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https://www.readbyqxmd.com/read/28328032/product-ion-tandem-mass-spectrometric-differentiation-of-regioisomeric-side-chain-groups-in-cathinone-derivatives
#1
Younis Abiedalla, Jack DeRuiter, C Randall Clark
RATIONALE: Precursor materials are available to prepare aminoketone drugs containing regioisomeric propyl and isopropyl side-chain groups related to the drug alpha-pyrrovalerone (Flakka) and MDPV (3,4-methylenedioxypyrrovalerone). These compounds yield equivalent regioisomeric iminium cation base peaks in electron ionization mass spectrometry (EI-MS). METHODS: The propyl and isopropyl side-chain groups related to alpha-pyrrovalerone and MDPV were prepared and evaluated in EI-MS and tandem mass spectrometry (MS/MS) product ion experiments...
July 30, 2016: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/28325154/the-behavioral-profile-of-methylenedioxypyrovalerone-mdpv-and-%C3%AE-pyrrolidinopentiophenone-pvp-a-systematic-review
#2
Cornel N Stanciu, Thomas M Penders, Samantha A Gnanasegaram, Elvin Pirapakaran, Juvraj S Padda, Jeeven S Padda
BACKGROUND: New psychoactive substances are emerging at an alarming rate. With novel structures and properties they produce unique behavioral characteristics during intoxication. Synthetic cathinones are some of the most common. More and more are presenting to emergency departments due to consequences of use. Aside from isolated reports, little is known about these compounds. OBJECTIVE: Here we review literature pertaining to two common synthetic cathinones, MDPV and alphaPVP, and correlate clinically with guidance on management of intoxications...
March 21, 2017: Current Drug Abuse Reviews
https://www.readbyqxmd.com/read/28267375/university-students-attributions-for-abstinence-from-synthetic-cannabinoids-and-synthetic-cathinones
#3
Kirstin J Lauritsen, Harold Rosenberg, Jon E Sprague
BACKGROUND: Synthetic cannabinoids and synthetic cathinones are two increasingly available and potentially dangerous classes of substances. OBJECTIVE: We designed this study to test whether university students rated the influence of different types of reasons for abstaining differently as a function of type of drug (synthetic cannabinoids vs. synthetic cathinones) and gender (male vs. female). METHOD: Using a web-based survey, 176 male and 437 female undergraduate university students rated the degree to which each of 42 reasons for not taking drugs influenced their abstinence from those two classes of substances...
March 7, 2017: American Journal of Drug and Alcohol Abuse
https://www.readbyqxmd.com/read/28263006/rapid-analysis-of-forensic-related-samples-using-two-ambient-ionization-techniques-coupled-to-high-resolution-mass-spectrometers
#4
Eshwar Jagerdeo, Amanda Wriston
RATIONALE: This paper highlights the versatility of interfacing two ambient ionization techniques, Laser Diode Thermal Desorption (LDTD) and Atmospheric Solids Analysis probe (ASAP), to high resolution mass spectrometers and demonstrate the method's capability to rapidly generate high-quality data from multiple sample types with minimal, if any sample preparation. METHODS: For ASAP-MS analysis of solid and liquid samples, the material was transferred to a capillary surface before being introduced into the mass spectrometer...
March 6, 2017: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/28262947/exposure-of-mice-to-mdpv-during-adolescence-increases-the-psychostimulant-rewarding-and-reinforcing-effects-of-cocaine-in-adulthood
#5
R López-Arnau, M A Luján, L Duart-Castells, D Pubill, J Camarasa, O Valverde, E Escubedo
BACKGROUND AND PURPOSE: 3,4-Methylenedioxypyrovalerone (MDPV) is a synthetic cathinone with powerful psychostimulant effects. It selectively inhibits dopamine transporter (DAT) being 10-50-fold more potent as DAT blocker than cocaine, pointing to a high abuse liability. The main objective of the present study was to assess the consequences of an early (adolescence) MDPV exposure on the psychostimulant, rewarding and reinforcing effects induced by cocaine in adult mice. EXPERIMENTAL APPROACH: 21 days after MDPV pretreatment (1...
