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Markus R Meyer
This summarizing and descriptive review article is an update on previously published reviews. It covers English-written and PubMed-listed review articles and original studies published between May 2016 and November 2017 on the toxicokinetics of new psychoactive substances (NPS). Compounds covered include stimulants and entactogens, synthetic cannabinoids, tryptamines, phenethylamine and phencyclidine-like drugs, benzodiazepines, and opioids. First, an overview and discussion is provided on selected review articles followed by an overview and discussion on selected original studies...
February 24, 2018: Handbook of Experimental Pharmacology
Jacob Fox, Alexis Smith, Alexander Yale, Christopher Chow, Elsa Alaswad, Tracy Cushing, Andrew A Monte
BACKGROUND: Drugs of abuse (DOA) are widely used in the United States and are ubiquitous at outdoor music festivals. Attendees at music festivals are at high-risk for novel psychoactive substance (NPS) use, which is becoming more prevalent worldwide. No U.S. studies have employed an qualitative approach to investigate the etiologies of both traditional DOA and NPS use amongst music festival attendees. OBJECTIVES: The objective of this study was to improve understanding of the knowledge, attitudes, beliefs, and practices of festival attendees using NPS and DOA...
November 17, 2017: Substance Use & Misuse
Sean B Dolan, Michael J Forster, Michael B Gatch
Novel psychoactive substances have maintained a prominent role in the global drug culture, despite increased regulation by governing bodies. Novel compounds continue to become available on the market, often in "Ecstasy" or "Molly" formulations in lieu of MDMA, at a much faster rate than they can be properly characterized. The current study aimed to investigate the discriminative stimulus and locomotor effects of three putatively entactogenic compounds that have become increasingly prevalent on the drug market: 5-(2-aminopropyl)-benzofuran (5-APB), 6-(2-aminopropryl)-2,3-dihydrobenzofuran (6-APDB), and 4-fluoroamphetamine (4-FA)...
August 24, 2017: Drug and Alcohol Dependence
Tomislav Majić, Henrik Jungaberle, Timo T Schmidt, Andrea Zeuch, Leo Hermle, Jürgen Gallinat
Background  Recently, scientific interest in the therapeutic potential of serotonergic and psilocybin hallucinogens (psychedelics) such as lysergic acid diethylamide (LSD) and entactogens like 3,4-methylendioxymethamphetamine (MDMA) within the framework of psychotherapy has resumed. The present article provides an overview on the current evidence on substance-assisted psychotherapy with these substances. Method  A selective search was carried out in the PubMed and Cochrane Library including studies investigating the clinical use of serotonergic psychoactive substances since 2000...
July 2017: Fortschritte der Neurologie-Psychiatrie
Dino Luethi, Karolina E Kolaczynska, Luca Docci, Stephan Krähenbühl, Marius C Hoener, Matthias E Liechti
BACKGROUND: Mephedrone is a synthetic cathinone and one of the most popular recreationally used new psychoactive substances. The aim of the present study was to characterize the in vitro pharmacology of novel analogs of mephedrone and related newly emerged designer stimulants. METHODS: We determined norepinephrine, dopamine, and serotonin transporter inhibition potencies and monoamine release in transporter-transfected human embryonic kidney 293 cells. We also assessed monoamine receptor and transporter binding affinities...
July 26, 2017: Neuropharmacology
Michael B Gatch, Sean B Dolan, Michael J Forster
There has been increasing use of novel synthetic hallucinogenic compounds, 2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine hydrochloride (25B-NBOMe), 2-(4-chloro-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine hydrochloride (25C-NBOMe), 2-(4-iodo-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine hydrochloride (25I-NBOMe), and N,N-diallyl-5-methoxy tryptamine (5-MeO-DALT), which have been associated with severe toxicities. These four compounds were tested for discriminative stimulus effects similar to a prototypical hallucinogen (-)-2,5-dimethoxy-4-methylamphetamine (DOM) and the entactogen (±)-3,4-methylenedioxymethamphetamine (MDMA)...
August 2017: Behavioural Pharmacology
Shawn M Aarde, Michael A Taffe
Animal models of drug self-administration are currently the gold standard for making predictions regarding the relative likelihood that a recreational drug substance will lead to continued use and addiction. Such models have been found to have high predictive accuracy and discriminative validity for a number of drug classes including ethanol, nicotine, opioids, and psychostimulants such as cocaine and methamphetamine. Members of the entactogen class of psychostimulants (drugs that produce an "open mind state" including feelings of interpersonal closeness, intimacy and empathy) have been less frequently studied in self-administration models...
