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https://www.readbyqxmd.com/read/29778945/self-administration-of-the-synthetic-cathinone-mpdv-enhances-reward-function-via-a-nicotinic-receptor-dependent-mechanism
#1
Jean R Geste, Marjory Pompilus, Marcelo Febo, Adriaan W Bruijnzeel
Methylenedioxypyrovalerone (MDPV) is an addictive synthetic drug with severe side effects. Previous studies have shown that MDPV has positive reinforcing properties. However, little is known about the effect of MDPV self-administration on the state of the brain reward system and the neuronal mechanisms by which MDPV mediates its effects. The goal of the present studies was to determine the effect of MDPV self-administration on reward function and the role of cholinergic neurotransmission in the reinforcing effects of MDPV...
May 9, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29740356/behavioural-pharmacokinetic-metabolic-and-hyperthermic-profile-of-3-4-methylenedioxypyrovalerone-mdpv-in-the-wistar-rat
#2
Rachel R Horsley, Eva Lhotkova, Katerina Hajkova, Barbara Feriancikova, Michal Himl, Martin Kuchar, Tomas Páleníček
3,4-methylenedioxypyrovalerone (MDPV) is a potent pyrovalerone cathinone that is substituted for amphetamines by recreational users. We report a comprehensive and detailed description of the effects of subcutaneous MDPV (1-4 mg/kg) on pharmacokinetics, biodistribution and metabolism, acute effects on thermoregulation under isolated and aggregated conditions, locomotion (open field) and sensory gating (prepulse inhibition, PPI). All studies used male Wistar rats. Pharmacokinetics after single dose of 2 mg/kg MDPV was measured over 6 h in serum, brain and lungs...
2018: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/29729891/functional-connectivity-behavioral-and-dopaminergic-alterations-24-hours-following-acute-exposure-to-synthetic-bath-salt-drug-methylenedioxypyrovalerone
#3
Luis M Colon-Perez, Jose A Pino, Kaustuv Saha, Marjory Pompilus, Sherman Kaplitz, Nafisa Choudhury, Darin A Jagnarine, Jean R Geste, Brandon A Levin, Isaac Wilks, Barry Setlow, Adriaan W Bruijnzeel, Habibeh Khoshbouei, Gonzalo E Torres, Marcelo Febo
Among cathinone drugs known as bath salts, methylenedioxypyrovalerone (MDPV) exerts its potent actions via the dopamine (DA) system, and at intoxicating doses may produce adverse behavioral effects. Previous work by our group suggests that prolonged alterations in correlated neural activity between cortical and striatal areas could underlie, at least in part, the adverse reactions to this bath salt drug. In the present study, we assessed the effect of acute MDPV administration on brain functional connectivity at 1 and 24 h in rats...
May 3, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29714473/dark-classics-in-chemical-neuroscience-cathinone-derived-psychostimulants
#4
Steven J Simmons, Jonna M Leyrer-Jackson, Chicora F Oliver, Callum Hicks, John Muschamp, Scott M Rawls, M Foster Olive
Cathinone is a plant alkaloid found in khat leaves of perennial shrubs grown in East Africa. Similar to cocaine, cathinone elicits psychostimulant effects which are in part attributed to its amphetamine-like structure. Around 2010, home laboratories began altering the parent structure of cathinone to synthesize derivatives with mechanisms of action, potencies, and pharmacokinetics permitting high abuse potential and toxicity. These "synthetic cathinones" include 4-methylmethcathinone (mephedrone), 3,4-methylenedioxypyrovalerone (MDPV) and the empathogenic agent 3,4-methylenedioxymethcathinone (methylone) which collectively gained international popularity following aggressive online marketing as well as availability in various retail outlets...
