keyword
https://read.qxmd.com/read/38401800/recreational-mdma-doses-do-not-elicit-hepatotoxicity-in-hepg2-spheroids-under-normo-and-hyperthermia
#1
JOURNAL ARTICLE
Arthur L de Oliveira, Raul G Miranda, Daniel J Dorta
MDMA (3,4-methylenedioxymethamphetamine), an entactogen with empathogenic and prosocial effects, is widely used in music festivals and other festive settings. High MDMA doses have been associated with drug-induced liver injury and cases of hyperthermia. Although the latter condition is thought to increase MDMA hepatotoxicity, this correlation remains poorly explored for recreational MDMA doses. On the other hand, the fact that MDMA acts to extinguish fear and to reconsolidate memory could be explored as an adjunct to psychotherapy during treatment of neuropsychiatric disorders such as post-traumatic stress disorder...
February 22, 2024: Toxicology
https://read.qxmd.com/read/38284341/the-psychedelic-future-of-post-traumatic-stress-disorder-treatment
#2
JOURNAL ARTICLE
Tamar Glatman Zaretsky, Kathleen M Jagodnik, Robert Barsic, Josimar Hernandez Antonio, Philip A Bonanno, Carolyn MacLeod, Charlotte Pierce, Hunter Carney, Morgan T Morrison, Charles Saylor, George Danias, Lauren Lepow, Rachel Yehuda
Post-traumatic stress disorder (PTSD) is a mental health condition that can occur following exposure to a traumatic experience. An estimated 12 million U.S. adults are presently affected by this disorder. Current treatments include psychological therapies (e.g., exposure-based interventions) and pharmacological treatments (e.g., selective serotonin reuptake inhibitors (SSRIs)). However, a significant proportion of patients receiving standard-of-care therapies for PTSD remain symptomatic, and new approaches for this and other trauma-related mental health conditions are greatly needed...
2024: Current Neuropharmacology
https://read.qxmd.com/read/38148518/therapeutic-frameworks-in-integration-sessions-in-substance-assisted-psychotherapy-a-systematised-review
#3
REVIEW
Sascha B Thal, Paris Baker, Jonathon Marinis, Michelle Wieberneit, Jason M Sharbanee, Raimundo Bruno, Petra M Skeffington, Stephen J Bright
Serotonergic psychedelics and related substances have been explored as potential adjuncts in substance-assisted psychotherapy (SAPT) for treating various disorders. SAPT can be divided into three phases: preparation, administration and integration. Integration is commonly defined as the comprehension and effective application of insights from psychedelic experiences into everyday life. However, there is limited research regarding the most appropriate therapeutic approach during SAPT. In this article, we discuss the current evidence for different therapeutic frameworks for integration sessions when serotonergic psychedelics and entactogens are used as adjuncts to psychotherapy...
December 26, 2023: Clinical Psychology & Psychotherapy
https://read.qxmd.com/read/38056906/acute-psychotropic-autonomic-and-endocrine-effects-of-5-6-methylenedioxy-2-aminoindane-mdai-compared-with-3-4-methylenedioxymethamphetamine-mdma-in-human-volunteers-a-self-administration-study
#4
JOURNAL ARTICLE
Verena Angerer, Yasmin Schmid, Florian Franz, Heike Gnann, Jan Manuel Speer, Anke Gnann, Stephan Helmecke, Armin Buchwald, Simon D Brandt, Torsten Passie, Matthias E Liechti, Volker Auwärter
The acute psychoactive, autonomic, and endocrine effects of the new psychoactive substance (NPS) 5,6-methylenedioxy-2-aminoindane (MDAI; 3.0 mg/kg, range 180-228 mg) were investigated in six healthy volunteers (four males, two females) in a non-blinded fashion without placebo. Subjective, cardiovascular, and endocrine responses were compared with two different doses of 3,4-methylenedioxymethamphetamine (MDMA) (75 mg and 125 mg) described in previously published placebo-controlled studies, which used identical outcome measures including Visual Analogue Scales (VAS), the Adjective Mood Rating Scale (AMRS), and the 5 Dimensions of Altered States of Consciousness (5D-ASC) scale...
