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Novel Amphetamine

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https://www.readbyqxmd.com/read/29030166/mdpv-and-%C3%AE-pvp-use-in-humans-the-twisted-sisters
#1
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/28985320/multiple-drug-toxicity-involving-novel-psychoactive-substances-3-fluorophenmetrazine-and-u-47700
#2
Kayla N Ellefsen, Elizabeth A Taylor, Paul Simmons, Vickie Willoughby, Brad J Hall
3-Fluorophenmetrazine (3-FPM) is a stimulant-like novel psychoactive substance (NPS) and fluorinated analog of phenmetrazine that has recently appeared on the recreational drug market, with limited published information. Likewise, the synthetic opioid U-47700 has gained popularity among recreational drug users and is frequently detected in postmortem casework. We present the case history, autopsy and toxicological findings of a fatality involving the designer drugs 3-FPM and U-47700 for the first time in the literature...
July 20, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28950240/prevalence-and-motivations-for-kratom-use-in-a-sample-of-substance-users-enrolled-in-a-residential-treatment-program
#3
Kirsten Elin Smith, Thomas Lawson
BACKGROUND: Kratom use in the West has increased recently, yet the prevalence and motives for use among individuals with a history of substance use disorder (SUD) have not been fully examined. Kratom has been documented as a means of treating chronic pain, mitigating drug dependence, and easing withdrawal symptoms, yet it is unclear if substance users are utilizing kratom as a self-medication. Abuse liability, side effects, and overall appeal of kratom remain uncertain. METHODS: In April 2017, an anonymous survey regarding kratom use and motivations was completed by clients enrolled in a 12-Step-oriented residential program...
September 20, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28910664/the-analysis-of-132-novel-psychoactive-substances-in-human-hair-using-a-single-step-extraction-by-tandem-lc-ms
#4
Vassiliki A Boumba, Matthew Di Rago, Melissa Peka, Olaf H Drummer, Dimitri Gerostamoulos
A rapid LC-MS/MS method for the targeted screening of 132 NPS in hair is described. Drugs include cathinones and synthetic cannabinoids, as well as amphetamine-type stimulants, piperazines and other hallucinogenic compounds. This method utilizes hair pulverization in acidified methanol followed by analysis using liquid chromatography coupled with tandem MS. The limit of detection varied from 0.001 to 0.1ng/mg hair among the various analytes. The method was validated in terms of sensitivity, selectivity, repeatability and stability...
October 2017: Forensic Science International
https://www.readbyqxmd.com/read/28894302/g%C3%AE-%C3%AE-subunit-activation-promotes-dopamine-efflux-through-the-dopamine-transporter
#5
J Garcia-Olivares, T Baust, S Harris, P Hamilton, A Galli, S G Amara, G E Torres
The dopamine transporter (DAT) is an important regulator of brain dopamine (DA) homeostasis, controlling the intensity and duration of DA signaling. DAT is the target for psychostimulants-like cocaine and amphetamine-and plays an important role in neuropsychiatric disorders, including attention-deficit hyperactivity disorder and drug addiction. Thus, a thorough understanding of the mechanisms that regulate DAT function is necessary for the development of clinical interventions to treat DA-related brain disorders...
September 12, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28889212/cocaine-like-discriminative-stimulus-effects-of-norepinephrine-preferring-monoamine-releasers-time-course-and-interaction-studies-in-rhesus-monkeys
#6
Stephen J Kohut, David S Jacobs, Richard B Rothman, John S Partilla, Jack Bergman, Bruce E Blough
RATIONALE: The therapeutic potential of monoamine releasers with prominent dopaminergic effects is hindered by their high abuse liability. OBJECTIVES: The present study examined the effects of several novel "norepinephrine (NE)-preferring" monoamine releasers relative to non-selective monoamine releasers, d-amphetamine and d-methamphetamine, in rhesus monkeys trained to discriminate cocaine. NE-preferring releasers were approximately 13-fold more potent for NE compared to dopamine release and ranged in potency for serotonin release (PAL-329 < l-methamphetamine < PAL-169)...
September 9, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28879579/novel-selectivity-based-forensic-toxicological-validation-of-a-paper-spray-mass-spectrometry-method-for-the-quantitative-determination-of-eight-amphetamines-in-whole-blood
#7
Sebastiaan F Teunissen, Patrick W Fedick, Bjorn J A Berendsen, Michel W F Nielen, Marcos N Eberlin, R Graham Cooks, Arian C van Asten
Paper spray tandem mass spectrometry is used to identify and quantify eight individual amphetamines in whole blood in 1.3 min. The method has been optimized and fully validated according to forensic toxicology guidelines, for the quantification of amphetamine, methamphetamine, 3,4-methylenedioxyamphetamine (MDA), 3,4-methylenedioxy-N-methylamphetamine (MDMA), 3,4-methylenedioxy-N-ethylamphetamine (MDEA), para-methoxyamphetamine (PMA), para-methoxymethamphetamine (PMMA), and 4-fluoroamphetamine (4-FA). Additionally, a new concept of intrinsic and application-based selectivity is discussed, featuring increased confidence in the power to discriminate the amphetamines from other chemically similar compounds when applying an ambient mass spectrometric method without chromatographic separation...