March 6, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28251297/glutamate-carboxypeptidase-ii-gcpii-inhibitor-2-pmpa-reduces-rewarding-effects-of-the-synthetic-cathinone-mdpv-in-rats-a-role-for-n-acetylaspartylglutamate-naag
#6
Callum Hicks, Ryan A Gregg, Sunil U Nayak, Lee Anne Cannella, Giana J Schena, Christopher S Tallarida, Allen B Reitz, Garry R Smith, Scott M Rawls
RATIONALE: Metabotropic glutamate 2 and 3 (mGluR2/3) receptors are implicated in drug addiction as they limit excessive glutamate release during relapse. N-acetylaspartylglutamate (NAAG) is an endogenous mGluR2/3 agonist that is inactivated by the glutamate carboxypeptidase II (GCPII) enzyme. GCPII inhibitors, and NAAG itself, attenuate cocaine-seeking behaviors. However, their effects on the synthetic cathinone 3,4-methylenedioxypyrovalerone (MDPV) have not been examined. OBJECTIVES: We determined whether withdrawal following repeated MDPV administration alters GCPII expression in corticolimbic regions...
March 1, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28220701/deconstructed-analogs-of-bupropion-reveal-structural-requirements-for-transporter-inhibition-versus-substrate-induced-neurotransmitter-release
#7
Abdelrahman R Shalabi, Donna Walther, Michael H Baumann, Richard A Glennon
Bupropion (1), an α-aminophenone uptake inhibitor at plasma membrane transporters for dopamine (DAT) and norepinephrine (NET), is a widely prescribed antidepressant and smoking cessation aid. Cathinone (2), a structurally simpler α-aminophenone, is a substrate-type releasing agent at the same transporters and a recognized drug of abuse. Our goal was to identify the structural features of α-aminophenones that govern the mechanistic transition from uptake inhibition to substrate-induced release. Deconstructed analogs of 1 were synthesized and compared for their ability to interact with DAT, NET, and the serotonin transporter (SERT) using in vitro assay methods...
February 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28219712/the-combination-of-mdpv-and-ethanol-results-in-decreased-cathinone-and-increased-alcohol-levels-study-of-such-pharmacological-interaction
#8
R López-Arnau, M Buenrostro-Jáuregui, P Muñoz-Villegas, J Rodríguez-Morató, A Ciudad-Roberts, L Duart, J Camarasa, R De la Torre, D Pubill, E Escubedo
Methylenedioxypyrovalerone (MDPV) is a new psychostimulant cathinone acting as a selective dopamine transporter blocker. Due to the concomitant consumption of ethanol (EtOH) and new psychoactive substances, it is of interest to explore a possible pharmacological interaction between MDPV and EtOH. In locomotor activity assays, EtOH (1g/kg i.p.) elicited a reduction in the stimulant effect induced by low doses of MDPV (0.1-0.3mg/kg, s.c.) in rats, jointly with a decrease in blood and brain MDPV concentrations...
February 17, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28210779/locomotor-activity-and-discriminative-stimulus-effects-of-a-novel-series-of-synthetic-cathinone-analogs-in-mice-and-rats
#9
Michael B Gatch, Sean B Dolan, Michael J Forster
RATIONALE: Recent years have seen an increase in the recreational use of novel, synthetic psychoactive substances. There are little or no data on the abuse liability of many of the newer compounds. OBJECTIVES: The current study investigated the discriminative stimulus and locomotor effects of a series of synthetic analogs of cathinone: α-pyrrolidinopropiophenone (α-PPP), α-pyrrolidinohexiophenone (α-PHP), α-pyrrolidinopentiothiophenone (α-PVT), 3,4-methylenedioxybutiophenone (MDPBP), and ethylone...
April 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28199890/gc-ms-gc-ms-ms-and-gc-ir-differentiation-of-desoxy-cathinone-derivatives-cyclic-tertiary-amines-related-to-mdpv
#10
Younis Abiedalla, Jack DeRuiter, C Randall Clark
The desoxy phenethylamine analogues in this study represent a combination of alkyl side-chain and cyclic amines (azetidine, pyrrolidine, piperidine and azepane) to yield a set of molecules of identical elemental composition as well as major mass spectral fragment ions (base peaks) of identical elemental composition. These desoxy phenethylamine analogues of the aminoketone designer drug, 3,4-methylenedioxy-pyrrovalerone (MDPV) related to the natural product cathinone were prepared from piperonal (3,4-methylenedioxybenzaldehyde) via the intermediate precursor ketones...