2017: Current Topics in Behavioral Neurosciences
Markus R Meyer
This review article covers English-written and PubMed-listed review articles and original studies published between January 2015 and April 2016 dealing with the toxicodynamics and toxicokinetics of new psychoactive substances. Compounds covered include stimulants and entactogens, synthetic cannabinoids, tryptamines, NBOMes, phencyclidine-like drugs, benzodiazepines, and opioids. First, an overview and discussion is provided on timely review articles followed by an overview and discussion on recent original studies...
October 2016: Archives of Toxicology
Natalie R Sealover, Bruce Felts, Charles P Kuntz, Rachel E Jarrard, Gregory H Hockerman, Patrick W Lamb, Eric L Barker, L Keith Henry
The substituted amphetamine, 3,4-methylenedioxy-methamphetamine (MDMA, ecstasy), is a widely used drug of abuse that induces non-exocytotic release of serotonin, dopamine, and norepinephrine through their cognate transporters as well as blocking the reuptake of neurotransmitter by the same transporters. The resulting dramatic increase in volume transmission and signal duration of neurotransmitters leads to psychotropic, stimulant, and entactogenic effects. The mechanism by which amphetamines drive reverse transport of the monoamines remains largely enigmatic, however, promising outcomes for the therapeutic utility of MDMA for post-traumatic stress disorder and the long-time use of the dopaminergic and noradrenergic-directed amphetamines in treatment of attention-deficit hyperactivity disorder and narcolepsy increases the importance of understanding this phenomenon...
November 15, 2016: Biochemical Pharmacology
Albert Garcia-Romeu, Brennan Kersgaard, Peter H Addy
Hallucinogens fall into several different classes, as broadly defined by pharmacological mechanism of action, and chemical structure. These include psychedelics, entactogens, dissociatives, and other atypical hallucinogens. Although these classes do not share a common primary mechanism of action, they do exhibit important similarities in their ability to occasion temporary but profound alterations of consciousness, involving acute changes in somatic, perceptual, cognitive, and affective processes. Such effects likely contribute to their recreational use...
August 2016: Experimental and Clinical Psychopharmacology
Monika Židková, Igor Linhart, Marie Balíková, Michal Himl, Lubomír Váňa, Michal Vetýška, Tomáš Páleníček, Eva Lhotková, Martin Dušek
1. 5,6-Methylenedioxy-2-aminoindane (MDAI) is a member of aminoindane drug family with serotoninergic effect, which appeared on illicit drug market as a substitute for banned stimulating and entactogenic drugs. 2. Metabolism of MDAI, which has been hitherto unexplored, was studied in rats dosed with a subcutaneous dose of 20 mg MDAI.HCl/kg body weight. The urine of rats was collected within 24 h after dosing for analyses by HPLC-ESI-HRMS and GC/MS. 3. The main metabolic pathways proceeding in parallel were found to be oxidative demethylenation followed by O-methylation and N-acetylation...
June 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Lewis Jones, Phil Reed, Andrew Parrott
AIMS: The purpose of this study was to compare the effects of mephedrone and 3,4-methylenedioxy-methamphetamine (MDMA), as reported by young recreational polydrug users. METHODS: 152 MDMA users and 81 mephedrone users were recruited through snowballing on social network sites. They completed a standard online questionnaire for either mephedrone or MDMA. The questions covered the average amount taken per session, the longest duration of usage in the last 12-months, subjective effects while on-drug, and recovery effects in the days afterwards...
December 2016: Journal of Psychopharmacology
Tomáš Páleníček, Eva Lhotková, Monika Žídková, Marie Balíková, Martin Kuchař, Michal Himl, Petra Mikšátková, Martin Čegan, Karel Valeš, Filip Tylš, Rachel R Horsley
MDAI (5,6-Methylenedioxy-2-aminoindane) has a reputation as a non-neurotoxic ecstasy replacement amongst recreational users, however the drug has been implicated in some severe and lethal intoxications. Due to this, and the fact that the drug is almost unexplored scientifically we investigated a broad range of effects of acute MDAI administration: pharmacokinetics (in sera, brain, liver and lung); behaviour (open field; prepulse inhibition, PPI); acute effects on thermoregulation (in group-/individually-housed rats); and systemic toxicity (median lethal dose, LD50) in Wistar rats...