September 6, 2017: Journal of the American Society for Mass Spectrometry
https://www.readbyqxmd.com/read/28878698/synthetic-cathinone-and-cannabinoid-designer-drugs-pose-a-major-risk-for-public-health
#8
REVIEW
Aviv M Weinstein, Paola Rosca, Liana Fattore, Edythe D London
As part of an increasing worldwide use of designer drugs, recent use of compounds containing cathinones and synthetic cannabinoids is especially prevalent. Here, we reviewed current literature on the prevalence, epidemiology, bio-behavioral effects, and detection of these compounds. Gender differences and clinical effects will also be examined. Chronic use of synthetic cathinone compounds can have major effects on the central nervous system and can induce acute psychosis, hypomania, paranoid ideation, and delusions, similar to the effects of other better-known amphetamine-type stimulants...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/28865391/discriminative-stimulus-and-locomotor-effects-of-para-substituted-and-benzofuran-analogs-of-amphetamine
#9
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
https://www.readbyqxmd.com/read/28862809/novel-luciferase-opsin-combinations-for-improved-luminopsins
#10
Sung Young Park, Sang-Ho Song, Brandon Palmateer, Akash Pal, Eric D Petersen, Gabrielle P Shall, Ryan M Welchko, Keiji Ibata, Atsushi Miyawaki, George J Augustine, Ute Hochgeschwender
Previous work has demonstrated that fusion of a luciferase to an opsin, to create a luminescent opsin or luminopsin, provides a genetically encoded means of manipulating neuronal activity via both chemogenetic and optogenetic approaches. Here we have expanded and refined the versatility of luminopsin tools by fusing an alternative luciferase variant with high light emission, Gaussia luciferase mutant GLucM23, to depolarizing and hyperpolarizing channelrhodopsins with increased light sensitivity. The combination of GLucM23 with Volvox channelrhodopsin-1 produced LMO4, while combining GLucM23 with the anion channelrhodopsin iChloC yielded iLMO4...
September 1, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28857068/anti-manic-efficacy-of-a-novel-kv3-potassium-channel-modulator
#11
Puja K Parekh, Michelle M Sidor, Andrea Gillman, Darius Becker-Krail, Letizia Bettelini, Roberto Arban, Giuseppe S Alvaro, Erika Zambello, Chiara Mutinelli, Yanhua Huang, Charles H Large, Colleen A McClung
Kv3.1 and Kv3.2 voltage-gated potassium channels are expressed on parvalbumin-positive GABAergic interneurons in corticolimbic brain regions and contribute to high frequency neural firing. The channels are also expressed on GABAergic neurons of the basal ganglia, substantia nigra, and ventral tegmental area (VTA) where they regulate firing patterns critical for movement control, reward, and motivation. Modulation of Kv3.1 and Kv3.2 channels may therefore have potential in the treatment of disorders in which these systems have been implicated, such as bipolar disorder...
August 31, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28855876/the-non-peptide-arginine-vasopressin-v1a-selective-receptor-antagonist-sr49059-blocks-the-rewarding-prosocial-and-anxiolytic-effects-of-3-4-methylenedioxymethamphetamine-and-its-derivatives-in-zebra-fish
#12
Luisa Ponzoni, Daniela Braida, Gianpietro Bondiolotti, Mariaelvina Sala
3,4-Methylenedioxymethamphetamine (MDMA) and its derivatives, 2,5-dimethoxy-4-bromo-amphetamine hydrobromide (DOB) and para-methoxyamphetamine (PMA), are recreational drugs whose pharmacological effects have recently been attributed to serotonin 5HT2A/C receptors. However, there is growing evidence that the oxytocin (OT)/vasopressin system can modulate some the effects of MDMA. In this study, MDMA (2.5-10 mg/kg), DOB (0.5 mg/kg), or PMA (0.005, 0.1, or 0.25 mg/kg) were administered intramuscularly to adult zebra fish, alone or in combination with the V1a vasopressin antagonist, SR49059 (0...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/28755886/pharmacological-profile-of-mephedrone-analogs-and-related-new-psychoactive-substances
#13
REVIEW
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
https://www.readbyqxmd.com/read/28713291/an-expanding-world-of-novel-psychoactive-substances-opioids
#14
REVIEW
Jolanta B Zawilska
The abuse of novel psychoactive substances (NPS) has been increasing dramatically worldwide since late 2000s. By the end of 2015, more than 560 NPS had been reported to the European Monitoring Centre for Drugs and Drug Addiction. Although the most popular compounds are synthetic cannabinoids and psychostimulatory derivatives of cathinone (so-called β-keto-amphetamines), novel synthetic opioids have recently emerged on the recreational drug market. They include fentanyl (a potent narcotic analgesic) and its analogs (e...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/28695243/cns-metabolism-in-high-risk-drug-abuse-insights-gained-from-1-h-31-p-mrs-and-pet
#15
REVIEW
S Bodea
BACKGROUND: High-risk drug consumption is a matter of great concern for public health actors in industrialised countries. The latest trends show a market tendency towards diversification and increasing demand for high-purity synthetic drugs. While most consumers seek medical help after cannabis use, it is high-risk drugs like cocaine, heroin and amphetamines that account for most of the 1000 drug-related deaths that occur in Germany every year. PURPOSE: This article presents the most prominent in vivo cerebral metabolic information in cocaine, heroin and methamphetamine users provided by MRI spectroscopy and PET imaging...