December 6, 2023: Drug Testing and Analysis
https://read.qxmd.com/read/37935915/can-research-on-entactogens-contribute-to-a-deeper-understanding-of-human-sexuality
#5
REVIEW
Justyna Holka-Pokorska
In recent years, scientific research into the therapeutic potential of psychedelic compounds has experienced a resurgence of interest. New studies have shown promising results, supporting the use of psychedelic drugs in treating various psychiatric disorders, including treatment-resistant depression, post-traumatic stress disorder, and even alcohol addiction. The FDA has recognized 3,4-methylenedioxymethamphetamine (MDMA) as a breakthrough therapy to treat symptoms of post-traumatic stress disorder. At the same time, interviews with recreational MDMA users have documented experiences of emotional intimacy while using MDMA, often without the desire for penetrative sex...
November 8, 2023: Pharmacological Reports: PR
https://read.qxmd.com/read/37925136/psychedelic-renaissance-revitalized-potential-therapies-for-psychiatric-disorders
#6
REVIEW
Taeho Greg Rhee, Pasha A Davoudian, Gerard Sanacora, Samuel T Wilkinson
Psychiatric disorders represent the largest cause of disability worldwide. Global interests in psychedelic substances as potentially therapeutic agents for psychiatric disorders has recently re-emerged. Here, we review progress in the development of psychedelic compounds that have potential therapeutic effects as well as the safety concerns. We include psilocybin, N,N-dimethyltryptamine (DMT), lysergic acid diethylamide (LSD), and the entactogen 3,4-methyl-enedioxy-methamphetamine (MDMA). We also review the potential interactive effects these compounds can have with psychotherapeutic approaches...
November 2, 2023: Drug Discovery Today
https://read.qxmd.com/read/37913982/methylone-produces-antidepressant-relevant-actions-and-prosocial-effects
#7
JOURNAL ARTICLE
Zhenlong Li, Hsien-Yu Peng, Chau-Shoun Lee, Tzer-Bin Lin, Ming-Chun Hsieh, Cheng-Yuan Lai, Han-Fang Wu, Lih-Chyang Chen, Mei-Ci Chen, Dylan Chou
Methylone (3,4-methylenedioxy-N-methylcathinone) is a rapid-acting entactogen that has been shown to have significant benefits in patients with post-traumatic stress disorder and major depressive disorder and is well tolerated in phase 1 clinical trials. A recent preclinical study reported that methylone produced robust antidepressant-like actions in naïve rats. However, its antidepressant effects on various stress-related psychopathologies and other neuropsychological actions remain unclear. In the present study, we examined the antidepressant-relevant effects of methylone in learned helplessness (LH) and social defeat stress C57BL/6J male mouse models and further explored its sociability-relevant neuropsychological actions...
October 30, 2023: Neuropharmacology
https://read.qxmd.com/read/37703919/mephedrone-induces-partial-release-at-human-dopamine-transporters-but-full-release-at-human-serotonin-transporters
#8
JOURNAL ARTICLE
Felix P Mayer, Marco Niello, Simon Bulling, Yuan-Wei Zhang, Yang Li, Oliver Kudlacek, Marion Holy, Fatemeh Kooti, Walter Sandtner, Gary Rudnick, Diethart Schmid, Harald H Sitte
Mephedrone (4-methylmethcathinone) is a cathinone derivative that is recreationally consumed for its energizing and empathogenic effects. The stimulating properties are believed to arise from the ability of mephedrone to interact with the high-affinity transporters for dopamine (DA) (DAT) and norepinephrine (NET), whereas the entactogenic effect presumably relies on its activity at the serotonin (5-HT) transporter (SERT). Early studies found that mephedrone acts as a releaser at NET, DAT and SERT, and thus promotes efflux of the respective monoamines...
