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synthetic cathinone

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https://www.readbyqxmd.com/read/29042316/concurrent-repeated-exposure-to-3-4-methylenedioxypyrovalerone-and-cocaine-produce-locomotor-sensitization-with-minimal-effects-on-brain-monoamines
#1
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
#2
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
#3
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
#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/28985394/a-validated-method-for-the-detection-of-32-bath-salts-in-oral-fluid
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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/28866386/effects-of-orally-self-administered-bath-salt-constituent-3-4-methylenedioxypyrovalerone-mdpv-in-mice
#15
Brenda M Gannon, Lauren N Russell, Meet S Modi, Kenner C Rice, William E Fantegrossi
Synthetic cathinones in bath salts products are psychostimulant drugs of abuse, and 3,4-methylenedioxypyrovalerone (MDPV) is a common constituent of these products. Oral MDPV has been show to stimulate locomotor activity but reinforcing, locomotor and appetitive stimulus effects of oral MDPV are unknown. Choice procedures evaluated preference for 0.03, 0.10, 0.30, and 1.00mg/mL MDPV solutions versus 0.10mg/mL quinine solution or water. To verify that oral MDPV produced pharmacological effects, locomotor activity was monitored during and after consumption of water, quinine, or MDPV solutions...
August 4, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28828691/pharmacokinetics-of-mephedrone-and-its-metabolites-in-human-by-lc-ms-ms
#16
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...
August 21, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28815279/evaluation-of-training-dose-in-male-sprague-dawley-rats-trained-to-discriminate-4-methylmethcathinone
#17
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...
August 16, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28813207/examination-of-synthetic-cannabinoid-and-cathinone-use-among-a-drug-using-offender-sample-2013-2015
#18
Kirsten Elin Smith, Amanda M Bunting, Michele Staton, Robert Walker, Sara Shalash, Erin Winston, Kevin Pangburn
Use of novel psychoactive substances (NPS) such as synthetic cannabinoids (e.g., "Spice," "Serenity") and cathinones (e.g., "bath salts") has proliferated in recent years; however, there is a gap in research examining prevalence among offender samples. This study examined demographics, drug use, mental health characteristics, and criminal histories of NPS users compared to non-NPS users within an offender sample entering drug treatment. Using logistic regression analysis, combined 2013-2015 assessment data were examined (N = 8,791)...
August 16, 2017: Journal of Psychoactive Drugs
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
#19
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
https://www.readbyqxmd.com/read/28811141/the-pharmacokinetic-profile-of-synthetic-cathinones-in-a-pregnancy-model
#20
Lauren G Strange, Kerri Kochelek, Robert Keasling, Stacy D Brown, Brooks B Pond
In recent years, the abuse of synthetic cathinones or 'bath salts' has become a major public health concern. Although these compounds were initially sold legally and labeled "not for human consumption", the 'bath salts' are psychostimulants, with similar structures and pharmacologic mechanisms to cocaine, the amphetamines, and 3,4 methylendioxymethamphetamine (MDMA, Molly, or Ecstasy). The reported use of these substances by women of child-bearing age highlights the necessity of studies seeking to delineate risks of prenatal exposure...
August 12, 2017: Neurotoxicology and Teratology
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