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https://www.readbyqxmd.com/read/29714473/dark-classics-in-chemical-neuroscience-cathinone-derived-psychostimulants
#1
Steven J Simmons, Jonna M Leyrer-Jackson, Chicora F Oliver, Callum Hicks, John Muschamp, Scott M Rawls, M Foster Olive
Cathinone is a plant alkaloid found in khat leaves of perennial shrubs grown in East Africa. Similar to cocaine, cathinone elicits psychostimulant effects which are in part attributed to its amphetamine-like structure. Around 2010, home laboratories began altering the parent structure of cathinone to synthesize derivatives with mechanisms of action, potencies, and pharmacokinetics permitting high abuse potential and toxicity. These "synthetic cathinones" include 4-methylmethcathinone (mephedrone), 3,4-methylenedioxypyrovalerone (MDPV) and the empathogenic agent 3,4-methylenedioxymethcathinone (methylone) which collectively gained international popularity following aggressive online marketing as well as availability in various retail outlets...
May 1, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29674947/health-and-social-problems-associated-with-recent-novel-psychoactive-substance-nps-use-amongst-marginalised-nightlife-and-online-users-in-six-european-countries
#2
Marie Claire Van Hout, Annemieke Benschop, Michal Bujalski, Katarzyna Dąbrowska, Zsolt Demetrovics, Katalin Felvinczi, Evelyn Hearne, Susana Henriques, Zsuzsa Kaló, Gerrit Kamphausen, Dirk Korf, Joana Paula Silva, Łukasz Wieczorek, Bernd Werse
Continued diversification and use of new psychoactive substances (NPS) across Europe remains a public health challenge. The study describes health and social consequences of recent NPS use as reported in a survey of marginalised, nightlife and online NPS users in the Netherlands, Hungary, Portugal, Ireland, Germany and Poland ( n  = 3023). Some respondents were unable to categorise NPS they had used. Use of ' herbal blends ' and ' synthetic cannabinoids obtained pure ' was most reported in Germany, Poland and Hungary, and use of ' branded stimulants ' and ' stimulants/empathogens/nootropics obtained pure ' was most reported in the Netherlands...
2018: International Journal of Mental Health and Addiction
https://www.readbyqxmd.com/read/29148866/drugs-of-abuse-and-novel-psychoactive-substances-at-outdoor-music-festivals-in-colorado
#3
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
https://www.readbyqxmd.com/read/29030166/mdpv-and-%C3%AE-pvp-use-in-humans-the-twisted-sisters
#4
REVIEW
Laurent Karila, Geneviève Lafaye, Amandine Scocard, Olivier Cottencin, Amine Benyamina
The new psychoactive substances phenomenon continues to represent a considerable public health challenge. Synthetic cathinones are β-keto amphetamine analogues, also known as legal highs, research chemicals, bath salts. These drugs have surfaced as a popular alternative to other illicit drugs of abuse, such as cocaine, MDMA, and methamphetamine, due to their potent psychostimulant and empathogenic effects. Pyrovalerone cathinones (a-pyrrolidinophenones) form a distinct group of designer cathinones, such as MDPV...
October 10, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28631526/lifetime-experience-with-classic-psychedelics-predicts-pro-environmental-behavior-through-an-increase-in-nature-relatedness
#5
Matthias Forstmann, Christina Sagioglou
In a large-scale ( N = 1487) general population online study, we investigated the relationship between past experience with classic psychedelic substances (e.g. LSD, psilocybin, mescaline), nature relatedness, and ecological behavior (e.g. saving water, recycling). Using structural equation modeling we found that experience with classic psychedelics uniquely predicted self-reported engagement in pro-environmental behaviors, and that this relationship was statistically explained by people's degree of self-identification with nature...
June 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28631397/the-effects-and-toxicity-of-cathinones-from-the-users-perspectives-a-qualitative-study
#6
Sulaf Assi, Nargilya Gulyamova, Paul Kneller, David Osselton
OBJECTIVE: The objective of this study is to explore the users' perspectives regarding the effects and toxicity of cathinones. METHODS: A systematic search of Internet discussion forums yielded 303 threads relevant to the research objectives. The threads were analysed by conventional content analysis where concepts were developed from codes and themes. RESULTS: The study identified 3 main themes in relation to cathinone use, effects, and toxicity...