September 11, 2023: Neuropharmacology
https://read.qxmd.com/read/37600151/locomotor-and-discriminative-stimulus-effects-of-three-benzofuran-compounds-in-comparison-to-abused-psychostimulants
#9
JOURNAL ARTICLE
Rebecca D Hill, Ritu A Shetty, Nathalie Sumien, Michael J Forster, Michael B Gatch
AIMS: Benzofurans are used recreationally, due their ability to cause psychostimulant and/or entactogenic effects, but unfortunately produce substantial adverse effects, including death. Three benzofurans 5-(2-aminopropyl)-2,3-dihydrobenzofuran (5-APDB), 5-(2-aminopropyl)-2,3-dihydrobenzofuran (5-MAPB) and 6-(2-aminopropyl) benzofuran (6-APB) were tested to determine their behavioral effects in comparison with 2,3-methylenedioxymethamphetamine (MDMA), cocaine, and methamphetamine. METHODS: Locomotor activity was tested in groups of 8 male Swiss-Webster mice in an open-field task to screen for locomotor stimulant or depressant effects and to identify behaviorally active doses and times of peak effect...
September 2023: Drug Alcohol Depend Rep
https://read.qxmd.com/read/37590793/perioperative-considerations-for-patients-exposed-to-psychostimulants
#10
JOURNAL ARTICLE
Trent D Emerick, Thomas J Martin, Douglas G Ririe
Concerns regarding the perioperative management of acute psychostimulant intoxication have been recognized for decades, but novel and diverse substances in this class continue to be developed. Despite the similarities in mechanisms of action among psychostimulants, each subclass within this broad category has unique receptor specificity and different mechanisms that play a role in patient clinical presentation. These issues present challenges to anesthesia providers when caring for patients with either acute or chronic exposure to psychostimulants during the perioperative period...
September 1, 2023: Anesthesia and Analgesia
https://read.qxmd.com/read/37488282/therapeutic-mechanisms-of-psychedelics-and-entactogens
#11
REVIEW
Boris D Heifets, David E Olson
Recent clinical and preclinical evidence suggests that psychedelics and entactogens may produce both rapid and sustained therapeutic effects across several indications. Currently, there is a disconnect between how these compounds are used in the clinic and how they are studied in preclinical species, which has led to a gap in our mechanistic understanding of how these compounds might positively impact mental health. Human studies have emphasized extra-pharmacological factors that could modulate psychedelic-induced therapeutic responses including set, setting, and integration-factors that are poorly modelled in current animal experiments...
July 24, 2023: Neuropsychopharmacology
https://read.qxmd.com/read/37360440/swim-in-the-chiral-pool-mdma-and-mda-enantiomers-from-alanine-derived-precursors
#12
JOURNAL ARTICLE
Alexander M Sherwood, Elise K Burkhartzmeyer, Samuel E Williamson, Michael T Faley
A divergent two-step process has provided access to optically pure enantiomers of MDMA and MDA, clinically relevant phenylisopropylamine entactogens. Target compounds were synthesized from commercially available alanine-derived aziridines. Critical process parameters were identified, and the reactions were optimized to avoid chromatographic purifications toward gram-scale isolations, providing ( R )-(-)-MDMA, ( S )-(+)-MDMA, ( R )-(-)-MDA, and ( S )-(+)-MDA each in greater than 98% purity by UPLC, >99% enantiomeric excess, and net yields between 50 and 60% for the complete process...
June 20, 2023: ACS Omega
https://read.qxmd.com/read/37329303/n-n-dimethylpentylone-dipentylone-a-new-synthetic-cathinone-identified-in-a-postmortem-forensic-toxicology-case-series
#13
JOURNAL ARTICLE
Melissa F Fogarty, Alex J Krotulski, Donna M Papsun, Sara E Walton, Michael Lamb, Michael T Truver, Chris W Chronister, Bruce A Goldberger, Barry K Logan
Synthetic cathinones emerged on the novel psychoactive substance (NPS) drug market as alternatives to controlled stimulants and entactogens such as methamphetamine and 3,4-methylenedioxymethamphetamine (MDMA). The majority of synthetic cathinones can be subclassified into two groups: beta-keto amphetamines (i.e., NPS with the suffix "drone") and beta-keto methylenedioxyamphetamines (i.e., NPS with the suffix "lone"). Although a significant number of beta-keto amphetamines have been identified, beta-keto methylenedioxyamphetamines have dominated the NPS market, including notable drugs like methylone, butylone, N-ethyl pentylone (ephylone), eutylone, and now N, N-dimethylpentylone...
