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https://www.readbyqxmd.com/read/27910188/comparing-rewarding-and-reinforcing-properties-between-bath-salt-3-4-methylenedioxypyrovalerone-mdpv-and-cocaine-using-ultrasonic-vocalizations-in-rats
#1
Steven J Simmons, Ryan A Gregg, Fionya H Tran, Lili Mo, Eva von Weltin, David J Barker, Taylor A Gentile, Lucas R Watterson, Scott M Rawls, John W Muschamp
Abuse of synthetic psychostimulants like synthetic cathinones has risen in recent years. 3,4-Methylenedioxypyrovalerone (MDPV) is one such synthetic cathinone that demonstrates a mechanism of action similar to cocaine. Compared to cocaine, MDPV is more potent at blocking dopamine and norepinephrine reuptake and is readily self-administered by rodents. The present study compared the rewarding and reinforcing properties of MDPV and cocaine using systemic injection dose-response and self-administration models...
December 1, 2016: Addiction Biology
https://www.readbyqxmd.com/read/27830575/neuropharmacology-of-3-4-methylenedioxypyrovalerone-mdpv-its-metabolites-and-related-analogs
#2
Michael H Baumann, Mohammad O Bukhari, Kurt R Lehner, Sebastien Anizan, Kenner C Rice, Marta Concheiro, Marilyn A Huestis
3,4-Methylenedioxypyrovalerone (MDPV) is a psychoactive component of so-called bath salts products that has caused serious medical consequences in humans. In this chapter, we review the neuropharmacology of MDPV and related analogs, and supplement the discussion with new results from our preclinical experiments. MDPV acts as a potent uptake inhibitor at plasma membrane transporters for dopamine (DAT) and norepinephrine (NET) in nervous tissue. The MDPV formulation in bath salts is a racemic mixture, and the S isomer is much more potent than the R isomer at blocking DAT and producing abuse-related effects...
November 10, 2016: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/27814952/liquid-chromatography-tandem-mass-spectrometry-determination-of-synthetic-cathinones-and-phenethylamines-in-influent-wastewater-of-eight-european-cities
#3
Richard Bade, Lubertus Bijlsma, Juan V Sancho, Jose A Baz-Lomba, Sara Castiglioni, Erika Castrignanò, Ana Causanilles, Emma Gracia-Lor, Barbara Kasprzyk-Hordern, 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, Félix Hernández
The popularity of new psychoactive substances (NPS) has grown in recent years, with certain NPS commonly and preferentially consumed even following the introduction of preventative legislation. With the objective to improve the knowledge on the use of NPS, a rapid and very sensitive method was developed for the determination of ten priority NPS (N-ethylcathinone, methylenedioxypyrovalerone (MDPV), methylone, butylone, methedrone, mephedrone, naphyrone, 25-C-NBOMe, 25-I-NBOMe and 25-B-NBOMe) in influent wastewater...
November 1, 2016: Chemosphere
https://www.readbyqxmd.com/read/27753008/neurotoxicology-of-synthetic-cathinone-analogs
#4
Mariana Angoa-Pérez, John H Anneken, Donald M Kuhn
The present review briefly explores the neurotoxic properties of methcathinone, mephedrone, methylone, and methylenedioxypyrovalerone (MDPV), four synthetic cathinones most commonly found in "bath salts." Cathinones are β-keto analogs of the commonly abused amphetamines and display pharmacological effects resembling cocaine and amphetamines, but despite their commonalities in chemical structures, synthetic cathinones possess distinct neuropharmacological profiles and produce unique effects. Among the similarities of synthetic cathinones with their non-keto analogs are their targeting of monoamine systems, the release of neurotransmitters, and their stimulant properties...
October 18, 2016: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/27733481/gc-ms-ms-ms-and-gc-ir-analysis-of-a-series-of-methylenedioxyphenyl-aminoketones-precursors-ring-regioisomers-and-side-chain-homologs-of-3-4-methylenedioxypyrovalerone
#5
Younis F Hamad Abiedalla, Karim Abdel-Hay, Jack DeRuiter, C Randall Clark
A combination of GC-MS, MS/MS and GC-IR techniques were used to characterize the ring substitution pattern, the alkyl side-chain and the cyclic tertiary amine portions of a series of six homologous and regioisomeric methylenedioxyphenyl-aminoketones related to the designer drug, 3,4-methylenedioxypyrovalerone (MDPV). Chromatographic retention increases with the hydrocarbon content of the alkyl side-chain and the 3,4-methylenedioxy substitution pattern shows higher retention than the corresponding 2,3-methylenedioxy isomer...