May 1, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29703999/amphetamine-maintenance-differentially-modulates-effects-of-cocaine-methylenedioxypyrovalerone-mdpv-and-methamphetamine-on-intracranial-self-stimulation-and-nucleus-accumbens-dopamine-in-rats
#5
Amy R Johnson, Matthew L Banks, Dana E Selley, S Stevens Negus
Amphetamine maintenance is effective clinically to reduce the consumption of the monoamine uptake inhibitor cocaine but not of the monoamine releaser methamphetamine, and its effectiveness in treating the abuse of other psychostimulants is not known. The mechanisms for differential amphetamine-maintenance effectiveness to treat different types of psychostimulant abuse are also not known. Accordingly, the present study compared the effects of amphetamine maintenance on abuse-related behavioral and neurochemical effects of cocaine, methamphetamine, and the "bath salts" constituent 3,4-methylenedioxypyrovalerone (MDPV) in rats...
April 19, 2018: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29597343/dopamine-d1-like-receptor-agonist-and-d2-like-receptor-antagonist-stepholidine-reduces-reinstatement-of-drug-seeking-behavior-for-3-4-methylenedioxypyrovalerone-mdpv-in-rats
#6
Callum Hicks, Peng Huang, Linnet Ramos, Sunil U Nayak, Yohanka Caro, Allen B Reitz, Garry R Smith, David Y-W Lee, Scott M Rawls, Lee-Yuan Liu-Chen
Psychostimulant reinforcement is mediated by stimulation of both dopamine (DA) D1-like and D2-like receptors, suggesting that pharmacotherapy agents with a dual DA receptor mechanism may be useful for managing psychostimulant abuse. (-)-Stepholidine (L-SPD) is a Chinese herbal extract that functions as a D1-like receptor agonist and D2-like receptor antagonist. L-SPD has been shown to attenuate the reinforcing effects of heroin; however, its effects on the synthetic cathinone 3,4-methylenedioxypyrovalerone (MDPV) have not been examined...
April 6, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29572046/neurotoxicity-screening-of-new-psychoactive-substances-nps-effects-on-neuronal-activity-in-rat-cortical-cultures-using-microelectrode-arrays-mea
#7
Anne Zwartsen, Laura Hondebrink, Remco Hs Westerink
While the prevalence and the use of new psychoactive substances (NPS) is steadily increasing, data on pharmacological, toxicological and clinical effects is limited. Considering the large number of NPS available, there is a clear need for efficient in vitro screening techniques that capture multiple mechanisms of action. Neuronal cultures grown on multi-well microelectrode arrays (mwMEAs) have previously proven suitable for neurotoxicity screening of chemicals, pharmaceuticals and (illicit) drugs. We therefore used rat primary cortical cultures grown on mwMEA plates to investigate the effects of eight NPS (PMMA, α-PVP, methylone, MDPV, 2 C-B, 25B-NBOMe, BZP and TFMPP) and two 'classic' illicit drugs (cocaine, methamphetamine) on spontaneous neuronal activity...
March 20, 2018: Neurotoxicology
https://www.readbyqxmd.com/read/29558687/cathinone-stability-in-authentic-urine-specimens
#8
Lindsay Glicksberg, Sumandeep Rana, Sarah Kerrigan
PURPOSE: Synthetic cathinones are encountered in a variety of antemortem and postmortem forensic toxicology investigations. Earlier experimental studies using fortified urine have evaluated analyte, temperature and pH-dependent variables associated with their stability. The purpose of this study was to compare experimental findings with those obtained using authentic urine from cathinone users. METHODS: In this report we compare cathinone concentrations in 180 authentic unpreserved urine specimens, following known periods of refrigerated storage...
March 8, 2018: Forensic Science International
https://www.readbyqxmd.com/read/29550625/chemokines-and-bath-salts-cxcr4-receptor-antagonist-reduces-rewarding-and-locomotor-stimulant-effects-of-the-designer-cathinone-mdpv-in-rats
#9
Chicora F Oliver, Steven J Simmons, Sunil U Nayak, Garry R Smith, Allen B Reitz, Scott M Rawls
BACKGROUND AND PURPOSE: Little is known about how chemokine systems influence the behavioral effects of designer cathinones and psychostimulants. The chemokine CXCL12 and its principal receptor target, CXCR4, are of particular interest because CXCR4 activation enhances mesolimbic dopamine output that facilitates psychostimulant reward, reinforcement, and locomotor activation. Repeated cocaine enhances CXCL12 gene expression in the midbrain and produces conditioned place preference (CPP) that is inhibited by a CXCR4 antagonist...