June 17, 2023: Journal of Analytical Toxicology
https://read.qxmd.com/read/37253161/assessment-of-the-acute-effects-of-2c-b-vs-psilocybin-on-subjective-experience-mood-and-cognition
#14
JOURNAL ARTICLE
Pablo Mallaroni, Natasha L Mason, Johannes T Reckweg, Riccardo Paci, Sabrina Ritscher, Stefan W Toennes, Eef L Theunissen, Kim P C Kuypers, Johannes G Ramaekers
2,5-dimethoxy-4-bromophenethylamine (2C-B) is a hallucinogenic phenethylamine derived from mescaline. Observational and preclinical data have suggested it to be capable of producing both subjective and emotional effects on par with other classical psychedelics and entactogens. Whereas it is the most prevalently used novel serotonergic hallucinogen to date, it's acute effects and distinctions from classical progenitors have yet to be characterised in a controlled study. We assessed for the first time the immediate acute subjective, cognitive, and cardiovascular effects of 2C-B (20 mg) in comparison to psilocybin (15mg) and placebo in a within-subjects, double-blind, placebo-controlled study of 22 healthy psychedelic-experienced participants...
May 30, 2023: Clinical Pharmacology and Therapeutics
https://read.qxmd.com/read/36969854/acute-pharmacological-profile-of-2c-b-fly-nbome-in-male-wistar-rats-pharmacokinetics-effects-on-behaviour-and-thermoregulation
#15
JOURNAL ARTICLE
Kateřina Syrová, Klára Šíchová, Hynek Danda, Eva Lhotková, Pascal Jorratt, Nikola Pinterová-Leca, Čestmír Vejmola, Lucie Olejníková-Ladislavová, Kateřina Hájková, Martin Kuchař, Jiří Horáček, Tomáš Páleníček
Introduction: N -2-methoxy-benzylated ("NBOMe") analogues of phenethylamine are a group of new psychoactive substances (NPS) with reported strong psychedelic effects in sub-milligram doses linked to a number of severe intoxications, including fatal ones. In our present work, we provide a detailed investigation of pharmacokinetics and acute behavioural effects of 2C-B-Fly-NBOMe (2-(8-bromo-2,3,6,7-tetrahydrobenzo [1,2-b:4,5-b']difuran-4-yl)- N- [(2-methoxybenzyl]ethan-1-amine), an analogue of popular psychedelic entactogen 2C-B (4-Bromo-2,5-dimethoxyphenethylamine)...
2023: Frontiers in Pharmacology
https://read.qxmd.com/read/36835133/aromatic-bromination-abolishes-deficits-in-visuospatial-learning-induced-by-mdma-ecstasy-in-rats-while-preserving-the-ability-to-increase-ltp-in-the-prefrontal-cortex
#16
JOURNAL ARTICLE
Patricio Sáez-Briones, Boris Palma, Héctor Burgos, Rafael Barra, Alejandro Hernández
It has recently been demonstrated that aromatic bromination at C(2) abolishes all typical psychomotor, and some key prosocial effects of the entactogen MDMA in rats. Nevertheless, the influence of aromatic bromination on MDMA-like effects on higher cognitive functions remains unexplored. In the present work, the effects of MDMA and its brominated analog 2Br-4,5-MDMA (1 mg/kg and 10 mg/kg i.p. each) on visuospatial learning, using a radial, octagonal Olton maze (4 × 4) which may discriminate between short-term and long-term memory, were compared with their influence on in vivo long-term potentiation (LTP) in the prefrontal cortex in rats...