May 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28244748/the-2014-philip-s-portoghese-medicinal-chemistry-lectureship-the-phenylalkylaminome-with-a-focus-on-selected-drugs-of-abuse
#7
Richard A Glennon
The phenylalkylamine, particularly the phenylethylamine, moiety is a common structural feature found embedded in many clinically approved agents. Greater still is its occurrence in drugs of abuse. The simplest phenylethylamine, 2-phenylethylamine itself, is without significant central action when administered at moderate doses, but fairly simple structural modifications profoundly impact its pharmacology and result in large numbers of useful pharmacological tools, agents with therapeutic potential, and in drugs of abuse (e...
April 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27799294/structure-activity-relationships-of-substituted-cathinones-with-transporter-binding-uptake-and-release
#8
Amy J Eshleman, Katherine M Wolfrum, John F Reed, Sunyoung O Kim, Tracy Swanson, Robert A Johnson, Aaron Janowsky
Synthetic cathinones are components of "bath salts" and have physical and psychologic side effects, including hypertension, paranoia, and hallucinations. Here, we report interactions of 20 "bath salt" components with human dopamine, serotonin, and norepinephrine transporters [human dopamine transporter (hDAT), human serotonin transporter (hSERT), and human norepinephrine transporter (hNET), respectively] heterologously expressed in human embryonic kidney 293 cells. Transporter inhibitors had nanomolar to micromolar affinities (Ki values) at radioligand binding sites, with relative affinities of hDAT>hNET>hSERT for α-pyrrolidinopropiophenone (α-PPP), α-pyrrolidinobutiophenone, α-pyrrolidinohexiophenone, 1-phenyl-2-(1-pyrrolidinyl)-1-heptanone, 3,4-methylenedioxy-α-pyrrolidinopropiophenone, 3,4-methylenedioxy-α-pyrrolidinobutiophenone, 4-methyl-α-pyrrolidinopropiophenone, α-pyrrolidinovalerophenone, 4-methoxy-α-pyrrolidinovalerophenone, α-pyrrolidinopentiothiophenone (alpha-PVT), and α-methylaminovalerophenone, and hDAT>hSERT>hNET for methylenedioxypentedrone...
January 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/26543863/acute-effects-of-the-novel-psychoactive-drug-2c-b-on-emotions
#9
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
https://www.readbyqxmd.com/read/26209926/gamma-hydroxybutyrate-enhances-mood-and-prosocial-behavior-without-affecting-plasma-oxytocin-and-testosterone
#10
RANDOMIZED CONTROLLED TRIAL
Oliver G Bosch, Christoph Eisenegger, Jürg Gertsch, Robin von Rotz, Dario Dornbierer, M Salomé Gachet, Markus Heinrichs, Thomas C Wetter, Erich Seifritz, Boris B Quednow
Gamma-hydroxybutyrate (GHB) is a GHB-/GABAB-receptor agonist. Reports from GHB abusers indicate euphoric, prosocial, and empathogenic effects of the drug. We measured the effects of GHB on mood, prosocial behavior, social and non-social cognition and assessed potential underlying neuroendocrine mechanisms. GHB (20mg/kg) was tested in 16 healthy males, using a randomized, placebo-controlled, cross-over design. Subjective effects on mood were assessed by visual-analogue-scales and the GHB-Specific-Questionnaire...
December 2015: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/25861156/recent-advances-in-methamphetamine-neurotoxicity-mechanisms-and-its-molecular-pathophysiology
#11
REVIEW
Shaobin Yu, Ling Zhu, Qiang Shen, Xue Bai, Xuhui Di
Methamphetamine (METH) is a sympathomimetic amine that belongs to phenethylamine and amphetamine class of psychoactive drugs, which are widely abused for their stimulant, euphoric, empathogenic, and hallucinogenic properties. Many of these effects result from acute increases in dopamine and serotonin neurotransmission. Subsequent to these acute effects, METH produces persistent damage to dopamine and serotonin release in nerve terminals, gliosis, and apoptosis. This review summarized the numerous interdependent mechanisms including excessive dopamine, ubiquitin-proteasome system dysfunction, protein nitration, endoplasmic reticulum stress, p53 expression, inflammatory molecular, D3 receptor, microtubule deacetylation, and HIV-1 Tat protein that have been demonstrated to contribute to this damage...