May 1, 2018: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29524346/drug-facilitated-sexual-assault-dfsa-involving-4-methylethcathinone-4-mec-3-4-methylenedioxypyrovalerone-mdpv-and-doxylamine-highlighted-by-hair-analysis
#10
Islam Amine Larabi, Marie Martin, Isabelle Etting, Pauline Penot, Nicolas Fabresse, Jean Claude Alvarez
Recently, the emergence of new psychoactive substances (NPS) has led to their wide use among clubbers and men who have sex with men (MSM) for their stimulant effects. However, their use in drug-facilitated sexual assault (DFSA) has rarely been described. Herein we report a case of a 44-year-old man who was assaulted after a party. Due to late reporting of the offense, only hair (black) was sampled 15 days later and a segmental analysis was achieved to look for most DFSA agents and NPS. Twenty mg of each segment (A: 0-1 cm, B: 1-3 cm, and C: 3-5 cm) were incubated in phosphate buffer pH 5...
March 10, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29459818/gestational-exposure-to-the-synthetic-cathinone-methylenedioxypyrovalerone-results-in-reduced-maternal-care-and-behavioral-alterations-in-mouse-pups
#11
László I Gerecsei, András Csillag, Gergely Zachar, Lőrinc Gévai, László Simon, Árpád Dobolyi, Ágota Ádám
The member of synthetic cathinone family, methylenedioxypyrovalerone (MDPV), is a frequently used psychoactive drug of abuse. The objective of our study was to determine the effect of MDPV (administered from the 8th to the 14th day of gestation) on the behavior of neonatal and adolescent mice, as well as its effect on maternal care. We measured maternal care (pup retrieval test, nest building), locomotor activity (open field test), and motor coordination (grip strength test) of dams, whereas on pups we examined locomotor activity at postnatal day 7 and day 21 (open field test) and motor coordination on day 21 (grip strength test)...
2018: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/29364498/synthetic-cathinones-related-fatalities-an-update
#12
S Zaami, R Giorgetti, S Pichini, F Pantano, E Marinelli, F P Busardò
OBJECTIVE: Synthetic cathinones, more commonly known as "bath salts", are synthetic drugs chemically related to cathinone, a psychostimulant found in the khat plant. They are the first most consumed products among new psychoactive substances, which cause psychostimulant and hallucinogenic effects determining a number of fatalities worldwide.  In this paper, we have systematically reviewed cases of synthetic cathinones-related fatalities analytically confirmed, which have occurred in the last few years...
January 2018: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/29361056/in-vitro-isolation-of-small-molecule-binding-aptamers-with-intrinsic-dye-displacement-functionality
#13
Haixiang Yu, Weijuan Yang, Obtin Alkhamis, Juan Canoura, Kyung-Ae Yang, Yi Xiao
Aptamer-based sensors offer a powerful tool for molecular detection, but the practical implementation of these biosensors is hindered by costly and laborious sequence engineering and chemical modification procedures. We report a simple strategy for directly isolating signal-reporting aptamers in vitro through systematic evolution of ligands by exponential enrichment (SELEX) that transduce binding events into a detectable change of absorbance via target-induced displacement of a small-molecule dye. We first demonstrate that diethylthiatricarbocyanine (Cy7) can stack into DNA three-way junctions (TWJs) in a sequence-independent fashion, greatly altering the dye's absorbance spectrum...
January 19, 2018: Nucleic Acids Research
https://www.readbyqxmd.com/read/29275216/mdpv-in-forensic-routine-cases-psychotic-and-aggressive-behavior-in-relation-to-plasma-concentrations
#14
Marco Diestelmann, Anna Zangl, Inge Herrle, Eva Koch, Matthias Graw, Liane D Paul
The new psychoactive substance 3,4-methylenedioxypyrovalerone (MDPV) belongs to the group of synthetic cathinones and is purchased mainly as "research chemical" or "bath salt" on the illegal drug market, also in South Bavaria. MDPV was detected in blood and urine samples from 2010 on in 50 authentic routine cases in a forensic setting. Plasma concentrations in 46 cases with available blood specimens ranged from approximately 1.0 to 301μg/L (median 23.7; mean 47.9μg/L), detected by a fully validated LC-MS/MS method...
