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https://www.readbyqxmd.com/read/28220701/deconstructed-analogs-of-bupropion-reveal-structural-requirements-for-transporter-inhibition-versus-substrate-induced-neurotransmitter-release
#1
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
#2
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
#3
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...
February 16, 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
#4
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...
February 7, 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
#5
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
#6
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
#7
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...
February 6, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28163218/atypical-dopamine-efflux-caused-by-3-4-methylenedioxypyrovalerone-mdpv-via-the-human-dopamine-transporter
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
https://www.readbyqxmd.com/read/28087976/the-role-of-diode-array-ultraviolet-detection-for-the-identification-of-synthetic-cathinones
#15
Walter F Rowe, Ioan Marginean, Stephanie Carnes, Ira S Lurie
The utility of diode array UV detection for aiding in the identification of synthetic cathinones, including different sub classes and positional isomers is presented. For 35 synthetic cathinones' unique UV spectra are obtained for seven sub classes including mostly beta ketones, where position and type of substitution on benzene rings give rise to differences in UV maxima and relative intensity of the spectral bands. This aspect is key to distinguishing positional isomers which contain differences in R substitution (mono and di) around the benzene ring, which provides complementary information to electron ionization mass spectrometry, where the latter technique cannot distinguish between these types of positional isomers...
January 14, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28076917/multi-organ-dysfunction-due-to-bath-salts-are-we-aware-of-this-entity
#16
Rohith Valsalan, Benoj Varghese, Diya Soman, Jonathan Buckmaster, Steven Yew, David Cooper
Methylenedioxypyrovalerone (MDPV) is a synthetic, cathinone-derivative, central nervous system stimulant taken to produce a cocaine- or methamphetamine-like high. Physical manifestations include tachycardia, hypertension, arrhythmias, hyperthermia, sweating, rhabdomyolysis, hyperkalaemia, disseminated intravascular coagulation, oliguria and seizures. We report a patient who presented with severe metabolic acidosis, multi-organ dysfunction, rhabdomyolysis, hyperkalaemia and seizures. This case highlights that even though a urine drug screen for routine psychostimulant drugs is negative, clinicians need to be vigilant about the adverse effects of MDPV as a possible cause of multi-organ dysfunction...
January 2017: Internal Medicine Journal
https://www.readbyqxmd.com/read/28075189/11-analytically-confirmed-cases-of-mexedrone-use-among-polydrug-users
#17
Liam Roberts, Loretta Ford, Neel Patel, J Allister Vale, Sally M Bradberry
INTRODUCTION: Mexedrone, 3-methoxy-2-(methylamino)-1-(4-methylphenyl)propan-1-one, is the alpha-methoxy-derivative of mephedrone (4-methyl-N-methyl cathinone). Mexedrone inhibits the re-uptake of serotonin and dopamine in a dose-dependent manner and has affinity for serotonin and dopamine membrane transporters and receptors (5-HT2 and D2 receptors), producing sympathomimetic effects similar to amfetamines. To date there are no published clinical reports on mexedrone use that are analytically confirmed...
March 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28074662/misuse-of-2-ethylamino-1-4-methylphenyl-1-pentanone-4-meap-a-synthetic-cathinone
#18
Anneka Varma, Neel Patel, Loretta Ford, Rachel Jones, J Allister Vale
No abstract text is available yet for this article.
March 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28070621/behavioral-evidence-for-the-abuse-potential-of-the-novel-synthetic-cathinone-alpha-pyrrolidinopentiothiophenone-pvt-in-rodents
#19
Jae Hoon Cheong, Mee Jung Choi, Choon-Gon Jang, Yong Sup Lee, Sooyeun Lee, Hee Jin Kim, Joung-Wook Seo, Seong Shoon Yoon
RATIONALE: Synthetic cathinones are chemical derivatives of cathinone that are pharmacologically similar to cocaine and methamphetamine. Recently, abuse of synthetic cathinones among young people has increased. OBJECTIVES: The present study aimed to characterize the behavioral effects of alpha-pyrrolidinopentiothiophenone (PVT), an analog of alpha-pyrrolidinovalerophenone and second-generation synthetic cathinone, as well as to evaluate its abuse potential, using conditioned place preference, intravenous self-administration (SA), and drug discrimination paradigms in rodent models...
January 9, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28067045/neurotoxicity-of-%C3%AE-keto-amphetamines-deathly-mechanisms-elicited-by-methylone-and-mdpv-in-human-dopaminergic-sh-sy5y-cells
#20
Maria João Valente, Maria de Lourdes Bastos, Eduarda Fernandes, Félix Carvalho, Paula Guedes de Pinho, Márcia Carvalho
Synthetic cathinones (β-keto amphetamines) act as potent CNS stimulants similarly to classical amphetamines, which raise concerns about their potential neurotoxic effects. The present in vitro study aimed to explore and compare the mechanisms underlying the neurotoxicity of two commonly abused cathinone derivatives, 3,4-methylenedioxymethcathinone (methylone) and 3,4-methylenedioxypyrovalerone (MDPV), with those of 3,4-methylenedioxymethamphetamine (MDMA), using undifferentiated and differentiated SH-SY5Y cells...
January 26, 2017: ACS Chemical Neuroscience
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