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Remco H S Westerink

9 papers in the library · 188 citations · publishing 2011-2018

Papers

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Effect fingerprinting of new psychoactive substances (NPS): What can we learn from in vitro data?

Pharmacology & Therapeutics February 1, 2018 Laura Hondebrink, Anne Zwartsen, Remco H S Westerink 78 citations

The use of new psychoactive substances (NPS) is increasing and currently >600 NPS have been reported. However, limited information on neuropharmacological and toxicological effects of NPS is available, hampering risk characterization. We reviewed the literature on the in vitro neuronal modes of action to obtain effect fingerprints of different classes of illicit drugs and NPS. The most...

DOI: 10.1016/j.pharmthera.2017.10.022 (opens in new tab) Full text (opens in new tab) Designer drugs Mechanism of action Receptors Transporters +5

Measuring inhibition of monoamine reuptake transporters by new psychoactive substances (NPS) in real-time using a high-throughput, fluorescence-based assay.

Toxicology in Vitro December 1, 2017 Anne Zwartsen, Anouk H A Verboven, Regina G D M Van Kleef et al. 59 citations

The prevalence and use of new psychoactive substances (NPS) is increasing and currently over 600 NPS exist. Many illicit drugs and NPS increase brain monoamine levels by inhibition and/or reversal of monoamine reuptake transporters (DAT, NET and SERT). This is often investigated using labor-intensive, radiometric endpoint measurements. We investigated the applicability of a novel and innovative...

DOI: 10.1016/j.tiv.2017.05.010 (opens in new tab) Full text (opens in new tab) Designer drugs Dopamine transporter Drug screening Fluorescent monoamine substrate +2

Neuropharmacological characterization of the new psychoactive substance methoxetamine

Neuropharmacology September 1, 2017 Laura Hondebrink, E. Kasteel, A. Tukker et al.

&NA; The use of new psychoactive substances (NPS) is steadily increasing. One commonly used NPS is methoxetamine (MXE), a ketamine analogue. Several adverse effects have been reported following MXE exposure, while only limited data are available on its neuropharmacological modes of action. We investigated the effects of MXE and ketamine on several endpoints using multiple in vitro models. These...

Hallucinogen persisting perception disorder and the serotonergic system: a comprehensive review including new MDMA-related clinical cases.

European Neuropsychopharmacology August 2014 Ruud P. W. Litjens, Tibor M Brunt, Gerard-Jan Alderliefste et al.

Hallucinogen persisting perception disorder (HPPD) is a drug-induced condition associated with inaccurate visual representations. Since the underlying mechanism(s) are largely unknown, this review aims to uncover aspects underlying its etiology. Available evidence on HPPD and drug-related altered visual processing was reviewed and the majority of HPPD cases were attributed to drugs with...

Additive inhibition of human α1β2γ2 GABAA receptors by mixtures of commonly used drugs of abuse.

Neurotoxicology March 2013 Laura Hondebrink, Sijie Tan, Elise Hermans et al.

Yearly, exposure to drugs of abuse results in ∼1 million emergency department visits in the US. In ∼50% of the visits, stimulant drugs like cocaine and amphetamine-like substances (e.g. 3,4-methylenedioxymethamphetamine (MDMA, the main active ingredient of ecstasy)) are involved, whereas in ∼60% multiple drugs are involved. These drugs induce higher dopamine and serotonin levels resulting in...

Pharmacokinetics and pharmacodynamics of 3,4-methylenedioxymethamphetamine (MDMA): interindividual differences due to polymorphisms and drug–drug interactions

Critical Reviews in Toxicology October 3, 2012 Saskia J. Rietjens, Laura Hondebrink, Remco H S Westerink et al. 51 citations

Clinical outcome following 3,4-methylenedioxymethamphetamine (MDMA) intake ranges from mild entactogenic effects to a life-threatening intoxication. Despite ongoing research, the clinically most relevant mechanisms causing acute MDMA-induced adverse effects remain largely unclear. This complicates the triage and treatment of MDMA users needing medical care. The user's genetic profile and...

Methamphetamine, amphetamine, MDMA ('ecstasy'), MDA and mCPP modulate electrical and cholinergic input in PC12 cells.

Neurotoxicology March 2012 Laura Hondebrink, Jan Meulenbelt, Saskia J. Rietjens et al.

Reversal of the dopamine (DA) membrane transporter is the main mechanism through which many drugs of abuse increase DA levels. However, drug-induced modulation of exocytotic DA release by electrical (depolarization) and neurochemical inputs (e.g., acetylcholine (ACh)) may also contribute. We therefore investigated effects of methamphetamine, amphetamine, 3,4-methylenedioxymethamphetamine...

Modulation of human GABAA receptor function: a novel mode of action of drugs of abuse.

Neurotoxicology December 2011 Laura Hondebrink, Jan Meulenbelt, Regina G D M Van Kleef et al.

Drugs of abuse are known to mainly affect the dopaminergic and serotonergic system, although behavioral studies indicated that the GABA-ergic system also plays a role. We therefore investigated the acute effects of several commonly used drugs of abuse (methamphetamine, amphetamine, 3,4-methylenedioxymethamphetamine (MDMA), 3,4-methylenedioxyamphetamine (MDA) and meta-chlorophenylpiperazine...

High concentrations of MDMA ('ecstasy') and its metabolite MDA inhibit calcium influx and depolarization-evoked vesicular dopamine release in PC12 cells.

Neuropharmacology 2011 Laura Hondebrink, Jan Meulenbelt, Marieke Meijer et al.

The popular synthetic drug of abuse 3,4-methylenedioxymethampetamine (MDMA) and its metabolite 3,4-methylenedioxyamphetamine (MDA) act mainly on the serotonergic system, though they also increase the amount of extracellular dopamine (DA) in the brain, presumably via reversal of the membrane dopamine transporter (DAT). As the involvement of exocytotic DA release is debated, we investigated if...