March 24, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28187296/toxicological-investigation-of-forensic-cases-related-to-the-designer-drug-3-4-methylenedioxypyrovalerone-mdpv-detection-quantification-and-studies-on-human-metabolism-by-gc-ms
#11
Marcel Grapp, Christoph Kaufmann, Martin Ebbecke
3,4-methylenedioxypyrovalerone (MDPV) is a synthetic cathinone belonging to the class of α-pyrrolidinophenones that become increasingly popular as a designer psychostimulant. Here, we report a comprehensive collection of MDPV exposure with quantitative serum level confirmation in Germany. During the years 2014-2016, we could proof consumption of MDPV in 23 cases where urine and blood samples were submitted to our laboratory by the police of Lower Saxony. Most of the samples underwent systematic toxicological analysis by gas chromatography-mass spectrometry (GC-MS), where MDPV could be detected in urine and/or serum samples...
February 2, 2017: Forensic Science International
https://www.readbyqxmd.com/read/28179474/individual-differences-in-the-relative-reinforcing-effects-of-3-4-methylenedioxypyrovalerone-mdpv-under-fixed-and-progressive-ratio-schedules-of-reinforcement-in-rats
#12
Brenda M Gannon, Kayla I Galindo, Kenner C Rice, Gregory T Collins
The recreational use of designer drugs, including synthetic cathinones (bath salts), is associated with high levels of abuse and toxicity, and represents a growing threat to public health. MDPV (3,4-methylenedioxypyrovalerone) is a cocaine-like monoamine uptake inhibitor, and one of the most widely available and abused synthetic cathinones. The present study used male Sprague-Dawley rats to directly compare: (1) the acquisition of responding for MDPV and cocaine under a fixed ratio (FR) 1 schedule of reinforcement; (2) full dose-response curves for MDPV and cocaine under FR5; and (3) progressive ratio (PR) schedules of reinforcement...
February 8, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28173643/the-abuse-potential-of-%C3%AE-piperidinopropiophenone-pipp-and-%C3%AE-piperidinopentiothiophenone-pivt-two-new-synthetic-cathinones-with-piperidine-ring-substituent
#13
Chrislean Jun Botanas, Seong Shoon Yoon, June Bryan de la Peña, Irene Joy Dela Peña, Mikyung Kim, Taeseon Woo, Joung-Wook Seo, Choon-Gon Jang, Kyung-Tae Park, Young Hun Lee, Yong Sup Lee, Hee Jin Kim, Jae Hoon Cheong
A diversity of synthetic cathinones has flooded the recreational drug marketplace worldwide. This variety is often a response to legal control actions for one specific compound (e.g. methcathinone) which has resulted in the emergence of closely related replacement. Based on recent trends, the nitrogen atom is one of the sites in the cathinone molecule being explored by designer type modifications. In this study, we designed and synthesized two new synthetic cathinones, (1) α-piperidinopropiophenone (PIPP) and (2) α-piperidinopentiothiophenone (PIVT), which have piperidine ring substituent on their nitrogen atom...
March 1, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28163218/atypical-dopamine-efflux-caused-by-3-4-methylenedioxypyrovalerone-mdpv-via-the-human-dopamine-transporter
#14
Aparna Shekar, Jenny I Aguilar, Greta Galli, Nicholas V Cozzi, Simon D Brandt, Arnold E Ruoho, Michael H Baumann, Heinrich J G Matthies, Aurelio Galli
Synthetic cathinones are similar in chemical structure to amphetamines, and their behavioral effects are associated with enhanced dopaminergic signaling. The past ten years of research on the common constituent of bath salts, MDPV (the synthetic cathinone 3,4-methylenedioxypyrovalerone), has aided the understanding of how synthetic cathinones act at the dopamine (DA) transporter (DAT). Several groups have described the ability of MDPV to block the DAT with high-affinity. In this study, we demonstrate for the first time a new mode of action of MDPV, namely its ability to promote DAT-mediated DA efflux...
February 3, 2017: Journal of Chemical Neuroanatomy
https://www.readbyqxmd.com/read/28161577/motivations-for-new-psychoactive-substance-use-among-regular-psychostimulant-users-in-australia
#15
Rachel Sutherland, Raimondo Bruno, Amy Peacock, Simon Lenton, Allison Matthews, Caroline Salom, Paul Dietze, Kerryn Butler, Lucinda Burns, Monica J Barratt
BACKGROUND: Examine the motivations for new psychoactive substance (NPS) use amongst a sample of regular psychostimulant users (RPU) in Australia, and determine whether motivations differ across substances. METHOD: Data were obtained from 419 RPU interviewed for the 2014 Ecstasy and related Drugs Reporting System who reported lifetime NPS use. Based on the most recent NPS used, motivations for use were rated on an 11-point scale (0 'no influence'-10 'maximum influence')...