August 1, 2016: Progress in Neuro-psychopharmacology & Biological Psychiatry
Jacques D Nguyen, Yanabel Grant, Kevin M Creehan, Sophia A Vandewater, Michael A Taffe
The recreational use of substituted cathinones continues to grow as a public health concern in the United States. Studies have shown that extended access to intravenous (i.v.) self-administration of stimulants, such as cocaine and methamphetamine, results in escalation of drug intake relative to shorter access; however, little is known about the impact of extended access on self-administration of entactogen class stimulants such as methylone and 4-methylmethcathinone (mephedrone). Male Wistar rats were randomly assigned to short-access (ShA, 2- h) and long-access (LgA, 6- h) groups and trained to self-administer methylone or mephedrone (0...
September 2017: Addiction Biology
Débora González, Marta Torrens, Magí Farré
BACKGROUND: 2C-B (Nexus) is one of the most widespread novel psychoactive substances. There is limited information about its pharmacological properties, and few studies in humans concern its acute and chronic effects. 2C-B has been classified as a stimulant, hallucinogen, entactogen, and/or empathogen. OBJECTIVES: To evaluate the emotional, subjective, and cardiovascular effects of 2C-B. METHODS: Twenty healthy recreational 2C-B users (12 women) self-administered a 20 mg dose of 2C-B...
2015: BioMed Research International
Sophia A Vandewater, Kevin M Creehan, Michael A Taffe
The intravenous self-administration (IVSA) of 3,4-methylenedioxymethamphetamine (MDMA) is inconsistent in rats, with up to half of subjects failing to acquire reliable drug intake. It is unknown if this changes under long-access conditions (6 h sessions) under which the IVSA of cocaine and methamphetamine escalates. The entactogen class cathinone stimulants which exhibit MDMA-like monoamine effects in the nucleus accumbens, mephedrone (4-methylmethcathinone) and methylone (3,4-methylenedioxymethcathinone), may support more reliable IVSA but results have been mixed...
December 2015: Neuropharmacology
Rodrigo Álvarez-Ruiz, María Jesús Andrés-Costa, Vicente Andreu, Yolanda Picó
An analytical method for determining traditional and emerging drugs of abuse in particulate matter, sewage sludge and sediment has been developed and validated. A total of 41 drugs of abuse and metabolites including cocainics, tryptamines, amphetamines, arylcyclohexylamines, cathinones, morphine derivatives, pyrrolidifenones derivatives, entactogens, piperazines and other psychostimulants were selected. Samples were ultrasound extracted with McIlvaine buffer and methanol, and the extracts were cleaned up by solid phase extraction (SPE) using Strata-X cartridges...
July 31, 2015: Journal of Chromatography. A
François Chavant, Alexandra Boucher, Reynald Le Boisselier, Sylvie Deheul, Danièle Debruyne
New substances, also known as "designer drugs" or "legal highs" are increasingly available to drug users. Two hundred and fifteen hitherto unlisted substances have been notified by European Union member states since 2005. These synthetic drugs, which have been developed to side-step the legislation on drugs, are analogues or derivatives of existing drugs and medications. The availability of these "legal highs", sold on Internet under various denominations such as bath salt, plant fertilizer, chemical not intended for human use, or spice, is unlimited...
March 2015: Thérapie
Anna Rickli, Simone Kopf, Marius C Hoener, Matthias E Liechti
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 2C-B-FLY on the human noradrenaline (NA), dopamine and 5-HT uptake transporters using HEK 293 cells that express the respective transporters...
July 2015: British Journal of Pharmacology
Daniel José Barbosa, João Paulo Capela, Rita Feio-Azevedo, Armanda Teixeira-Gomes, Maria de Lourdes Bastos, Félix Carvalho
Amphetamines are a class of psychotropic drugs with high abuse potential, as a result of their stimulant, euphoric, emphathogenic, entactogenic, and hallucinogenic properties. Although most amphetamines are synthetic drugs, of which methamphetamine, amphetamine, and 3,4-methylenedioxymethamphetamine ("ecstasy") represent well-recognized examples, the use of natural related compounds, namely cathinone and ephedrine, has been part of the history of humankind for thousands of years. Resulting from their amphiphilic nature, these drugs can easily cross the blood-brain barrier and elicit their well-known psychotropic effects...
October 2015: Archives of Toxicology
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