October 12, 2016: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/27714779/pharmacological-mechanisms-underlying-the-cardiovascular-effects-of-the-bath-salt-constituent-3-4-methylenedioxypyrovalerone-mdpv
#6
Charles W Schindler, Eric B Thorndike, Masaki Suzuki, Kenner C Rice, Michael H Baumann
BACKGROUND AND PURPOSE: 3,4-Methylenedioxypyrovalerone (MDPV) is a synthetic cathinone with stimulatory cardiovascular effects that can lead to serious medical complications. Here, we examined the pharmacological mechanisms underlying these cardiovascular actions of MDPV in conscious rats. EXPERIMENTAL APPROACH: Male Sprague-Dawley rats had telemetry transmitters surgically implanted for the measurement of BP and heart rate (HR). On test days, rats were placed individually in standard isolation cubicles...
December 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27697731/identification-and-quantification-of-synthetic-cathinones-in-blood-and-urine-using-liquid-chromatography-quadrupole-time-of-flight-lc-q-tof-mass-spectrometry
#7
Lindsay Glicksberg, Kelsie Bryand, Sarah Kerrigan
Synthetic cathinones continue to present a formidable challenge to forensic toxicology laboratories despite the fact that they are often encountered in impaired driving and death investigations. Due to limitations in immunoassay-based screening technologies, many forensic toxicology laboratories must rely on more labor intensive chromatographic-based screening approaches in order to detect these drugs in biological evidence. Solid phase extraction (SPE) and liquid chromatography-quadrupole/time of flight (LC-Q/TOF) mass spectrometry were used to identify twenty-two synthetic cathinones in urine and blood...
November 1, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/27678045/occurrence-of-new-psychoactive-substances-in-wastewater-of-major-chinese-cities
#8
Tingting Gao, Peng Du, Zeqiong Xu, Xiqing Li
New psychoactive substances have become increasingly popular across the globe in recent years, which may cause certain public health issues. In this work, sewage-based epidemiology was applied to examine the use of two synthetic cathinones, mephedrone and methylenedioxypyrovalerone (MDPV), and three piperazines, benzylpiperazine (BZP), trifluoromethylphenylpiperazine (TFMPP), and 1-(3-Chlorophenyl)piperazine (mCPP), across China. Influent wastewater samples were collected from 36 sewage treatment plants (STPs) in 18 major cities that cover all the geographic regions of the country...
September 24, 2016: Science of the Total Environment
https://www.readbyqxmd.com/read/27677783/electrophysiological-actions-of-synthetic-cathinones-on-monoamine-transporters
#9
Ernesto Solis
Products containing psychoactive synthetic cathinones, such as mephedrone and 3,4-methylenedioxypyrovalerone (MDPV) are prevalent in our society. Synthetic cathinones are structurally similar to methamphetamine, and numerous synthetics have biological activity at dopamine, serotonin, and norepinephrine transporters. Importantly, monoamine transporters co-transport sodium ions along with their substrate, and movement of substrates and ions through the transporter can generate measurable ionic currents. Here we review how electrophysiological information has enabled us to determine how synthetic cathinones affect transporter-mediated currents in cells that express these transporters...
September 28, 2016: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/27677782/mdma-methylone-and-mdpv-drug-induced-brain-hyperthermia-and-its-modulation-by-activity-state-and-environment
#10
Eugene A Kiyatkin, Suelynn E Ren
Psychomotor stimulants are frequently used by humans to intensify the subjective experience of different types of social interactions. Since psychomotor stimulants enhance metabolism and increase body temperatures, their use under conditions of physiological activation and in warm humid environments could result in pathological hyperthermia, a life-threatening symptom of acute drug intoxication. Here, we will describe the brain hyperthermic effects of MDMA, MDPV, and methylone, three structurally related recreational drugs commonly used by young adults during raves and other forms of social gatherings...