February 13, 2023: International Journal of Molecular Sciences
https://read.qxmd.com/read/36768197/behavioral-and-pharmacokinetics-studies-of-n-methyl-2-aminoindane-nm2ai-in-mice-an-aminoindane-briefly-used-in-the-illicit-drug-market
#17
JOURNAL ARTICLE
Micaela Tirri, Giorgia Corli, Raffaella Arfè, Beatrice Marchetti, Sabrine Bilel, Tatiana Bernardi, Federica Boccuto, Sara Odoardi, Serena Mestria, Sabina Strano-Rossi, Matteo Marti
Drug forums are considered as the main platform sources that have contributed to the increase in NPS popularity, especially for those not yet known to law enforcement and therefore not yet illegal. An example is the new synthetic stimulant NM2AI, which has a very short history of human use and abuse. Little is known regarding this compound, but some information from internet forums and the scientific literature indicates NM2AI as a structural derivate of MDAI, which is known for its entactogenic activity. Indeed, the purpose of this study is to evaluate, for the first time, the in vivo acute effect induced by the intraperitoneal injection of NM2AI (1-10-30-100 mg/kg) in mice...
January 18, 2023: International Journal of Molecular Sciences
https://read.qxmd.com/read/36588452/psychedelic-drug-abuse-potential-assessment-for-new-drug-applications-and-controlled-substance-scheduling-a-united-states-perspective
#18
JOURNAL ARTICLE
Jack E Henningfield, Judy Ashworth, David J Heal, Sharon L Smith
BACKGROUND: Psychedelics are an increasingly active area of research and pharmaceutical development. This includes abuse potential assessment to better understand their pharmacological mechanisms and effects and guide controlled substance regulation. Psychedelics pose challenges to abuse assessments to ensure valid, reliable, and generalizable outcomes and safe study conduct. FINDINGS: Key nonclinical techniques, for example, receptor binding and functional assays in vitro, and nonclinical physical dependence determinations, are easily adaptable to psychedelics...
January 2023: Journal of Psychopharmacology
https://read.qxmd.com/read/36529260/experimental-strategies-to-discover-and-develop-the-next-generation-of-psychedelics-and-entactogens-as-medications
#19
REVIEW
D J Heal, J Gosden, S L Smith, C K Atterwill
Research on classical psychedelics (psilocybin, LSD and DMT) and entactogen, MDMA, has produced a renaissance in the search for more effective drugs to treat psychiatric, neurological and various peripheral disorders. Psychedelics and entactogens act though interaction with 5-HT2A and other serotonergic receptors and/or monoamine reuptake transporters. 5-HT, which serves as a neurotransmitter and hormone, is ubiquitously distributed in the brain and peripheral organs, tissues and cells where it has vasoconstrictor, pro-inflammatory and pro-nociceptive actions...
December 15, 2022: Neuropharmacology
https://read.qxmd.com/read/36191546/a-century-of-research-on-psychedelics-a-scientometric-analysis-on-trends-and-knowledge-maps-of-hallucinogens-entactogens-entheogens-and-dissociative-drugs
#20
REVIEW
Marco Solmi, Chaomei Chen, Charles Daure, Anne Buot, Michael Ljuslin, Vincent Verroust, Luc Mallet, Yasser Khazaal, Stephane Rothen, Gabriel Thorens, Daniele Zullino, Gabriella Gobbi, Joshua Rosenblat, Muhammad Ishrat Husain, Danilo De Gregorio, David Castle, Michel Sabé
A scientometric analysis was realized to outline clinical research on psychedelics over the last century. Web of Science Core Collection was searched up to March 18, 2022, for publications on psychedelics. Network analyses and bibliometrics were combined, to identify research themes and trends with Bibliometrix and CiteSpace. The primary aim was to measure research trends evolution over time, and the secondary aims were to identify bibliometric performance and influence networks of publications, authors, institutions, and countries...
September 30, 2022: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
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