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Cathinone

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https://www.readbyqxmd.com/read/28646714/synthetic-cathinones-and-stereochemistry-s-enantiomer-of-mephedrone-reduces-anxiety-and-depressant-like-effects-in-cocaine-or-mdpv-abstinent-rats
#1
Helene L Philogene-Khalid, Callum Hicks, Allen B Reitz, Lee-Yuan Liu-Chen, Scott M Rawls
BACKGROUND AND PURPOSE: The neuropharmacological profile of the synthetic cathinone mephedrone (MEPH) is influenced by stereochemistry. Both MEPH enantiomers are monoamine transporter substrates, but R-MEPH is primarily responsible for rewarding effects of MEPH as it produces greater locomotor activation and intracranial self-stimulation than S-MEPH. S-MEPH is a 50-fold more potent 5-HT releaser than R-MEPH and does not place preference in rats. MEPH is also structurally similar to the cathinone derivative bupropion, an antidepressant and smoking cessation medication, suggesting MEPH has therapeutic and addictive properties...
June 13, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28646469/the-cathinones-mdpv-and-%C3%AE-pvp-elicit-different-behavioral-and-molecular-effects-following-acute-exposure
#2
Giuseppe Giannotti, Isabella Canazza, Lucia Caffino, Sabrine Bilel, Andrea Ossato, Fabio Fumagalli, Matteo Marti
Since the mid-to-late 2000s, synthetic cathinones have gained popularity among drug users due to their psychostimulant effects greater than those produced by cocaine and amphetamine. Among them, 3,4-methylenedioxypyrovalerone (MDPV) and 1-phenyl-2-(pyrrolidin-1-yl)pentan-1-one (α-PVP) are ones of the most popular cathinones available in the clandestine market as "bath salts" or "fertilizers." Pre-clinical studies indicate that MDPV and α-PVP induced psychomotor stimulation, affected thermoregulation, and promoted reinforcing properties in rodents...
June 23, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28645576/mechanisms-of-hepatocellular-toxicity-associated-with-new-psychoactive-synthetic-cathinones
#3
Dino Luethi, Matthias E Liechti, Stephan Krähenbühl
Synthetic cathinones are a new class of psychostimulant substances. Rarely, they can cause liver injury but associated mechanisms are not completely elucidated. In order to increase our knowledge about mechanisms of hepatotoxicity, we investigated the effect of five frequently used cathinones on two human cell lines. Bupropion was included as structurally related drug used therapeutically. In HepG2 cells, bupropion, MDPV, mephedrone and naphyrone depleted the cellular ATP content at lower concentrations (0...
June 20, 2017: Toxicology
https://www.readbyqxmd.com/read/28631432/profile-effects-and-toxicity-of-novel-psychoactive-substances-a-systematic-review-of-quantitative-studies
#4
Sulaf Assi, Nargilya Gulyamova, Kinda Ibrahim, Paul Kneller, David Osselton
OBJECTIVE: To investigate the profile, effects, and toxicity of novel psychoactive substances (NPS). METHODS: A systematic literature review was conducted between May 2015 and February 2016 and included 19 databases. Search terms included "novel psychoactive substance(s)," "effect(s)," and "toxicity" and their synonyms. Studies included were those from any country, in any language, and between January 2007 and April 2015. Studies published before 2007 and those regarding the synthesis of NPS were excluded...
June 19, 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28631397/the-effects-and-toxicity-of-cathinones-from-the-users-perspectives-a-qualitative-study
#5
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...
June 20, 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28628897/diverted-medications-and-new-psychoactive-substances-a-chemical-network-analysis-of-discarded-injecting-paraphernalia-in-hungary
#6
Valéria Anna Gyarmathy, Anna Péterfi, Tamás Figeczki, József Kiss, Katalin Medgyesi-Frank, János Posta, József Csorba
BACKGROUND: Until about 2010, people who inject drugs (PWIDs) injected almost exclusively heroin and amphetamines in Hungary. After 2010, self-reported studies have indicated a dominance of new psychoactive substances on the drug market for injectable drugs. METHODS: Between March 2015 and February 2016, we collected used and discarded injecting paraphernalia. We utilized chemical analysis to assess and UCINet to visualize the connections between the most prevalent main substances and their respective co-occurring additional components at 7 locations in Hungary...
