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https://www.readbyqxmd.com/read/29216482/enantiomeric-profiling-of-chiral-illicit-drugs-in-a-pan-european-study
#1
Erika Castrignanò, Zhugen Yang, Richard Bade, Jose A Baz-Lomba, Sara Castiglioni, Ana Causanilles, Adrian Covaci, Emma Gracia-Lor, Felix Hernandez, Juliet Kinyua, Ann-Kathrin McCall, Alexander L N van Nuijs, Christoph Ort, Benedek G Plósz, Pedram Ramin, Nikolaos I Rousis, Yeonsuk Ryu, Kevin V Thomas, Pim de Voogt, Ettore Zuccato, Barbara Kasprzyk-Hordern
The aim of this paper is to present the first study on spatial and temporal variation in the enantiomeric profile of chiral drugs in eight European cities. Wastewater-based epidemiology (WBE) and enantioselective analysis were combined to evaluate trends in illicit drug use in the context of their consumption vs direct disposal as well as their synthetic production routes. Spatial variations in amphetamine loads were observed with higher use in Northern European cities. Enantioselective analysis showed a general enrichment of amphetamine with the R-(-)-enantiomer in wastewater indicating its abuse...
December 1, 2017: Water Research
https://www.readbyqxmd.com/read/29204127/synthetic-aminoindanes-a-summary-of-existing-knowledge
#2
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/29149685/simultaneous-drug-identification-in-urine-of-sexual-assault-victims-by-using-liquid-chromatography-tandem-mass-spectrometry
#3
Hei Hwa Lee, Suen Chi Chen, Jong Feng Lee, Hsin Yu Lin, Bai Hsiun Chen
According to domestic and international epidemiological investigation, the proportion of substance involved sexual assault has the trend of ascent. In the past, laboratory methods that investigated urine sample of the sexual assault victims was to screen with enzyme immunoassay and then confirmed with mass spectrometry. The objective of the study is to simultaneously identify abused drugs in 126 decoded urine samples of sexual assault victims by liquid chromatography tandem mass spectrometry. The instrument was operated in multiple-reaction monitoring with an electro-spray positive ionization mode...
November 11, 2017: Forensic Science International
https://www.readbyqxmd.com/read/29119924/deaths-in-the-lesbian-gay-bisexual-and-transgender-united-kingdom-communities-associated-with-ghb-and-precursors
#4
John M Corkery, Barbara Loi, Hugh Claridge, Christine Goodair, Fabrizio Schifano
Background Misuse of gammahydroxybutrate (GHB) and its prodrugs gammabutyrolactone (GBL) and 1,4 butanediol (1,4-BD) has increased greatly since the early 1990s, particularly amongst lesbian, gay, bisexual and transgender (LGBT) individuals in recreational and sexual settings, e.g. 'chemsex'. Objective and method This paper presents an overview of GHB pharmacotoxicology and provides analyses of cases in the LGBT population associated with use of these substances extracted from the UK's National Programme on Substance Abuse Deaths database, to which notification is voluntary...
November 8, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/29105555/toxicity-of-new-synthetic-amphetamine-drug-mephedrone-on-rat-heart-mitochondria-a-warning-for-its-abuse
#5
Parvaneh Naserzadeh, Farzaneh Jokar, Farzaneh Vafaei, Enayatollah Seydi, Jalal Pourahmad
1. Mephedrone, a new and popular amphetamine drug, is widely abused and is still legal in some parts around the world. Little data on mechanisms involved in mephedrone induced cardiotoxicity are available. 2. Therefore, we decided to explain the mechanisms of mephedrone cardiotoxicity by using mitochondria isolated from rat heart. The isolated heart mitochondria were incubated with different concentrations of mephedrone (5, 10 and 20 µM). 3. Results showed that mephedrone induced mitochondrial dysfunction via an increase in mitochondrial reactive oxygen species (ROS) production, MMP collapse, mitochondrial swelling and damage in the mitochondrial outer membrane (MOM) which is associated with the cytochrome c release...
November 6, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29097766/a-new-approach-towards-biomarker-selection-in-estimation-of-human-exposure-to-chiral-chemicals-a-case-study-of-mephedrone
#6
Erika Castrignanò, Marie Mardal, Axel Rydevik, Bram Miserez, John Ramsey, Trevor Shine, G Dan Pantoș, Markus R Meyer, Barbara Kasprzyk-Hordern
Wastewater-based epidemiology is an innovative approach to estimate public health status using biomarker analysis in wastewater. A new compound detected in wastewater can be a potential biomarker of an emerging trend in public health. However, it is currently difficult to select new biomarkers mainly due to limited human metabolism data. This manuscript presents a new framework, which enables the identification and selection of new biomarkers of human exposure to drugs with scarce or unknown human metabolism data...