September 28, 2016: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/27594923/chiral-enantioresolution-of-cathinone-derivatives-present-in-legal-highs-and-enantioselectivity-evaluation-on-cytotoxicity-of-3-4-methylenedioxypyrovalerone-mdpv
#11
Bárbara Silva, Carla Fernandes, Maria Elizabeth Tiritan, Madalena M M Pinto, Maria João Valente, Márcia Carvalho, Paula Guedes de Pinho, Fernando Remião
Recently, great interest has been focused on synthetic cathinones since their consumption has increased exponentially. All synthetic cathinones exist as chiral molecules; the biological and/or toxicological properties of cathinones generally differ according to the enantiomers in human body. In this study, a chiral liquid chromatography method was developed to separate and determine the enantiomeric ratio of synthetic cathinones present in "legal highs" acquired in old smart shops or over the Internet. All the synthetic cathinones were efficiently enantio-separated with α and Rs ranging from 1...
2016: Forensic Toxicology
https://www.readbyqxmd.com/read/27592254/characterization-of-in-vitro-metabolites-of-methylenedioxypyrovalerone-mdpv-an-n-oxide-metabolite-formation-mediated-by-flavin-monooxygenase
#12
In Sook Kim, Shaheed Ur Rehman, Min Sun Choi, Moonhee Jang, Wonkyung Yang, Eunmi Kim, Hye Hyun Yoo
Methylenedioxypyrovalerone (MDPV) has emerged in recent years as a recreational substance with psychostimulant properties. In this study, in vitro metabolites of MDPV were characterized based on liquid chromatography/quadrupole-time-of-flight mass spectrometry (LC/QTOF MS). MDPV was incubated with human liver microsomes, human recombinant cDNA-expressed cytochrome P450 enzymes and flavin monooxygenase (FMO). MDPV was metabolized to yield eight metabolites (M1-M8) with major metabolic reactions such as demethylenation and oxidation...
November 30, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27538886/psychosis-associated-with-acute-recreational-drug-toxicity-a-european-case-series
#13
Odd Martin Vallersnes, Alison M Dines, David M Wood, Christopher Yates, Fridtjof Heyerdahl, Knut Erik Hovda, Isabelle Giraudon, Paul I Dargan
BACKGROUND: Psychosis can be associated with acute recreational drug and novel psychoactive substance (NPS) toxicity. However, there is limited data available on how common this is and which drugs are most frequently implicated. We describe a European case series of psychosis associated with acute recreational drug toxicity, and estimate the frequency of psychosis for different recreational drugs. METHODS: The European Drug Emergencies Network (Euro-DEN) collects data on presentations to Emergency Departments (EDs) with acute recreational drug and NPS toxicity at 16 centres in ten countries...
August 18, 2016: BMC Psychiatry
https://www.readbyqxmd.com/read/27520883/effects-of-3-4-methylenedioxypyrovalerone-mdpv-pre-exposure-on-the-aversive-effects-of-mdpv-cocaine-and-lithium-chloride-implications-for-abuse-vulnerability
#14
Claudia J Woloshchuk, Katharine H Nelson, Kenner C Rice, Anthony L Riley
BACKGROUND: Drug use is thought to be a balance of the rewarding and aversive effects of drugs. Understanding how various factors impact these properties and their relative balance may provide insight into their abuse potential. In this context, the present study attempted to evaluate the effects of drug history on the aversive effects of 3,4-methylenedioxypyrovalerone (MDPV), one of a variety of synthetic cathinones (collectively known as "bath salts"). METHODS: Different groups of male Sprague-Dawley rats were exposed to either vehicle or MDPV (1...
October 1, 2016: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/27493274/discriminative-stimulus-effects-of-binary-drug-mixtures-studies-with-cocaine-mdpv-and-caffeine
#15
Gregory T Collins, Megan Abbott, Kayla Galindo, Elise L Rush, Kenner C Rice, Charles P France
Illicit drug preparations often include more than one pharmacologically active compound. For example, cocaine and synthetic cathinones [e.g., 3,4-methylenedioxypyrovalerone (MDPV)] are often mixed with caffeine before sale. Caffeine is likely added to these preparations because it is inexpensive and legal; however, caffeine might also mimic or enhance some of the effects of cocaine or MDPV. In these studies, male Sprague-Dawley rats were trained to discriminate 10 mg/kg cocaine from saline, and the discriminative stimulus effects of cocaine, caffeine, and MDPV were evaluated alone and as binary mixtures (cocaine and caffeine, MDPV and caffeine, and cocaine and MDPV) at fixed-dose ratios of 3:1, 1:1, and 1:3 relative to the dose of each drug that produced 50% cocaine-appropriate responding...
