Journal of Psychopharmacology
September 3, 2026
Katelijne V. van der Heijden, Gabriël E. Jacobs, Ellen James et al.
Serotonergic psychedelics, such as N,N-dimethyltryptamine (DMT), have shown therapeutic potential in various psychiatric disorders. However, DMT demonstrates pharmacokinetic (PK) variability and a short half-life. This exploratory study investigated the PK, pharmacodynamic (PD), and safety profile of CYB004, a deuterated DMT analogue, following intravenous administration in healthy volunteers....
Journal of Psychopharmacology
August 31, 2026
Katelijne V. van der Heijden, Soma Makai‐bölöni, Amir Inamdar et al.
BACKGROUND: -dimethyltryptamine (DMT) might have therapeutic effects in various psychiatric disorders. AIMS: Prior to exploring this clinical potential, it is essential to determine an optimal administration regimen for DMT, explore the relationship between its pharmacokinetics (PK) and pharmacodynamics and identify potential sources of pharmacokinetic variability. METHODS: Therefore, DMT was...
Journal of Psychopharmacology
June 25, 2026
Joost C Van Mechelen, Tobias A Wieles, Laura Borghans et al.
Oral S-ketamine (S-KETPO) is being explored as an alternative to intravenous maintenance treatment (S-KETIV) in treatment-resistant depression (TRD). However, the first-pass effect with S-KETPO significantly alters S-ketamine's bioavailability and the systemic exposure of its active metabolites, raising potential safety and efficacy concerns. This study characterized the pharmacodynamic and...
Clinical and Translational Science
May 1, 2025
Katelijne V. van der Heijden, Rob G J A Zuiker, Marije E. Otto et al.
7 citations
The serotonergic psychedelic N,N-dimethyltryptamine (DMT) presumably stimulates neuroplasticity in vitro and in vivo, by which it may exert neuroprotective effects during acute ischemic stroke. Since neuroplasticity has been implicated in the mechanism of action of rehabilitative therapy in stroke recovery, a pharmacological augmentation strategy facilitating neuroplasticity could be...
Frontiers in Neuroscience
2025
Kasper Recourt, Joop van Gerven, Nadieh Drenth et al.
1 citation
Ketamine demonstrates robust and rapidly occurring antidepressant effects in patients with difficult-to-treat major depressive disorder. Ketamine's antidepressant effects and its impact on functional networks in non-resistant forms of major depressive disorder are expected to provide valuable insight into ketamine's mechanism of action related to depression. This study employs an existing...
British Journal of Clinical Pharmacology
September 19, 2023
Francis M. Dijkstra, Rob G J A Zuiker, Jules A A C Heuberger et al.
1 citation
AIMS: To characterise the safety, tolerability, pharmacokinetics (PK) and pharmacodynamics (PD) of single ascending doses of oxathridine, a first-in-class histamine-3 receptor partialagonist, in healthy male volunteers. METHODS: A randomised, double-blind, placebo-controlled study including the NeuroCart, consisting of a battery of drug sensitive neurophysiological tests, was performed....
Psychopharmacology
February 1, 2018
Randall L. Morrison, Maggie Fedgchin, Jaskaran Singh et al.
72 citations
BACKGROUND: The effect of intranasal esketamine on cognitive functioning in healthy participants is assessed in this study. METHODS: computerized test battery assessed at 1 h predose and 40 min, 2, 4, and 6 h postdose. Secondary measures included the Mental Effort Scale, Karolinska Sleepiness Scale (KSS), and safety. RESULTS: Esketamine was associated with significant cognitive performance...
Brain Connectivity
December 2015
Daniel Kleinloog, Serge A.r.b. Rombouts, Remco Zoethout et al.
This analysis examines the neuronal foundation of drug-induced psychomimetic symptoms by relating the severity of these symptoms to changes in functional connectivity for a range of different psychoactive compounds with varying degrees of psychomimetic effects. The repeated measures design included 323 resting-state functional magnetic resonance imaging time series and measures of subjective...
Psychiatry Research
December 30, 2014
Daniel Kleinloog, Jasper Stevens, Jules A A C Heuberger et al.
The effects of drugs are not only determined by their pharmacological action, but also by user characteristics. This analysis explored the influence of personality on the differences in subjective effects in response to a standardized pharmacological challenge with the cannabinoid CB1/CB2 partial agonist Δ9-tetrahydrocannabinol (THC). To express the sensitivity to THC,...
International Journal of Methods in Psychiatric Research
June 2014
Daniel Kleinloog, Frits Roozen, Willem De Winter et al.
The subjective effects of cannabis and its main psychoactive component Δ(9) -tetrahydrocannabinol (THC) have played an important part in determining the therapeutic potential of cannabinoid agonists and antagonists. The effects mainly consist of feeling high, changes in perception, feelings of relaxation and occasionally dysphoric reactions. These effects are captured by two of the most...