2015: Behavioural Neurology
https://www.readbyqxmd.com/read/25711990/metabolic-fate-mass-spectral-fragmentation-detectability-and-differentiation-in-urine-of-the-benzofuran-designer-drugs-6-apb-and-6-mapb-in-comparison-to-their-5-isomers-using-gc-ms-and-lc-hr-ms-n-techniques
#12
COMPARATIVE STUDY
Jessica Welter, Simon D Brandt, Pierce Kavanagh, Markus R Meyer, Hans H Maurer
The number of so-called new psychoactive substances (NPS) is still increasing by modification of the chemical structure of known (scheduled) drugs. As analogues of amphetamines, 2-aminopropyl-benzofurans were sold. They were consumed because of their euphoric and empathogenic effects. After the 5-(2-aminopropyl)benzofurans, the 6-(2-aminopropyl)benzofuran isomers appeared. Thus, the question arose whether the metabolic fate, the mass spectral fragmentation, and the detectability in urine are comparable or different and how an intake can be differentiated...
May 2015: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/25575620/acute-effects-of-lysergic-acid-diethylamide-in-healthy-subjects
#13
RANDOMIZED CONTROLLED TRIAL
Yasmin Schmid, Florian Enzler, Peter Gasser, Eric Grouzmann, Katrin H Preller, Franz X Vollenweider, Rudolf Brenneisen, Felix Müller, Stefan Borgwardt, Matthias E Liechti
BACKGROUND: After no research in humans for >40 years, there is renewed interest in using lysergic acid diethylamide (LSD) in clinical psychiatric research and practice. There are no modern studies on the subjective and autonomic effects of LSD, and its endocrine effects are unknown. In animals, LSD disrupts prepulse inhibition (PPI) of the acoustic startle response, and patients with schizophrenia exhibit similar impairments in PPI. However, no data are available on the effects of LSD on PPI in humans...
October 15, 2015: Biological Psychiatry
https://www.readbyqxmd.com/read/25471293/benzofuran-analogues-of-amphetamine-and-methamphetamine-studies-on-the-metabolism-and-toxicological-analysis-of-5-apb-and-5-mapb-in-urine-and-plasma-using-gc-ms-and-lc-hr-ms-n-techniques
#14
Jessica Welter, Pierce Kavanagh, Markus R Meyer, Hans H Maurer
5-APB (5-(2-aminopropyl)benzofuran) and its N-methyl derivative 5-MAPB (N-methyl-5-(2-aminopropyl)benzofuran) are analogues of amphetamine and methamphetamine, respectively, and belong to the so-called novel psychoactive substances (NPS). They were consumed as stimulants or entactogens with euphoric and empathogenic effects. Being controlled in some countries, both compounds should be covered by drug testing in clinical and forensic toxicology. Therefore, metabolism studies have been performed by working up rat urine samples after a high single dose of the corresponding NPS with solid-phase extraction without and after enzymatic conjugates cleavage...
February 2015: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/25052243/differential-effects-of-mdma-and-methylphenidate-on-social-cognition
#15
RANDOMIZED CONTROLLED TRIAL
Yasmin Schmid, Cédric M Hysek, Linda D Simmler, Molly J Crockett, Boris B Quednow, Matthias E Liechti
Social cognition is important in everyday-life social interactions. The social cognitive effects of 3,4-methylenedioxymethamphetamine (MDMA, 'ecstasy') and methylphenidate (both used for neuroenhancement and as party drugs) are largely unknown. We investigated the acute effects of MDMA (75 mg), methylphenidate (40 mg) and placebo using the Facial Emotion Recognition Task, Multifaceted Empathy Test, Movie for the Assessment of Social Cognition, Social Value Orientation Test and the Moral Judgment Task in a cross-over study in 30 healthy subjects...