October 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27474358/quantification-of-synthetic-cathinones-in-rat-brain-using-hilic-esi-ms-ms
#16
Jacob R Peters, Robert Keasling, Stacy D Brown, Brooks B Pond
The abuse of synthetic cathinones, formerly marketed as "bath salts", has emerged over the last decade. Three common drugs in this class include 3,4-methylenedioxypyrovalerone (MDPV), 4-methylmethcathinone (mephedrone), and 3,4-methylenedioxymethcathinone (methylone). An LC-MS/MS method has been developed and validated for the simultaneous quantification of MDPV, mephedrone, and methylone in brain tissue. Briefly, MDPV, mephedrone, methylone, and their deuterium-labeled analogs were subjected to solid phase extraction (SPE) and separated using an HILIC Silica Column...
July 29, 2016: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/27465234/enantioselective-determination-of-cathinone-derivatives-in-human-hair-by-capillary-electrophoresis-combined-in-line-with-solid-phase-extraction
#17
Tatiana Baciu, Francesc Borrull, Marta Calull, Carme Aguilar
A suitable method has been developed and validated for the chiral separation and determination of R,S-mephedrone and one of its metabolites, R,S-4-methylephedrine, and R,S-methylenedioxypyrovalerone (R,S-MDPV) in human hair samples by the in-line coupling between SPE and CD-assisted CE with a previous sample pretreatment procedure based on pressurized liquid extraction. Optimum separation was achieved on a fused silica-capillary of 50 μm id and 80 cm total length using 12 mg/mL β-CD in an aqueous solution of 80 mM disodium phosphate at pH 2...
September 2016: Electrophoresis
https://www.readbyqxmd.com/read/27365137/the-presence-of-stimulant-drugs-in-wastewater-from-krakow-poland-a-snapshot
#18
Katarzyna Styszko, Agnieszka Dudarska, Dariusz Zuba
An analysis of wastewater from Krakow (Poland) for the presence of controlled and uncontrolled stimulant drugs of abuse was performed. Samples were collected from the Plaszow wastewater treatment plant, Krakow, Poland, and prepared by solid phase extraction. The LC-QTOFMS method was applied for identification and quantification of popular stimulants: MDMA, mephedrone, 4-MEC, MDPV and mCPP. Environmental loads of illicit drugs were calculated; the WWTP discharged loads ranging from 3.6 to 6.7 mg day(-1) 1000 inhabitants(-1) of MDMA, 3...
September 2016: Bulletin of Environmental Contamination and Toxicology
https://www.readbyqxmd.com/read/27344160/analysis-of-the-genome-sequence-of-the-pathogenic-muscovy-duck-parvovirus-strain-yy-reveals-a-14-nucleotide-pair-deletion-in-the-inverted-terminal-repeats
#19
Jianye Wang, Yu Huang, Mingxu Zhou, Guoqiang Zhu
Genomic information about Muscovy duck parvovirus is still limited. In this study, the genome of the pathogenic MDPV strain YY was sequenced. The full-length genome of YY is 5075 nucleotides (nt) long, 57 nt shorter than that of strain FM. Sequence alignment indicates that the 5' and 3' inverted terminal repeats (ITR) of strain YY contain a 14-nucleotide-pair deletion in the stem of the palindromic hairpin structure in comparison to strain FM and FZ91-30. The deleted region contains one "E-box" site and one repeated motif with the sequence "TTCCGGT" or "ACCGGAA"...
September 2016: Archives of Virology
https://www.readbyqxmd.com/read/27329377/construction-and-sequencing-of-an-infectious-clone-of-the-goose-embryo-adapted-muscovy-duck-parvovirus-vaccine-strain-fz91-30
#20
Jianye Wang, Yu Huang, Mingxu Zhou, Philip R Hardwidge, Guoqiang Zhu
BACKGROUND: Muscovy duck parvovirus (MDPV) is the etiological agent of Muscovy duckling parvoviral disease, which is characterized by diarrhea, locomotive dysfunction, stunting, and death in young ducklings, and causes substantial economic losses in the Muscovy duck industry worldwide. FZ91-30 is an attenuated vaccine strain that is safe and immunogenic to ducklings, but the genomic information and molecular mechanism underlining the attenuation are not understood. METHODS: The FZ91-30 strain was propagated in 11-day-old embryonated goose eggs, and viral particles were purified from the pooled allantoic fluid by differential centrifugation and ultracentrifugation...
2016: Virology Journal
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