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Nashmiah Aid Alrashedy, Jeanmaire Molina
Psychoactive plants contain chemicals that presumably evolved as allelochemicals but target certain neuronal receptors when consumed by humans, altering perception, emotion and cognition. These plants have been used since ancient times as medicines and in the context of religious rituals for their various psychoactive effects (e.g., as hallucinogens, stimulants, sedatives). The ubiquity of psychoactive plants in various cultures motivates investigation of the commonalities among these plants, in which a phylogenetic framework may be insightful...
2016: PeerJ
Nathan Line, Aaron Burns, Sean Butler, Jerry Cashbolm, Craig J Forsyth
Salvinorin A (1) is natural product that in humans is a hallucinogen which binds the human κ-opioid receptor. A total synthesis has been developed that parlays L-(+)-tartaric acid into that of (-)-1 via an unprecedented allylic dithiane intramolecular Diels-Alder reaction to obtain the trans-decalin scaffold. Tsuji allylation set the C9 quaternary center and a late-stage stereoselective chiral ligand-assisted addition of a 3-titanium furan upon a C12 aldehyde / C17 methyl ester established the furanyl lactone moiety...
October 18, 2016: Chemistry: a European Journal
Matthias E Liechti, Patrick C Dolder, Yasmin Schmid
RATIONALE: Lysergic acid diethylamide (LSD) is used recreationally and in clinical research. Acute mystical-type experiences that are acutely induced by hallucinogens are thought to contribute to their potential therapeutic effects. However, no data have been reported on LSD-induced mystical experiences and their relationship to alterations of consciousness. Additionally, LSD dose- and concentration-response functions with regard to alterations of consciousness are lacking. METHODS: We conducted two placebo-controlled, double-blind, cross-over studies using oral administration of 100 and 200 μg LSD in 24 and 16 subjects, respectively...
October 7, 2016: Psychopharmacology
Bas T H de Veen, Arnt F A Schellekens, Michel M M Verheij, Judith R Homberg
INTRODUCTION: Evidence based treatment for Substance use disorders (SUD) includes psychotherapy and pharmacotherapy. However, these are only partially effective. Hallucinogens, such as psilocybin, may represent potential new treatment options for SUD. This review provides a summary of (human) studies on the putative therapeutic effects of psilocybin, and discusses the receptor systems, brain regions and cognitive and emotional processes mediating psilocybin's effects. Psilocybin's chemical structure is similar to that of serotonin...
August 12, 2016: Expert Review of Neurotherapeutics
Attila Szabo, Attila Kovacs, Jordi Riba, Srdjan Djurovic, Eva Rajnavolgyi, Ede Frecska
N,N-dimethyltryptamine (DMT) is a potent endogenous hallucinogen present in the brain of humans and other mammals. Despite extensive research, its physiological role remains largely unknown. Recently, DMT has been found to activate the sigma-1 receptor (Sig-1R), an intracellular chaperone fulfilling an interface role between the endoplasmic reticulum (ER) and mitochondria. It ensures the correct transmission of ER stress into the nucleus resulting in the enhanced production of antistress and antioxidant proteins...
2016: Frontiers in Neuroscience
L Garcin, M Le Roch, C-A Agbessi, J-B Lobut, A Lecoeur, G Benoist
"Purple drank" is a dangerous hallucinogenic cocktail commonly used by teenagers, made popular by American rappers and social networks. It combines codeine-based cough syrup, antihistamines such as promethazine, and soda. Unknown by caregivers, it may be responsible for serious neuropsychological complications. We report the effects of this new risky behavior in three patients: a 14-year-old girl and her boyfriend, both found in an initial state of drowsiness, followed by hallucinations and anticholinergic toxidrome; and another teenager whose chronic use led to addiction with increasing doses...
September 23, 2016: Archives de Pédiatrie: Organe Officiel de la Sociéte Française de Pédiatrie
Somandla Ncube, Anna Poliwoda, Hlanganani Tutu, Piotr Wieczorek, Luke Chimuka
A liquid phase microextraction based on hollow fibre followed by liquid chromatographic determination was developed for the extraction and quantitation of the hallucinogenic muscimol from urine samples. Method applicability on polar hallucinogens was also tested on two alkaloids, a psychedelic hallucinogen, tryptamine and a polar amino acid, tryptophan which exists in its charged state in the entire pH range. A multivariate design of experiments was used in which a half fractional factorial approach was applied to screen six factors (donor phase pH, acceptor phase HCl concentration, carrier composition, stirring rate, extraction time and salt content) for their extent of vitality in carrier mediated liquid microextractions...