November 2, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29097307/effect-fingerprinting-of-new-psychoactive-substances-nps-what-can-we-learn-from-in-vitro-data
#7
REVIEW
Laura Hondebrink, Anne Zwartsen, Remco H S Westerink
The use of new psychoactive substances (NPS) is increasing and currently >600 NPS have been reported. However, limited information on neuropharmacological and toxicological effects of NPS is available, hampering risk characterization. We reviewed the literature on the in vitro neuronal modes of action to obtain effect fingerprints of different classes of illicit drugs and NPS. The most frequently reported NPS were selected for review: cathinones (MDPV, α-PVP, mephedrone, 4-MEC, pentedrone, methylone), cannabinoids (JWH-018), (hallucinogenic) phenethylamines (4-fluoroamphetamine, benzofurans (5-APB, 6-APB), 2C-B, NBOMes (25B-NBOMe, 25C-NBOMe, 25I-NBOMe)), arylcyclohexylamines (methoxetamine) and piperazine derivatives (mCCP, TFMPP, BZP)...
October 30, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29042260/pldt-planarian-light-dark-test-an-invertebrate-assay-to-quantify-defensive-responding-and-study-anxiety-like-effects
#8
Ashenafi Mebratu Zewde, Frances Yu, Sunil Nayak, Christopher Tallarida, Allen B Reitz, Lynn G Kirby, Scott M Rawls
BACKGROUND: Planarians, like rodents, instinctively spend more time in dark versus light environments when given a choice. This behavioral phenomenon is called negative phototaxis, which may reflect defensive responding related to an anxiety-like phenotype. NEW METHOD: We propose a planarian light/dark test, designated PLDT, to predict anxiogenic- or anxiolytic-like effects. Experimentally, we placed a planarian at the midline of a Petri dish, containing test compound or water, that was split evenly into light and dark compartments and determined time spent in the light over 10min...
October 16, 2017: Journal of Neuroscience Methods
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/28985394/a-validated-method-for-the-detection-of-32-bath-salts-in-oral-fluid
#10
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/28890655/comparison-of-3-derivatization-methods-for-the-analysis-of-amphetamine-related-drugs-in-oral-fluid-by-gas-chromatography-mass-spectrometry
#11
Khaled M Mohamed, Abdulsallam Bakdash
The heptafluorobutyric anhydride (HFBA), pentafluoropropionic anhydride (PFPA), and trifluoroacetic anhydride (TFAA) are compared as derivatizing reagents to use as the optimal method for the analysis of 10 amphetamines and cathinones in oral fluid. The target compounds were amphetamine (AMP), methamphetamine (MA), 4-methylamphetamine, 3,4-methylenedioxyamphetamine (MDA), 3,4-methylenedioxymethamphetamine (MDMA), 3,4-methylenedioxy-N-ethylamphetamine (MDEA), cathinone (CAT), methcathinone, mephedrone, and ephedrine...
2017: Analytical Chemistry Insights
https://www.readbyqxmd.com/read/28885007/stereoselective-differences-between-the-reinforcing-and-motivational-effects-of-cathinone-derived-4-methylmethcathinone-mephedrone-in-self-administering-rats
#12
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
#13
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/28873977/one-step-derivatization-extraction-method-for-rapid-analysis-of-eleven-amphetamines-and-cathinones-in-oral-fluid-by-gc-ms
#14
Khaled Mohamed
A simple analytical method was developed for in-matrix derivatization of 11 amphetamine-like molecules. Ethyl chloroformate as the derivatization reagent and ethyl acetate as the extraction solvent were added directly to oral fluid samples at alkaline pH. Samples were analyzed by gas chromatography-mass spectrometry. Ions monitored for quantification were m/z 44, 91 and 116 for amphetamine (AMP); m/z 58, 91 and 130 for methamphetamine (MA); m/z 44, 105 and 116 for 4-methylamphetamine; m/z 44, 116 and 251 for 3,4-methylenedioxyamphetamine; m/z 58, 130 and 265 for 3,4-methylenedioxymethamphetamine (MDMA); m/z 72, 116 and 144 for 3,4-methylenedioxyethylamphetamine; m/z 44, 105 and 116 for cathinone; m/z 58, 105 and 130 for methcathinone; m/z 58, 119 and 130 for mephedrone; m/z 58, 107 and 130 for ephedrine (EPH); m/z 207, 250 and 322 for fenethylline; m/z 48, 92 and 120 for AMP-D5; m/z 62, 92 and 134 for MA-D5; m/z 48, 120 and 256 for MDA-D5; and m/z 62, 134 and 270 for MDMA-D5...