July 10, 2017: Der Radiologe
https://www.readbyqxmd.com/read/28657744/discovery-of-n-substituted-2-phenylcyclopropyl-methylamines-as-functionally-selective-serotonin-2c-receptor-agonists-for-potential-use-as-antipsychotic-medications
#16
Guiping Zhang, Jianjun Cheng, John D McCorvy, Paul J Lorello, Barbara J Caldarone, Bryan L Roth, Alan P Kozikowski
A series of N-substituted (2-phenylcyclopropyl)methylamines were designed and synthesized, with the aim of finding serotonin 2C (5-HT2C)-selective agonists with a preference for Gq signaling. A number of these compounds exhibit 5-HT2C selectivity with a preference for Gq-mediated signaling compared with β-arrestin recruitment. Furthermore, the N-methyl compound (+)-15a, which displayed an EC50 of 23 nM in the calcium flux assay while showing no β-arrestin recruitment activity, is the most functionally selective 5-HT2C agonist reported to date...
July 27, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28647359/mild-hypothermia-ameliorates-muscle-wasting-in-septic-rats-associated-with-hypothalamic-ampk-induced-autophagy-and-neuropeptides
#17
Chun Cao, Tao Gao, Minhua Cheng, Fengchan Xi, Chenyan Zhao, Wenkui Yu
Sepsis, always developing muscle wasting, contributes to serious complications and mortality. Mild hypothermia has been reported to have protective effects on the prognosis of septic patients. However, the underlying mechanisms remain unclear. We therefore hypothesized that mild hypothermia could ameliorate muscle wasting during sepsis and whether it was associated with hypothalamus AMPK-induced autophagy and neuropeptides. Adult male Sprague-Dawley rats were intraperitoneally injected with lipopolysaccharide (LPS) (5 mg/kg) or saline...
August 26, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28634445/antioxidant-treatment-with-n-acetyl-cysteine-prevents-the-development-of-cognitive-and-social-behavioral-deficits-that-result-from-perinatal-ketamine-treatment
#18
Aarron Phensy, Hasmik E Duzdabanian, Samantha Brewer, Anurag Panjabi, Christopher Driskill, Annuska Berz, George Peng, Sven Kroener
Alterations of the normal redox state can be found in all stages of schizophrenia, suggesting a key role for oxidative stress in the etiology and maintenance of the disease. Pharmacological blockade of N-methyl-D-aspartic acid (NMDA) receptors can disrupt natural antioxidant defense systems and induce schizophrenia-like behaviors in animals and healthy human subjects. Perinatal administration of the NMDA receptor (NMDAR) antagonist ketamine produces persistent behavioral deficits in adult mice which mimic a range of positive, negative, and cognitive symptoms that characterize schizophrenia...
2017: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/28623171/broad-analgesic-activity-of-a-novel-selective-m1-agonist
#19
Michael W Wood, Giovanni Martino, Martin Coupal, Mattias Lindberg, Patricia Schroeder, Vijayaratnam Santhakumar, Manon Valiquette, Johan Sandin, Daniel Widzowski, Jennifer Laird
Although the muscarinic receptor family has long been a source of potentially compelling targets for small molecule drug discovery, it was difficult to achieve agonist selectivity within the family. A new class of M1 muscarinic agonists has emerged, and these compounds have been characterized as agonists that activate the receptor at an allosteric site. Members of this class of M1 agonists have been shown to be selective across the muscarinic receptors. However, upon introduction of a novel pharmacologic mechanism, it is prudent to ensure that no new off-target activities have arisen, particularly within the context of in vivo experiments...
June 13, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28618002/novel-psychoactive-substance-use-among-treatment-seeking-opiate-users-the-role-of-life-events-and-psychiatric-symptoms
#20
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)...
May 2017: Human Psychopharmacology
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