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https://www.readbyqxmd.com/read/29204127/synthetic-aminoindanes-a-summary-of-existing-knowledge
#1
REVIEW
Nikola Pinterova, Rachel R Horsley, Tomas Palenicek
Objectives: Aminoindanes ("bath salts," a class of novel psychoactive substances, NPSs) increased rapidly in popularity on the recreational drug market, particularly after mephedrone and other synthetic cathinones were banned in the UK in 2010. Novel aminoindanes continue to emerge, but relatively little is known about their effects and risks. Their history, chemistry, pharmacology, behavioral effects, pharmacokinetics, and toxicity are reviewed in this paper. Methods: Scientific literature was searched on ISI Web of Knowledge: Web of Science (WoS) during June and July 2017, using English language terms: aminoindanes such as 5,6-methylenedioxy-2-aminoindane (MDAI), 5-iodo-2-aminoindane (5-IAI), 2-aminoindane (2-AI), 5,6-methylenedioxy-N-methyl-2-aminoindane (MDMAI), and 5-methoxy-6-methyl-2-aminoindane (MMAI)...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/29204126/pharmacokinetic-ambulatory-and-hyperthermic-effects-of-3-4-methylenedioxy-n-methylcathinone-methylone-in-rats
#2
Kristýna Štefková, Monika Židková, Rachel R Horsley, Nikola Pinterová, Klára Šíchová, Libor Uttl, Marie Balíková, Hynek Danda, Martin Kuchař, Tomáš Páleníček
Methylone (3,4-methylenedioxy-N-methylcathinone) is a synthetic cathinone analog of the recreational drug ecstasy. Although it is marketed to recreational users as relatively safe, fatalities due to hyperthermia, serotonin syndrome, and multi-organ system failure have been reported. Since psychopharmacological data remain scarce, we have focused our research on pharmacokinetics, and on a detailed evaluation of temporal effects of methylone and its metabolite nor-methylone on behavior and body temperature in rats...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/29194549/stability-of-synthetic-cathinones-in-urine
#3
Lindsay Glicksberg, Sarah Kerrigan
In this report, we evaluate the concentration, pH, temperature and analyte-dependent effects on cathinone stability in preserved human urine. A total of 22 synthetic cathinones were evaluated at 100 ng/mL and 1,000 ng/mL in pH 4 and pH 8 urine over 6 months. Specimens were stored at -20°C, 4°C, 20°C and 32°C. The stability of synthetic cathinones was highly dependent on urine pH and storage temperature. Cathinones were considerably more stable in acidic urine (pH 4) at low temperature. In alkaline urine (pH 8) at 32°C, significant losses (>20%) were observed within hours for the majority of drugs...
November 29, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29183686/neurocognitive-dysfunction-following-repeated-binge-like-self-administration-of-the-synthetic-cathinone-3-4-methylenedioxypyrovalerone-mdpv
#4
REVIEW
Kaveish Sewalia, Lucas R Watterson, Alyssa Hryciw, Anna Belloc, J Bryce Ortiz, M Foster Olive
Synthetic cathinones, frequently referred to as "bath salts", have significant abuse potential, and recent evidence suggests that these novel psychoactive substances can also produce cognitive deficits as well as cytotoxic effects. However, most of these latter findings have been obtained either using high concentrations in vitro or following non-contingent high dose administration in vivo. The present study utilized a model of long-term voluntary binge-like self-administration to determine potential detrimental effects of synthetic cathinones on cognitive function and their known underlying neural circuits, collectively referred to as neurocognitive dysfunction...
November 25, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29128711/polysubstance-use-profiles-among-electronic-dance-music-party-attendees-in-new-york-city-and-their-relation-to-use-of-new-psychoactive-substances
#5
Fermín Fernández-Calderón, Charles M Cleland, Joseph J Palamar
BACKGROUND: Electronic Dance Music (EDM) party attendees are often polysubstance users and are at high risk for use of new psychoactive substances (NPS). We sought to identify patterns of use of common illegal drugs among EDM party attendees, sociodemographic correlates, and use of NPS as a function of patterns of use of more common drugs to inform prevention and harm reduction. METHOD: Using time-space-sampling, 1045 individuals aged 18-40 were surveyed entering EDM parties in New York City...
November 4, 2017: Addictive Behaviors
https://www.readbyqxmd.com/read/29078252/analysis-of-new-psychoactive-substances-in-oral-fluids-by-means-of-microextraction-by-packed-sorbent-followed-by-uhplc-ms-ms
#6
Rachele Rocchi, Maria Chiara Simeoni, Camilla Montesano, Gabriele Vannutelli, Roberta Curini, Manuel Sergi, Dario Compagnone
In recent years, new drugs, commonly known as "new psychoactive substances" (NPS), appeared on the market, which include, among others, synthetic cannabinoids, cathinones and tryptamine analogs of psilocin. The aim of this work was to develop and validate a new method for simultaneous screening and quantification of 31 NPS in oral fluid by ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS). The chosen target analytes represented different chemical and toxicological NPS classes, such as synthetic cathinones, piperazines, phenethylamines, synthetic cannabinoids and their metabolites...