September 1, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28868040/novel-psychoactive-substances-recent-progress-on-neuropharmacological-mechanisms-of-action-for-selected-drugs
#15
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
https://www.readbyqxmd.com/read/28851615/assessing-the-role-of-dopamine-in-the-differential-neurotoxicity-patterns-of-methamphetamine-mephedrone-methcathinone-and-4-methylmethamphetamine
#16
REVIEW
John H Anneken, Mariana Angoa-Perez, Girish C Sati, David Crich, Donald M Kuhn
Methamphetamine and mephedrone are designer drugs with high abuse liability and they share extensive similarities in their chemical structures and neuropharmacological effects. However, these drugs differ in one significant regard: methamphetamine elicits dopamine neurotoxicity and mephedrone does not. From a structural perspective, mephedrone has a β-keto group and a 4-methyl ring addition, both of which are lacking in methamphetamine. Our previous studies found that methcathinone, which contains only the β-keto substituent, is neurotoxic, while 4-methylmethamphetamine, which contains only the 4-methyl ring substituent, elicits minimal neurotoxicity...
August 26, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28835196/prevalence-of-recreational-drug-use-reported-by-men-who-have-sex-with-men-attending-sexual-health-clinics-in-manchester-uk
#17
A Tomkins, S Ahmad, L Cannon, S P Higgins, M Kliner, A Kolyva, C Ward, R Vivancos
Recreational drug use (RDU) has been reported to be disproportionately higher in men who have sex with men (MSM) when compared to their heterosexual counterparts. To identify RDU, links to risky sexual practices and infections for MSM attending three sexual health clinics across Manchester, United Kingdom, a retrospective case note review was conducted using a random powered sample of service users attending three sites during 2014. Three hundred and fifty-seven case notes were reviewed across three sites. Eighteen per cent of service users reported any type of RDU...
January 1, 2017: International Journal of STD & AIDS
https://www.readbyqxmd.com/read/28828691/pharmacokinetics-of-mephedrone-and-its-metabolites-in-human-by-lc-ms-ms
#18
Eulàlia Olesti, Magí Farré, Esther Papaseit, Aristotelis Krotonoulas, Mitona Pujadas, Rafael de la Torre, Óscar J Pozo
Mephedrone is a synthetic cathinone consumed as a recreational drug. Recently, it was identified several of its metabolites in vivo in humans but there is little information about its pharmacokinetics in plasma and urine. Although several analytical methods have been proposed for mephedrone quantification in different matrices, none are available for its metabolites. Therefore, the aim of the study was to develop and validate an analytical method using liquid chromatography-tandem mass spectrometry for the quantification of mephedrone, nor-mephedrone, N-succinyl-nor-mephedrone, 1'-dihydro-mephedrone, and 4'-carboxy-mephedrone...
November 2017: AAPS Journal
https://www.readbyqxmd.com/read/28815279/evaluation-of-training-dose-in-male-sprague-dawley-rats-trained-to-discriminate-4-methylmethcathinone
#19
Michael D Berquist, Nathyn A Thompson, Lisa E Baker
RATIONALE: Although the synthetic cathinone 4-methylmethcathinone (4-MMC, mephedrone) has been a subject of intensive research investigation, the pharmacological mechanisms involved in its interoceptive stimulus effects have yet to be fully characterized. OBJECTIVE: The present study employed drug discrimination methods in rats to compare the interoceptive stimulus properties of two different training doses of 4-MMC to other substances with similar pharmacological actions...
November 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28811192/relative-reinforcing-effects-of-second-generation-synthetic-cathinones-acquisition-of-self-administration-and-fixed-ratio-dose-response-curves-in-rats
#20
REVIEW
Brenda M Gannon, Kayla I Galindo, Melson P Mesmin, Agnieszka Sulima, Kenner C Rice, Gregory T Collins
"Bath salts" preparations contain synthetic cathinones which interact with monoamine transporters and function as either monoamine uptake inhibitors or releasers. 3,4-Methylenedioxypyrovalerone (MDPV), 3,4-methylenedioxymethcathinone (methylone), and 4-methylmethcathinone (mephedrone) were three of the most common cathinones (i.e., "first-generation" cathinones); however, after the US Drug Enforcement Administration placed them under Schedule I regulations, they were replaced with structurally related cathinones that were not subject to regulations (i...
August 12, 2017: Neuropharmacology
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