June 16, 2017: International Journal on Drug Policy
https://www.readbyqxmd.com/read/28618002/novel-psychoactive-substance-use-among-treatment-seeking-opiate-users-the-role-of-life-events-and-psychiatric-symptoms
#7
Máté Kapitány-Fövény, Judit Farkas, Patrícia Andrea Pataki, Anna Kiss, Janka Horváth, Róbert Urbán, Zsolt Demetrovics
OBJECTIVE: Over the past 5 years, a shift to the use of novel psychoactive substances (NPS) has been observed among opioid users. The aim of this study was to assess the potential reasons for NPS use among treatment-seeking patients receiving opiate substitution therapy. METHOD: A structured questionnaire was filled out by a sample of 198 opiate dependent patients of Hungary's National Institute of Psychiatry and Addiction. This questionnaire assessed demographics, treatment characteristics, lifetime substance use, potential reasons for NPS use, negative life events (Life Events Scale), and psychiatric symptoms (Brief Symptom Inventory)...
June 15, 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28617997/a-market-on-both-sides-of-the-law-the-use-of-the-hidden-web-for-the-sale-of-new-psychoactive-substances
#8
Elle Wadsworth, Colin Drummond, Andreas Kimergård, Paolo Deluca
OBJECTIVE: The hidden Web is used for the anonymous sale of drugs, and with the UK Psychoactive Substances Act, 2016, implemented on May 26th 2016; it could increase as a platform for obtaining new psychoactive substances (NPS). This study aims to describe the NPS market on the visible and hidden Web preban, and assess whether the hidden Web is a likely place for the sale of NPS postban. METHODS: Data collection of 113 online shops took place in October 2015. Data collection of 22 cryptomarkets took place every 2 months from October 2015 to 2016 as part of the CASSANDRA project...
June 15, 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28602505/proposal-of-5-methoxy-n-methyl-n-isopropyltryptamine-consumption-biomarkers-through-identification-of-in-vivo-metabolites-from-mice
#9
D Fabregat-Safont, M Barneo-Muñoz, F Martinez-Garcia, J V Sancho, F Hernández, M Ibáñez
New psychoactive substances (NPS) are a new breed of synthetically produced substances designed to mimic the effects of traditional illegal drugs. Synthetic cannabinoids and synthetic cathinones are the two most common groups, which try to mimic the effects of the natural compounds (9)Δ-tetrahydrocannabinol and cathinone, respectively. Similarly, synthetic tryptamines are designer compounds which are based on the compounds psilocin, N,N-dimethyltryptamine and 5-methoxy-N,N-dimethyltryptamine found in some mushrooms...
June 5, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28578026/%C3%AE-pyrrolidinononanophenone-provokes-apoptosis-of-neuronal-cells-through-alterations-in-antioxidant-properties
#10
Toshiyuki Matsunaga, Yoshifumi Morikawa, Kyohei Kamata, Akinobu Shibata, Hidetoshi Miyazono, Yasuhide Sasajima, Koichi Suenami, Kiyohito Sato, Yuji Takekoshi, Satoshi Endo, Ossama El-Kabbani, Akira Ikari
In this study, we found that exposure to α-pyrrolidinononanophenone (α-PNP), a highly lipophilic synthetic cathinone, provokes apoptosis of human neuronal SK-N-SH cells. The drug sensitivity of the cells (50% lethal concentration of 12μM) was similar to those of aortic endothelial and smooth muscle cells, and was higher than those of cells derived from colon, liver, lung and kidney, suggesting that α-PNP overdose and abuse cause serious damage in central nervous and vascular systems. SK-N-SH cell treatment with lethal concentrations (20 and 50μM) of α-PNP facilitated the reactive oxygen species (ROS) production...
