: the empirical evidence for its adverse effects in humans – no need for translation

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...

Carvedilol inhibits the cardiostimulant and thermogenic effects of MDMA in humans

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...

Mephedrone, compared with MDMA (ecstasy) and amphetamine, rapidly increases both dopamine and 5-HT levels in nucleus accumbens of awake rats

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...

Pro‐oxidant effects of Ecstasy and its metabolites in mouse brain synaptosomes

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...

Dopaminergic mechanisms of reinstatement of MDMA‐seeking behaviour in rats

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...

Adolescent cannabis use and psychosis: epidemiology and neurodevelopmental models

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...