February 2018: Forensic Science International
https://www.readbyqxmd.com/read/29217539/inhibition-of-cocaine-and-3-4-methylenedioxypyrovalerone-mdpv-self-administration-by-lorcaserin-is-mediated-by-5-ht2c-receptors-in-rats
#15
Brenda M Gannon, Agnieszka Sulima, Kenner C Rice, Gregory T Collins
Lorcaserin is a serotonin (5-HT)2C receptor-preferring agonist approved by the US Food and Drug Administration to treat obesity. Lorcaserin decreases cocaine self-administration in rats and monkeys. Although this effect is partially inhibited by a 5-HT2C receptor antagonist (SB242084), lorcaserin also has effects at 5-HT2A and 5-HT1A receptors, and the relative contribution of these receptors to its anti-cocaine effects has not been investigated. The goals of this study were to determine 1) the potency and effectiveness of lorcaserin to decrease self-administration of cocaine and 3,4-methylenedioxypyrovalerone (MDPV), a common "bath salts" constituent; and 2) the receptor(s) mediating the effects of lorcaserin on cocaine and MDPV self-administration...
March 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29214532/qualitative-and-quantitative-temporal-analysis-of-licit-and-illicit-drugs-in-wastewater-in-australia-using-liquid-chromatography-coupled-to-mass-spectrometry
#16
Richard Bade, Jason M White, Cobus Gerber
The combination of qualitative and quantitative bimonthly analysis of pharmaceuticals and illicit drugs using liquid chromatography coupled to mass spectrometry is presented. A liquid chromatography-quadrupole time of flight instrument equipped with Sequential Window Acquisition of all THeoretical fragment-ion spectra (SWATH) was used to qualitatively screen 346 compounds in influent wastewater from two wastewater treatment plants in South Australia over a 14-month period. A total of 100 compounds were confirmed and/or detected using this strategy, with 61 confirmed in all samples including antidepressants (amitriptyline, dothiepin, doxepin), antipsychotics (amisulpride, clozapine), illicit drugs (cocaine, methamphetamine, amphetamine, 3,4-methylenedioxymethamphetamine (MDMA)), and known drug adulterants (lidocaine and tetramisole)...
January 2018: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/29183686/neurocognitive-dysfunction-following-repeated-binge-like-self-administration-of-the-synthetic-cathinone-3-4-methylenedioxypyrovalerone-mdpv
#17
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 26, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29121936/molecular-characterization-of-a-novel-muscovy-duck-parvovirus-isolate-evidence-of-recombination-between-classical-mdpv-and-goose-parvovirus-strains
#18
Jianye Wang, Jueyi Ling, Zhixian Wang, Yu Huang, Jianzhong Zhu, Guoqiang Zhu
BACKGROUND: Muscovy duck parvovirus (MDPV) and Goose parvovirus (GPV) are important etiological agents for Muscovy duck parvoviral disease and Derzsy's disease, respectively; both of which can cause substantial economic losses in waterfowl industry. In contrast to GPV, the complete genomic sequence data of MDPV isolates are still limited and their phylogenetic relationships largely remain unknown. In this study, the entire genome of a pathogenic MDPV strain ZW, which was isolated from a deceased Muscovy duckling in 2006 in China, was cloned, sequenced, and compared with that of other classical MDPV and GPV strains...
November 9, 2017: BMC Veterinary Research
https://www.readbyqxmd.com/read/29097307/effect-fingerprinting-of-new-psychoactive-substances-nps-what-can-we-learn-from-in-vitro-data
#19
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 (mCPP, TFMPP, BZP)...
February 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29042316/concurrent-repeated-exposure-to-3-4-methylenedioxypyrovalerone-and-cocaine-produce-locomotor-sensitization-with-minimal-effects-on-brain-monoamines
#20
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
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