May 31, 2017: Toxicology
https://www.readbyqxmd.com/read/28570297/reinforcing-effects-of-abused-bath-salts-constituents-3-4-methylenedioxypyrovalerone-and-%C3%AE-pyrrolidinopentiophenone-and-their-enantiomers
#11
Brenda M Gannon, Kenner C Rice, Gregory T Collins
Synthetic cathinones found in abused 'bath salts' preparations are chiral molecules. Racemic 3,4-methylenedioxypyrovalerone (MDPV) and α-pyrrolidinopentiophenone (α-PVP) are two common constituents of these preparations that have been reported to be highly effective reinforcers; however, the relative contribution of each enantiomer toward these effects has not been determined. Thus, male Sprague-Dawley rats were trained to respond for racemic MDPV or α-PVP (n=9/drug), with full dose-response curves for the racemate and the S and R enantiomers of MDPV and α-PVP generated under a progressive ratio schedule of reinforcement...
May 31, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28544816/analytical-characterization-of-three-cathinone-derivatives-4-mpd-4%C3%A2-f-php-and-bk-epdp-purchased-as-bulk-powder-from-online-vendors
#12
Orapan Apirakkan, Anca Frinculescu, Trevor Shine, Mark C Parkin, Agostino Cilibrizzi, Nunzianda Frascione, Vincenzo Abbate
Novel emerging drugs of abuse, also referred as new psychoactive substances (NPS), constitute an ever-changing mixture of chemical compounds designed to circumvent legislative controls by means of chemical modifications of previously banned recreational drugs. One of such class, synthetic cathinones, namely β-keto derivatives of amphetamines, has been largely abused over the past decade. A number of new synthetic cathinones are detected each year, either in bulk powders/crystals or in biological matrices. It is therefore important to continuously monitor the supply of new synthetic derivatives and promptly report them...
May 23, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28544602/drug-residues-in-syringes-and-other-injecting-paraphernalia-in-hungary
#13
Anna Péterfi, József Csorba, Tamás Figeczki, József Kiss, Katalin Medgyesi-Frank, János Posta, V Anna Gyarmathy
The appearance and spread of new psychoactive substances (NPS) is a phenomenon detected throughout Europe since 2008. Synthetic cathinones, a group of NPS, have been self-reported as the drug injected by the vast majority of people who inject drugs (PWID) in Hungary. This study aims at updating our knowledge on what exactly the compounds injected by PWID. This multi-site study analysed residues from used injecting drug paraphernalia collected from PWID via low threshold services and from public places in Budapest, Debrecen, Miskolc, Szeged, Békéscsaba and Pécs between March 2015 and February 2016...
May 23, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28541461/screening-with-quantification-for-64-drugs-and-metabolites-in-human-urine-using-uplc-ms-ms-analysis-and-a-threshold-accurate-calibration
#14
Thomas G Rosano, Patrice Y Ohouo, Michelle Wood
Drug and metabolite (analytes) identification together with quantification is an important analytical tool in forensic and clinical toxicology. We report the development and validation of a definitive detection and quantification method (UPLC-MS-MS) for initial screening of 64 analytes in urine. The principle of the method is a quantitative extension of a recently reported threshold accurate calibration (TAC) technique which employs a rapid dual-specimen analysis i.e., with and without addition of a reference-analyte standard for normalization of matrix effects...
May 24, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28529142/gender-differences-in-the-effects-of-cathinone-and-the-interaction-with-caffeine-on-temperature-and-locomotor-activity-in-the-rat
#15
Hadeel A Alsufyani, James R Docherty
We have investigated gender differences in the effects of cathinone and the interaction with caffeine on temperature and movement activity in Wistar rats. Telemetry probes were implanted in rats under isoflurane anaesthesia, and 7 days later, temperature and activity were recorded in conscious unrestrained animals. Caffeine (10mg/lkg) or vehicle, and 30min later, cathinone (5mg/kg) or vehicle, were injected subcutaneously. Cathinone produced significant and marked increases in activity, and the response to cathinone was significantly greater in female animals...
