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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/27908258/neurotoxicity-induced-by-mephedrone-an-up-to-date-review
#2
Flaminia Pantano, Roberta Tittarelli, Giulio Mannocchi, Roberta Pacifici, Alessandro di Luca, Francesco Paolo Busardò, Enrico Marinelli
Mephedrone is a β-ketoamphetamine belonging to the family of synthetic cathinones, an emerging class of designer drugs known for their hallucinogenic and psychostimulant properties as well as for their abuse potential. The aim of this review was to examine the emerging scientific literature on the possible mephedrone-induced neurotoxicity, yet not well defined due to the limited number of experimental studies, mainly carried on animal models. Relevant scientific articles were identified from international literature databases (Medline, Scopus, etc...
November 30, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27896377/self-administration-and-behavioral-economics-of-second-generation-synthetic-cathinones-in-male-rats
#3
S L Huskinson, J E Naylor, E A Townsend, J K Rowlett, B E Blough, K B Freeman
RATIONALE: Synthetic cathinones have become increasingly available as drugs of abuse. Distribution of these drugs is made possible by altering the chemical structures of prohibited cathinones and marketing them under misleading labels. Very little is known about the relative reinforcing effectiveness of new synthetic cathinones relative to known drugs of abuse. OBJECTIVE: We examined self-administration of three second-generation synthetic cathinones: alpha-pyrrolidinopentiophenone (alpha-PVP), 4-methyl-N-ethylcathinone (4-MEC), and 4-methyl-alpha-pyrrolidinopropiophenone (4-MePPP) relative to methamphetamine...
November 28, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27891211/from-linked-open-data-to-molecular-interaction-studying-selectivity-trends-for-ligands-of-the-human-serotonin-and-dopamine-transporter
#4
Barbara Zdrazil, Eva Hellsberg, Michael Viereck, Gerhard F Ecker
Retrieval of congeneric and consistent SAR data sets for protein targets of interest is still a laborious task to do if no appropriate in-house data set is available. However, combining integrated open data sources (such as the Open PHACTS Discovery Platform) with workflow tools now offers the possibility of querying across multiple domains and tailoring the search to the given research question. Starting from two phylogenetically related protein targets of interest (the human serotonin and dopamine transporters), the whole chemical compound space was explored by implementing a scaffold-based clustering of compounds possessing biological measurements for both targets...
September 14, 2016: MedChemComm
https://www.readbyqxmd.com/read/27876594/successful-control-of-a-large-outbreak-of-hiv-infection-associated-with-injection-of-cathinone-derivatives-in-tel-aviv-israel
#5
Eugene Katchman, Ronen Ben-Ami, Michal Savyon, Daniel Chemtob, Boaz Avidor, Asaf Wasserman, Irena Zeldis, Shirley Girshengorn, Ziva Amitai, Rivka Sheffer, Dan Turner
OBJECTIVES: Outbreaks of HIV infection have been linked to injectable drug abuse, but specific triggers often remain obscure. We report on an outbreak of primary HIV infection among people who inject drugs (PWID) in Tel Aviv, associated with a local shift in drug-use practices. METHODS: A cluster of primary HIV infection cases in PWID was detected in May 2012. Retrospective and prospective multi-hospital case finding was initiated. PWID were interviewed and risk factors for primary HIV infection were identified...
November 19, 2016: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/27871070/khat-catha-edulis-and-obesity-a-scoping-review-of-animal-and-human-studies
#6
Mustafa Ahmed Alshagga, Mohammed Abdullah Alshawsh, Atefehalsadat Seyedan, Abdulsamad Alsalahi, Yan Pan, Suresh Kumar Mohankumar, Abdolgodose Alkebsi, Saba Kassim, Zahurin Mohamed
BACKGROUND: Khat (Catha edulis) is a plant that is deeply rooted in the cultural life of East African and Southwestern Arabian populations. Prevalent traditional beliefs about khat are that the plant has an effect on appetite and body weight. SUMMARY: This review assesses the accumulated evidences on the mutual influence of monoamines, hormones and neuropeptides that are linked to obesity. A few anti-obesity drugs that exert their mechanisms of action through monoamines are briefly discussed to support the notion of monoamines being a critical target of drug discovery for new anti-obesity drugs...