September 2014: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/24862256/5-hydroxytryptamine-and-dopamine-releasing-effects-of-ring-substituted-amphetamines-on-rat-brain-a-comparative-study-using-in-vivo-microdialysis
#16
COMPARATIVE STUDY
T Matsumoto, Y Maeno, H Kato, Y Seko-Nakamura, J Monma-Ohtaki, A Ishiba, M Nagao, Y Aoki
Using in vivo microdialysis, a comparative study was conducted to examine the effects of amphetamine-related compounds (methamphetamine, MAP; 3,4-methylenedioxymethamphetamine, MDMA; p-methoxyamphetamine, PMA; p-methoxymethamphetamine, PMMA; 4-methylthioamphetamine, 4-MTA; 3,4,5-trimethoxyamphetamine, TMA; 2,5-dimethoxy-4-iodoamphetamine, DOI) on extracellular levels of serotonin (5-HT) and dopamine (DA). Dialysates were assayed using HPLC equipped with electrochemical detector following i.p. administration with each drug at a dose of 5 mg/kg...
August 2014: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/24484988/bath-salts-mephedrone-and-methylenedioxypyrovalerone-as-emerging-illicit-drugs-that-will-need-targeted-therapeutic-intervention
#17
REVIEW
Richard A Glennon
The term "synthetic cathinones" is fairly new, but, although the abuse of synthetic cathinones is a recent problem, research on cathinone analogs dates back >100 years. One structural element cathinone analogs have in common is an α-aminophenone moiety. Introduction of amine and/or aryl substituents affords a large number of agents. Today, >40 synthetic cathinones have been identified on the clandestine market and many have multiple "street names." Many cathinone analogs, although not referred to as such until the late 1970s, were initially prepared as intermediates in the synthesis of ephedrine analogs...
2014: Advances in Pharmacology
https://www.readbyqxmd.com/read/24097374/mdma-enhances-emotional-empathy-and-prosocial-behavior
#18
RANDOMIZED CONTROLLED TRIAL
Cédric M Hysek, Yasmin Schmid, Linda D Simmler, Gregor Domes, Markus Heinrichs, Christoph Eisenegger, Katrin H Preller, Boris B Quednow, Matthias E Liechti
3,4-Methylenedioxymethamphetamine (MDMA, 'ecstasy') releases serotonin and norepinephrine. MDMA is reported to produce empathogenic and prosocial feelings. It is unknown whether MDMA in fact alters empathic concern and prosocial behavior. We investigated the acute effects of MDMA using the Multifaceted Empathy Test (MET), dynamic Face Emotion Recognition Task (FERT) and Social Value Orientation (SVO) test. We also assessed effects of MDMA on plasma levels of hormones involved in social behavior using a placebo-controlled, double-blind, random-order, cross-over design in 32 healthy volunteers (16 women)...
November 2014: Social Cognitive and Affective Neuroscience
https://www.readbyqxmd.com/read/23892199/neurotoxicity-of-methamphetamine-and-3-4-methylenedioxymethamphetamine
#19
REVIEW
Laura E Halpin, Stuart A Collins, Bryan K Yamamoto
Amphetamines are a class of psychostimulant drugs that are widely abused for their stimulant, euphoric, empathogenic and hallucinogenic properties. Many of these effects result from acute increases in dopamine and serotonin neurotransmission. Subsequent to these acute effects, methamphetamine and 3,4 methylenedioxymethamphetamine (MDMA) produce persistent damage to dopamine and serotonin nerve terminals. This review summarizes the numerous interdependent mechanisms including excitotoxicity, mitochondrial damage and oxidative stress that have been demonstrated to contribute to this damage...
February 27, 2014: Life Sciences
https://www.readbyqxmd.com/read/23711768/-ecstasy-enhances-noise-induced-hearing-loss
#20
Michael W Church, Jinsheng S Zhang, Megan M Langford, Shane A Perrine
'Ecstasy' or 3,4-methylenedioxy-N-methamphetamine (MDMA) is an amphetamine abused for its euphoric, empathogenic, hallucinatory, and stimulant effects. It is also used to treat certain psychiatric disorders. Common settings for Ecstasy use are nightclubs and "rave" parties where participants consume MDMA and dance to loud music. One concern with the club setting is that exposure to loud sounds can cause permanent sensorineural hearing loss. Another concern is that consumption of MDMA may enhance such hearing loss...
August 2013: Hearing Research
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