October 27, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29042316/concurrent-repeated-exposure-to-3-4-methylenedioxypyrovalerone-and-cocaine-produce-locomotor-sensitization-with-minimal-effects-on-brain-monoamines
#7
REVIEW
Robert J Kohler, Shane A Perrine, Lisa E Baker
Synthetic cathinones, known as "bath salts" on the illicit drug market, pose a significant public health concern. 3,4-Methylenedioxypyrovalerone (MDPV), one of several popular constituents of illicit bath salts, produces similar pharmacological actions to cocaine, albeit with greater potency and efficacy. The present study sought to characterize behavioral and neurochemical effects of repeated exposure to MDPV alone and in combination with cocaine. Male Sprague-Dawley rats were randomly assigned to one the following four treatments, administered once daily for seven days: 1 mg/kg MDPV, 5 mg/kg cocaine, 1 mg/kg MDPV +5 mg/kg cocaine, or saline...
October 14, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29036640/toxicokinetics-of-the-synthetic-cathinone-%C3%AE-pyrrolidinohexanophenone
#8
Yuji Fujita, Toshinori Mita, Kiyotaka Usui, Yoshito Kamijo, Satoshi Kikuchi, Makoto Onodera, Yasuhisa Fujino, Yoshihiro Inoue
Synthetic cathinones inhibit monoamine transporters, such as serotonin, norepinephrine, and dopamine transporters, and act on the central nervous system via increasing synaptic concentrations of monoamines. These compounds, which are highly addictive and potentially poisonous, are new psychoactive substances. In this study, we investigated the toxicokinetics of the synthetic cathinone, α-pyrrolidinohexanophenone (α-PHP), and assessed the relationship between the toxicokinetics and the long-term clinical symptoms induced by α-PHP in a male patient...
September 28, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29031971/solid-phase-extraction-followed-by-liquid-chromatography-high-resolution-mass-spectrometry-to-determine-synthetic-cathinones-in-different-types-of-environmental-water-samples
#9
N Fontanals, R M Marcé, F Borrull
Synthetic cathinones have become popular in recent years, which would explain why their determination in influent sewage samples has already been documented. In the present study a method based on solid-phase extraction followed by liquid chromatography and high resolution mass spectrometry is developed, validated and applied to determine twelve cathinones and one of their metabolites in different environmental samples including influent and effluent sewage and river water. Two cation-exchange sorbents (Oasis MCX and Oasis WCX) were compared, with better results achieved with Oasis WCX in terms of apparent recoveries (70-100%) and matrix effects (lower than -34%)...
October 4, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/29030166/mdpv-and-%C3%AE-pvp-use-in-humans-the-twisted-sisters
#10
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/28985394/a-validated-method-for-the-detection-of-32-bath-salts-in-oral-fluid
#11
Michelle Williams, Jennifer Martin, Peter Galettis
Workplace drug testing in Australia is usually adherent to one of two standards, AS/NZS 4308:2008 for urine or AS 4760:2006 for oral fluid. These standards prescribe the drugs tested, devices used and testing methodology followed by the testing agency. However, they are not comprehensive and for many years workers have been able to consume novel psychoactive substances to avoid detection and without consequences. Here, we present a validated method for the detection of 32 Synthetic Stimulant and Hallucogenic drugs, commonly sold as bath salts, in oral fluid...
July 14, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28977581/stability-of-synthetic-cathinones-in-blood
#12
Lindsay Glicksberg, Sarah Kerrigan
The synthetic cathinones are powerful psychostimulants that have been associated with impairment, intoxication and fatal overdose. Forensic laboratories must be able to identify these new drugs as part of antemortem and postmortem toxicology investigations. Preliminary reports have indicated that some of the synthetic cathinones are unstable in biological matrices. It is important to understand drug stability in biological evidence so that analytical findings can be interpreted appropriately. The objective of this study was to systematically evaluate the concentration, temperature and analyte-dependent stability of synthetic cathinones in preserved blood using liquid-chromatography/quadrupole-time of flight-mass spectrometry (LC/Q-TOF-MS)...
August 31, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28977427/chiral-resolution-and-enantioselectivity-of-synthetic-cathinones-a-brief-review
#13
Bárbara Silva, Carla Fernandes, Paula Guedes de Pinho, Fernando Remião
Chiral discrimination has become one of the most important fields in analytical and medicinal chemistry, and forensic toxicology. The enantiomers may have different binding to proteins that may lead to many pharmacological and toxicological differences between them, including kinetic (at the absorption, distribution, metabolism and excretion level) or dynamic (level of potency and efficacy or even differences in mechanism of action) variations. Cathinone derivatives are chiral compounds, sold via the internet for recreational use, and little is known about their enantiomeric selectivity...