British Journal of Clinical Pharmacology
July 2013
Linda E. Klumpers, Christine Roy, Geraldine Ferron et al.
Cannabinoid receptor type 1 (CB1 ) antagonists have been developed for the treatment of obesity and associated risk factors. Surinabant is a high affinity CB1 antagonist in vitro. The aim of this study was to assess the magnitude of inhibition by surinabant of CNS effects and heart rate induced by Δ(9) -tetrahydrocannabinol (THC) in humans. This was a double-blind, placebo-controlled,...
Neuroimage
November 15, 2012
Linda E. Klumpers, David M. Cole, Najmeh Khalili-Mahani et al.
Resting state-functional magnetic resonance imaging (RS-FMRI) is a neuroimaging technique that allows repeated assessments of functional connectivity in resting state. While task-related FMRI is limited to indirectly measured drug effects in areas affected by the task, resting state can show direct CNS effects across all brain networks. Hence, RS-FMRI could be an objective measure for compounds...
Anesthesiology
August 13, 2012
Marieke Niesters, Najmeh Khalili-Mahani, Christian H. Martini et al.
141 citations
Background The influence of psychoactive drugs on the central nervous system has been investigated with positron emission tomography and task-related functional magnetic resonance imaging. However, it is not known how these drugs affect the intrinsic large-scale interactions of the brain (resting-state functional magnetic resonance imaging connectivity). In this study, the effect of low-dose...
British Journal of Clinical Pharmacology
July 2012
Linda E. Klumpers, Tim L Beumer, Johan G C Van Hasselt et al.
• Cannabis based medicines are registered as a treatment for various indications, such as pain and spasms in multiple sclerosis (MS) patients, and anorexia and nausea in patients with HIV or receiving cancer treatment. • the pharmacokinetics of the various administration routes of cannabis and cannabis based medicines are variable and dosing is hard to regulate. • Namisol is a new tablet...
Psychopharmacology
February 2012
Hendrika H Van Hell, Gerry Jager, Matthijs G. Bossong et al.
Disturbed reward processing in humans has been associated with a number of disorders, such as depression, addiction, and attention-deficit hyperactivity disorder. The endocannabinoid (eCB) system has been implicated in reward processing in animals, but in humans, the relation between eCB functioning and reward is less clear. The current study uses functional magnetic resonance imaging (fMRI) to...
British Journal of Clinical Pharmacology
June 2011
Marieke Liem-Moolenaar, Peter de Boer, Maarten Timmers et al.
• The cholinergic system is important for different central nervous system functions, including memory, learning and attention. Scopolamine, a centrally active muscarinic antagonist, has been used to model dementia and to demonstrate the pharmacological effects of cholinergic drugs, but for most effects the concentration-effect relationships are unknown. • We determined the...
Psychopharmacology
February 2011
Marieke M Lansbergen, Glenn Dumont, Joop van Gerven et al.
Typical users of 3,4-methylenedioxymethamphetamine (MDMA or "ecstasy") are polydrug users, combining MDMA with alcohol or cannabis [most active compound: delta-9-tetrahydrocannabinol (THC)]. The aim of the present study was to investigate whether co-administration of alcohol or THC with MDMA differentially affects ongoing electroencephalogram (EEG) oscillations compared to the administration of...
Social Neuroscience
June 25, 2009
Glenn Dumont, Fred C.g.j. Sweep, R. van der Steen et al.
238 citations
MDMA (3,4-methylenedioxymethamphetamine or "ecstasy") is a recreationally used drug with remarkable and characteristic prosocial effects. In spite of abundant attention in the scientific literature, the mechanism of its prosocial effects has not been elucidated in humans. Recently, research in animals has suggested that the neuropeptide oxytocin may induce these effects. In a double blind,...
Neuropsychopharmacology
February 2009
Matthijs G. Bossong, Bart N M Van Berckel, Ronald Boellaard et al.
The influence of cannabis on mental health receives growing scientific and political attention. An increasing demand for treatment of cannabis dependence has refueled the discussion about the addictive potential of cannabis. A key feature of all addictive drugs is the ability to increase synaptic dopamine levels in the striatum, a mechanism involved in their rewarding and motivating effects....
British Journal of Clinical Pharmacology
January 2009
Lineke Zuurman, Annelies E Ippel, Eduard Moin et al.
An increasing number of novel therapeutic agents are targeted at cannabinoid receptors. Drug development programmes of new cannabinoid drugs may be facilitated by the identification of useful biomarkers. This systemic literature review aims to assess the usefulness of direct biomarkers for the effects of cannabis and tetrahydrocannabinol (THC) in healthy volunteers. One hundred and sixty-five...
Psychopharmacology
February 28, 2008
Glenn Dumont, E. Wezenberg, M. M. G. J. Valkenberg et al.
50 citations
Co-administration of MDMA and ethanol did not exacerbate the effects of either drug alone. Although the impairment of performance by all drug conditions was relatively moderate, all induced significant impairment of cognitive function.