February 2, 2017: International Journal on Drug Policy
https://www.readbyqxmd.com/read/28137731/clinical-presentation-autopsy-results-and-toxicology-findings-in-an-acute-n-ethylpentylone-fatality
#16
Phoutthasone Thirakul, Laura S Hair, Kirstin L Bergen, Julia M Pearson
The clinical presentation, autopsy findings and toxicology results in an acute fatality involving N-ethylpentylone, a new cathinone derivative, are described. Law enforcement transported a male who was agitated and exhibiting unusual behavior to a local hospital. Upon arrival at the hospital, his body temperature was 105.5 degrees Fahrenheit and his blood pH was 6.7. Clinical laboratory analysis revealed elevated troponins, rhabdomyolysis, hypoglycemia, hepatic and renal injury, respiratory failure and disseminated intravascular coagulation...
January 30, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28127410/spectroscopic-characterization-and-crystal-structures-of-two-cathinone-derivatives-n-ethyl-2-amino-1-phenylpropan-1-one-ethcathinone-hydrochloride-and-n-ethyl-2-amino-1-4-chlorophenyl-propan-1-one-4-cec-hydrochloride
#17
Piotr Kuś, Joachim Kusz, Maria Książek, Ewelina Pieprzyca, Marcin Rojkiewicz
Comprehensive chemical characterization for two cathinone derivatives, N-ethyl-2-amino-1-phenylpropan-1-one (ethcathinone) hydrochloride and N-ethyl-2-amino-1-(4-chlorophenyl)-propan-1-one (4-chloroethcathinone, 4-CEC) hydrochloride, in material seized by drug enforcement agencies was performed by nuclear magnetic resonance (NMR) spectroscopy, infrared spectroscopy, gas chromatography-mass spectrometry in positive electron ionization mode, liquid chromatography-mass spectrometry in positive electrospray ionization mode and X-ray crystallography...
2017: Forensic Toxicology
https://www.readbyqxmd.com/read/28124803/employing-two-stage-derivatisation-and-gc-ms-to-assay-for-cathine-and-related-stimulant-alkaloids-across-the-celastraceae
#18
Luke R Tembrock, Corey D Broeckling, Adam L Heuberger, Mark P Simmons, Frank R Stermitz, Jessica M Uvarov
INTRODUCTION: Catha edulis (qat, khat, mirra) is a woody plant species that is grown and consumed in East Africa and Yemen for its stimulant alkaloids cathinone, cathine and norephedrine. Two Celastraceae species, in addition to qat, have been noted for their stimulant properties in ethnobotanical literature. Recent phylogenetic reconstructions place four genera in a clade sister to Catha edulis, and these genera are primary candidates to search for cathine and related alkaloids. OBJECTIVE: Determine if cathine or related alkaloids are present in species of Celastraceae other than Catha edulis...
January 26, 2017: Phytochemical Analysis: PCA
https://www.readbyqxmd.com/read/28108082/analysis-of-drugs-of-abuse-in-human-plasma-using-microextraction-by-packed-sorbents-and-ultra-high-performance-liquid-chromatography
#19
P Fernández, M González, M Regenjo, A M Ares, A M Fernández, R A Lorenzo, A M Carro
A miniaturized and simple method based on digitally programmed microextraction by packed sorbent (eVol(®)-MEPS) coupled to ultra-performance liquid chromatography (UPLC) has been developed for quantitative determination of three synthetic cathinones and seven conventional drugs of abuse and metabolites. The influence of several extraction parameters, such as washing and elution solvents were tested. In addition important variables affecting MEPS performance, namely sample volume, sorbent drying time, washing solvent volume, elution volume, number of extraction cycles, sorbent phase and pH, were evaluated using an asymmetrical screening design...
February 17, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28088088/prevalence-of-new-psychoactive-substances-in-northeast-asia-from-2007-to-2015
#20
Junhui Lee, Songhee Yang, Yujin Kang, Eunyoung Han, Ling-Yi Feng, Jih-Heng Li, Heesun Chung
The proliferation of new psychoactive substances (NPS) has been a global trend in drug abuse and its regulation has been a worldwide concern. There is no doubt that it is necessary to share information related to these emerging substances between countries and continents for the effective regulation of NPS. With efforts for the efficient regulation of NPS, many studies and information have been published for the prevalence of NPS in the United States and other countries in Europe and Oceania. However, there is lack of information available for the prevalence of NPS in Asian and African countries...
October 20, 2016: Forensic Science International
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