September 6, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28911631/new-psychoactive-substances-of-natural-origin-a%C3%A2-brief-review
#14
REVIEW
Ling-Yi Feng, Altansuvd Battulga, Eunyoung Han, Heesun Chung, Jih-Heng Li
Plant-based drugs of abuse are as old as recorded human history. Although traditional addictive substances, such as opium, cannabis and coca, have been controlled by the United Nations anti-drug conventions, many, if not most, natural plants with addictive or abuse liability remain elusive. Therefore, the United Nations Office on Drugs and Crime (UNODC) has warned the emerging threat from new psychoactive substances (NPS), which are mostly derived or modified from the constituents of natural origin. For example, synthetic cannabinoids and synthetic cathinones are derived from the cannabis and khat plant, respectively...
July 2017: Journal of Food and Drug Analysis
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
#15
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/28904288/alpha-pvp-induces-the-rewarding-effect-via-activating-dopaminergic-neuron
#16
Kyoko Hataoka, Asuka Kaizaki-Mitsumoto, Satoshi Numazawa
A synthetic cathinone, 1-phenyl-2-(1-pyrrolidinyl)-1-pentanone (α-PVP), was occasionally found in the "bath salt" type of designer drugs, as an active ingredient. It has been reported that drivers who consumed α-PVP were in an excited state and incapable of controlling their behavior, causing traffic accidents. Despite its acute excitatory effects, there is no information on the psychological dependency elicited by α-PVP use. The purpose of the present study was to clarify whether the reward pathway is activated with repeated doses of α-PVP in experimental animals...
2017: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/28885007/stereoselective-differences-between-the-reinforcing-and-motivational-effects-of-cathinone-derived-4-methylmethcathinone-mephedrone-in-self-administering-rats
#17
Helene L Philogene-Khalid, Steven J Simmons, Sunil Nayak, Rose M Martorana, Shu H Su, Yohanka Caro, Brona Ranieri, Kathryn DiFurio, Lili Mo, Taylor A Gentile, Ali Murad, Allen B Reitz, John W Muschamp, Scott M Rawls
Mephedrone (4-methylmethcathinone (4-MMC)) (MEPH) is a new psychoactive substance (NPS) of the synthetic cathinone class. MEPH has a chiral center and exists as two enantiomers (R-,S-MEPH), yet stereospecific effects of MEPH have not been extensively investigated in preclinical assays. Because significant behavioral and neurochemical differences can exist between enantiomers, probing effects of stereochemistry on biological activity enables separation of adverse and therapeutic effects. Our prior work showed that R-MEPH, relative to S-MEPH, produced greater locomotor activation, place preference, and facilitation of brain reward thresholds in rodents...
September 22, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28882561/locomotor-and-reinforcing-effects-of-pentedrone-pentylone-and-methylone-in-rats
#18
Mehrak Javadi-Paydar, Jacques D Nguyen, Sophia A Vandewater, Tobin J Dickerson, Michael A Taffe
The broad diversity of synthetic cathinone psychostimulant drugs that are available to users complicates research efforts to provide understanding of health risks. Second generation cathinones pentedrone and pentylone are distinguished from each other by the 3,4-methylenedioxy structural motif (which distinguishes methamphetamine from 3,4-methylenedioxymethamphetamine) and each incorporates the α-alkyl chain motif contained in the transporter-inhibitor cathinones (3,4-methylenedioxypyrovalerone (MDPV), α-pyrrolidinopentiophenone (α-PVP)) but not in the monoamine releasers (mephedrone, methylone)...
September 4, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28878698/synthetic-cathinone-and-cannabinoid-designer-drugs-pose-a-major-risk-for-public-health
#19
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/28868040/novel-psychoactive-substances-recent-progress-on-neuropharmacological-mechanisms-of-action-for-selected-drugs
#20
REVIEW
Zurina Hassan, Oliver G Bosch, Darshan Singh, Suresh Narayanan, B Vicknasingam Kasinather, Erich Seifritz, Johannes Kornhuber, Boris B Quednow, Christian P Müller
A feature of human culture is that we can learn to consume chemical compounds, derived from natural plants or synthetic fabrication, for their psychoactive effects. These drugs change the mental state and/or the behavioral performance of an individual and can be instrumentalized for various purposes. After the emergence of a novel psychoactive substance (NPS) and a period of experimental consumption, personal and medical benefits and harm potential of the NPS can be estimated on evidence base. This may lead to a legal classification of the NPS, which may range from limited medical use, controlled availability up to a complete ban of the drug form publically accepted use...
2017: Frontiers in Psychiatry
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