May 18, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28527032/methylone-and-mdpv-activate-autophagy-in-human-dopaminergic-sh-sy5y-cells-a-new-insight-into-the-context-of-%C3%AE-keto-amphetamines-related-neurotoxicity
#16
Maria João Valente, Cristina Amaral, Georgina Correia-da-Silva, José Alberto Duarte, Maria de Lourdes Bastos, Félix Carvalho, Paula Guedes de Pinho, Márcia Carvalho
Autophagy has an essential role in neuronal homeostasis and its dysregulation has been recently linked to neurotoxic effects of a growing list of psychoactive drugs, including amphetamines. However, the role of autophagy in β-keto amphetamine (β-KA) designer drugs-induced neurotoxicity has hitherto not been investigated. In the present study, we show that two commonly abused cathinone derivatives, 3,4-methylenedioxymethcathinone (methylone) and 3,4-methylenedioxypyrovalerone (MDPV), elicit morphological changes consistent with autophagy and neurodegeneration, including formation of autophagic vacuoles and neurite retraction in dopaminergic SH-SY5Y cells...
May 19, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/28506835/impact-of-common-clandestine-structural-modifications-on-synthetic-cathinone-bath-salt-pharmacokinetics
#17
Gregory G Grecco, David F Kisor, Joseph S Magura, Jon E Sprague
Since 2009, the synthetic cathinones ("bath salts") have risen in popularity as drugs of abuse. However, there are a paucity of studies that have determined the impact of functional group modifications in the synthetic cathinone chemical structures on plasma and central nervous system (CNS) pharmacokinetics. In the present study, we investigated the in vivo plasma and CNS pharmacokinetics of three synthetic cathinones whose structures differ by lengthening of the α-alkyl chain: methylone (-CH3), butylone (-CH2CH3), and pentylone (-CH2CH2CH3)...
August 1, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28485987/assessing-self-reported-use-of-new-psychoactive-substances-the-impact-of-gate-questions
#18
Joseph J Palamar, Patricia Acosta, Fermín Fernández Calderón, Scott Sherman, Charles M Cleland
BACKGROUND: New psychoactive substances (NPS) continue to emerge; however, few surveys of substance use ask about NPS use. Research is needed to determine how to most effectively query use of NPS and other uncommon drugs. OBJECTIVE: To determine whether prevalence of self-reported lifetime and past-year use differs depending on whether or not queries about NPS use are preceded by "gate questions." Gate questions utilize skip-logic, such that only a "yes" response to the use of specific drug class is followed by more extensive queries of drug use in that drug class...
May 9, 2017: American Journal of Drug and Alcohol Abuse
https://www.readbyqxmd.com/read/28472731/online-test-purchased-new-psychoactive-substances-in-5-different-european-countries-a-snapshot-study-of-chemical-composition-and-price
#19
Tibor Markus Brunt, Amanda Marie Atkinson, Thomas Nefau, Magali Martinez, Emmanuel Lahaie, Artur Malzcewski, Martin Pazitny, Vendula Belackova, Simon D Brandt
BACKGROUND: New psychoactive substances (NPS) are on offer worldwide online, in order to shed light on the purity and price of these substances in the European Union, a research collaboration was set up involving France, United Kingdom (UK), the Netherlands, Czech Republic and Poland. METHODS: Per country, around 10 different NPS were test purchased from different webshops. Then, chemical analysis of NPS was done with according reference standards to identify and quantify the contents...
May 1, 2017: International Journal on Drug Policy
https://www.readbyqxmd.com/read/28445860/brephedrone-a-new-psychoactive-substance-seized-in-brazil
#20
Yuri Machado, José Coelho Neto, Paulo Eduardo Nunes Barbosa, Rogério Araújo Lordeiro, Rosemeire Brondi Alves
At the beginning of 2015, sixty-two capsules containing red-brown crystals seized in a historical city in Brazil were sent to this forensic laboratory for drug testing analysis. The material was identified as being Brephedrone, a new psychoactive substance and a bromine synthetic cathinone that is related to serotonin transportation. This substance was analyzed by ATR-FTIR, GC-MS, LC-MS, (1)H, (13)C and 2D NMR. Brephedrone apprehensions have been previously reported in Finland, France and Spain. It was the first detection of this substance in the State of Minas Gerais...
April 15, 2017: Forensic Science International
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