November 22, 2016: Annals of Nutrition & Metabolism
https://www.readbyqxmd.com/read/27863142/identification-and-analytical-characterization-of-nine-synthetic-cathinone-derivatives-n-ethylhexedrone-4-cl-pentedrone-4-cl-%C3%AE-eapp-propylone-n-ethylnorpentylone-6-meo-bk-mdma-%C3%AE-pihp-4-cl-%C3%AE-php-and-4-f-%C3%AE-php
#7
Cuimei Liu, Wei Jia, Tao Li, Zhendong Hua, Zhenhua Qian
Clinical and forensic toxicology laboratories are continuously confronted by analytical challenges when dealing with the new psychoactive substances phenomenon. In this study, the analytical characterization of nine synthetic cathinones is described: 2-(ethylamino)-1-phenylhexan-1-one (N-ethylhexedrone 1), 1-(4-chlorophenyl)-2-(methylamino)pentan-1-one (4-Cl-pentedrone 2), 1-(4-chlorophenyl)-2-(ethylamino)pentan-1-one (4-Cl-α-EAPP 3), 1-(3,4-methylenedioxyphenyl)-2-propylaminopropan-1-one (propylone 4), 1-(3,4-methylenedioxyphenyl)-2-ethylaminopentan-1-one (N-ethylnorpentylone 5), 1-(6-methoxy-3,4-methylenedioxyphenyl)-2-methylaminopropan-1-one (6-MeO-bk-MDMA 6), 4-methyl-1-phenyl-2-(pyrrolidin-1-yl)pentan-1-one (α-PiHP 7), 1-(4-chlorophenyl)-2-(pyrrolidin-1-yl)hexan-1-one (4-Cl-α-PHP 8), and 1-(4-fluorophenyl)-2-(pyrrolidin-1-yl)hexan-1-one (4-F-α-PHP 9)...
November 9, 2016: Drug Testing and Analysis
https://www.readbyqxmd.com/read/27860344/combined-simulation-and-mutation-studies-to-elucidate-selectivity-of-unsubstituted-amphetamine-like-cathinones-at-the-dopamine-transporter
#8
Amir Seddik, Daan P Geerke, Thomas Stockner, Marion Holy, Oliver Kudlacek, Nicholas V Cozzi, Arnold E Ruoho, Harald H Sitte, Gerhard F Ecker
The dopamine and serotonin transporter proteins (DAT, SERT) play a vital role in behavior and mental illness. Although their substrate transport has been studied extensively, the molecular basis of their selectivity is not completely understood yet. In this study, we exploit molecular dynamics simulations combined with mutagenesis studies to shed light on the driving factors for DAT-over-SERT selectivity of a set of cathinones. Results indicate that these compounds can adopt two binding modes of which one is more favorable...
November 8, 2016: Molecular Informatics
https://www.readbyqxmd.com/read/27851549/1914-synthetic-cathinone-inhalation-resulting-in-diffuse-alveolar-hemorrhage
#9
Masakazu Nitta, Natsuo Kamimura, Hiroshi Endoh
No abstract text is available yet for this article.
December 2016: Critical Care Medicine
https://www.readbyqxmd.com/read/27836413/development-of-a-new-field-test-procedure-for-cocaine
#10
Kenji Tsujikawa, Yuko T Iwata, Hiroki Segawa, Tadashi Yamamuro, Kenji Kuwayama, Tatsuyuki Kanamori, Hiroyuki Inoue
The Scott test, widely used as the field test for cocaine, is performed in three steps. If a sample contains cocaine, blue precipitates appear in step 1, the precipitates are dissolved and the solution turns pink in step 2, and the lower layer turns blue in step 3. However, some pyrrolidine-type cathinones produce cocaine-like results when tested, necessitating modification of the test procedure. Filtration of the second-step mixture weakened the blue color in step 3; however, the blue color did not completely disappear...