October 15, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Amber L Bahorik, Derek D Satre, Andrea H Kline-Simon, Constance M Weisner, Cynthia I Campbell
OBJECTIVES: We examined prevalence of major medical conditions and extent of disease burden among patients with and without substance use disorders (SUDs) in an integrated health care system serving 3.8 million members. METHODS: Medical conditions and SUDs were extracted from electronic health records in 2010. Patients with SUDs (n = 45,461; alcohol, amphetamine, barbiturate, cocaine, hallucinogen, and opioid) and demographically matched patients without SUDs (n = 45,461) were compared on the prevalence of 19 major medical conditions...
September 8, 2016: Journal of Addiction Medicine
Tomohisa Mori, Tsutomu Suzuki
The subjective effects of drugs are related to the kinds of feelings they produce, such as euphoria or dysphoria. One of the methods that can be used to study these effects is the drug discrimination procedure. Many researchers have been trying to elucidate the mechanisms that underlie the discriminative stimulus properties of abused drugs (e.g., alcohol, psychostimulants, and opioids). Over the past two decades, patterns of drug abuse have changed, so that club/recreational drugs such as phencyclidine (PCP), 3,4-methylenedioxymethamphetamine (MDMA), ketamine, and cannabinoid, which induce perceptual distortions, like hallucinations, are now more commonly abused, especially in younger generations...
September 2, 2016: Current Topics in Behavioral Neurosciences
Sebastian Leth-Petersen, Ida Nymann Petersen, Anders A Jensen, Christoffer Bundgaard, Mathias Bæk, Jan Kehler, Jesper L Kristensen
The toxic hallucinogen 25B-NBOMe is very rapidly degraded by human liver microsomes and has low oral bioavailability. Herein we report on the synthesis, microsomal stability and 5-HT2A/5-HT2C receptor profile of novel analogs of 25B-NBOMe modified at the primary site of metabolism. Although microsomal stability could be increased while maintaining potent 5-HT2 receptor agonist properties, all analogs had an intrinsic clearance above 1.3 L/kg/h predictive of high first-pass metabolism.
August 26, 2016: ACS Chemical Neuroscience
Molly Howland, Jennifer Levin, Carol Blixen, Curtis Tatsuoka, Martha Sajatovic
BACKGROUND: Internalized stigma, which occurs when stigmatized individuals accept society's assessment and incorporate this assessment into their sense of self, is prevalent in individuals with bipolar disorder (BD). This study explored the correlates of internalized stigma in a research sample of patients with BD who were poorly adherent to their medications. METHODS: Both quantitative and qualitative analyses were performed. Scores of 115 individuals with BD on the Internalized Stigma of Mental Illness (ISMI) scale were correlated with scores on the General Self-Efficacy (GSE) Scale, Brief Psychiatric Rating Scale (BPRS), Montgomery-Asberg Depression Rating Scale (MADRS), and Young Mania Rating Scale (YMRS)...
October 2016: Comprehensive Psychiatry
Shruti Beharry, Simon Gibbons
The purpose of this review is to identify emerging or new psychoactive substances (NPS) by undertaking an online survey of the UK NPS market and to gather any data from online drug forums and published literature. Drugs from four main classes of NPS were identified: psychostimulants, dissociative anaesthetics, hallucinogens (phenylalkylamine-based and lysergamide-based materials) and finally benzodiazepines. For inclusion in the review, the 'user reviewers' on drugs forums were selected based on whether or not the particular NPS of interest was used alone or in combination...
October 2016: Forensic Science International
Theodore J Cicero, Matthew S Ellis, Zachary A Kasper
Physicians are frequently thought to be a major source of opioids diverted for non-therapeutic purposes, largely because it is so difficult for them to discern which patients might abuse them. In this study we sought to determine whether those who were first exposed to an opioid through a physician's prescription, and subsequently developed a substance use disorder, had a history of using psychoactive drugs prior to abusing opioids. Patients entering one of 125 drug treatment programs across the country for opioid abuse were asked to provide detailed histories of psychoactive drug use prior to their initial opioid exposure...
August 15, 2016: Addictive Behaviors
Danilo De Gregorio, Luca Posa, Rafael Ochoa-Sanchez, Ryan McLaughlin, Sabatino Maione, Stefano Comai, Gabriella Gobbi
d-lysergic diethylamide (LSD) is a hallucinogenic drug that interacts with the serotonin (5-HT) system binding to 5-HT1 and 5-HT2 receptors. Little is known about its potential interactions with the dopamine (DA) neurons of the ventral tegmental area (VTA). Using in-vivo electrophysiology in male adult rats, we evaluated the effects of cumulative doses of LSD on VTA DA neuronal activity, compared these effects to those produced on 5-HT neurons in the dorsal raphe nucleus (DRN), and attempted to identify the mechanism of action mediating the effects of LSD on VTA DA neurons...
August 17, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Bjoern Moosmann, Philippe Bisel, Florian Franz, Laura M Huppertz, Volker Auwärter
Designer benzodiazepines represent an emerging class of new psychoactive substances (NPS). While other classes of NPS such as cannabinoid receptor agonists and designer stimulants are mainly consumed for hedonistic reasons, designer benzodiazepines may also be consumed as 'self-medication' by persons with anxiety or other psychiatric disorders or as stand-by 'antidote' by users of stimulant and hallucinogenic drugs. In the present study, five benzodiazepines (adinazolam, cloniprazepam, fonazepam, 3-hydroxyphenazepam, and nitrazolam) and one thienodiazepine (metizolam) offered as 'research chemicals' on the Internet were characterized and their main in vitro phase I metabolites tentatively identified after incubation with pooled human liver microsomes...
August 17, 2016: Journal of Mass Spectrometry: JMS
Heather Kang, Pojeong Park, Zuner A Bortolotto, Simon D Brandt, Tristan Colestock, Jason Wallach, Graham L Collingridge, David Lodge
To avoid legislation based on chemical structure, research chemicals, frequently used for recreational purposes, are continually being synthesized. N-Ethyl-1,2-diphenylethanamine (ephenidine) is a diarylethylamine that has recently become popular with recreational users searching for dissociative hallucinogenic effects. In the present study, the pharmacological basis of its neural actions has been investigated, initially by assessing its profile in central nervous system receptor binding assays and subsequently in targeted electrophysiological studies...
August 9, 2016: Neuropharmacology
H Tegetmeyer
Background: The symptom "visual snow" describes the continuous perception of tiny flickering dots within the whole visual field of both eyes. The diagnosis of a visual snow syndrome requires the appearance of typical additional visual symptoms and the exclusion of ophthalmological or neurological causes, or pharmacological influences. Patients and Methods: Three male and four female subjects between 13 and 36 years of age referred with visual snow were investigated and asked about their symptoms. A complete ophthalmological investigation, including binocular fundoscopy, was performed in all patients...
August 10, 2016: Klinische Monatsblätter Für Augenheilkunde
Terrell Holloway, Jose L Moreno, Javier González-Maeso
The heteromeric receptor complex between 5-HT2A and mGlu2 has been implicated in some of the behavioral phenotypes in mouse models of psychosis(1,2). Consequently, investigation of structural details of the interaction between 5-HT2A and mGlu2 affecting schizophrenia-related behaviors represents a powerful translational tool. As previously shown, the head-twitch response (HTR) in mice is elicited by hallucinogenic drugs and this behavioral response is absent in 5-HT2A knockout (KO) mice(3,4). Additionally, by conditionally expressing the 5-HT2A receptor only in cortex, it was demonstrated that 5-HT2A receptor-dependent signaling pathways on cortical pyramidal neurons are sufficient to elicit head-twitch behavior in response to hallucinogenic drugs(3)...
2016: Journal of Visualized Experiments: JoVE
Jonathan D Moreno
Henry Knowles Beecher, an icon of human research ethics, and Timothy Francis Leary, a guru of the counterculture, are bound together in history by the synthetic hallucinogen lysergic acid diethylamide (LSD). Both were associated with Harvard University during a critical period in their careers and of drastic social change. To all appearances the first was a paragon of the establishment and a constructive if complex hero, the second a rebel and a criminal, a rogue and a scoundrel. Although there is no evidence they ever met, Beecher's indirect struggle with Leary over control of the 20th century's most celebrated psychedelic was at the very heart of his views about the legitimate, responsible investigator...
2016: Perspectives in Biology and Medicine
Sebastian Rojek, Filip Bolechała, Karol Kula, Martyna Maciów-Głąb, Małgorzata Kłys
Unlike amphetamine, amphetamine-like substances accessible on the drug market are less expensive and more easily available; they also produce hallucinogenic effects expected by the users. Such properties render them more attractive as compared to amphetamine. On the other hand, the knowledge of the toxicity of these compounds is very limited, what in consequence generates problems that create ever-expanding research areas, including analytical, clinical and medicolegal issues, thus leading to development of systemic databases...
July 2016: Legal Medicine
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