November 1, 2016: Forensic Science International
https://www.readbyqxmd.com/read/27834146/recent-trends-in-analytical-methods-to-determine-new-psychoactive-substances-in-hair
#11
Chrystalla Kyriakou, Manuela Pellegrini, Oscar García-Algar, Enrico Marinelli, Simona Zaami
New Psychoactive Substances (NPS) belong to several chemical classes, including phenethylamines, piperazines, synthetic cathinones and synthetic cannabinoids. Development and validation of analytical methods for the determination of NPS both in traditional and alternative matrices is of crucial importance to study drug metabolism and to associate consumption to clinical outcomes and eventual intoxication symptoms. Among different biological matrices, hair is the one with the widest time window to investigate drug-related history and demonstrate past intake...
November 11, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27830576/structure-activity-relationships-of-synthetic-cathinones
#12
Richard A Glennon, Małgorzata Dukat
Until recently, there was rather little interest in the structure-activity relationships (SARs) of cathinone analogs because so few agents were available and because they represented a relatively minor drug abuse problem. Most of the early SAR was formulated on the basis of behavioral (e.g., locomotor and drug discrimination) studies using rodents. With the emergence on the clandestine market in the last few years of a large number of new cathinone analogs, termed "synthetic cathinones", and the realization that they likely act at dopamine, norepinephrine, and/or serotonin transporters as releasing agents (i...
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
#13
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/27808572/poisoning-to-%C3%AE-pyrrolidinovalerophenone-%C3%AE-pvp-a-synthetic-cathinone
#14
Neel Patel, Loretta Ford, Rachel Jones, Sally M Bradberry, J Allister Vale
No abstract text is available yet for this article.
November 3, 2016: Clinical Toxicology
https://www.readbyqxmd.com/read/27799294/structure-activity-relationships-of-substituted-cathinones-with-transporter-binding-uptake-and-release
#15
Amy J Eshleman, Katherine M Wolfrum, John F Reed, Sunyoung O Kim, Tracy Swanson, Robert A Johnson, Aaron J Janowsky
Synthetic cathinones are components of "bath salts" and have physical and psychological side effects including hypertension, paranoia, and hallucinations. Herein we report interactions of 20 "bath salt" components with human dopamine, serotonin, and norepinephrine transporters (hDAT, hSERT, and hNET, respectively) heterologously expressed in HEK 293 cells. Transporter inhibitors had nanomolar to micromolar affinities (Ki values) at radioligand binding sites, with relative affinities of hDAT>hNET>hSERT for α-PPP, α-PBP, α-PHP, PV-8, 3,4-MDPPP, 3,4-MDPBP, 4-MePPP, α-PVP, 4-MeO- α-PVP, α-PVT and pentedrone, and hDAT>hSERT>hNET for pentylone...
October 31, 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27798075/gc-ms-quantification-method-for-mephedrone-in-plasma-and-urine-application-to-human-pharmacokinetics
#16
Eulàlia Olesti, Mitona Pujadas, Esther Papaseit, Clara Pérez-Mañá, Óscar J Pozo, Magí Farré, Rafael de la Torre
Increasing consumption has been observed among young people of new psychoactive substances, including synthetic cathinone derivatives. The most well known of these is mephedrone whose use has been related to acute intoxication and fatality. Several methods able to detect mephedrone have been reported, although to date, none have been applied to human pharmacokinetic studies in a controlled setting. We developed a gas chromatography-mass spectrometry technique for mephedrone quantification in human plasma and urine...
October 23, 2016: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/27790823/the-new-designer-drug-buphedrone-produces-rewarding-properties-via-dopamine-d1-receptor-activation
#17
Ji-Hwan Oh, Ji-Young Hwang, Sa-Ik Hong, Shi-Xun Ma, Jee-Yeon Seo, Seok-Yong Lee, Hyoung-Chun Kim, Choon-Gon Jang
Substituted cathinones are synthetic analogs of the active components of natural products and are widely abused worldwide. However, the rewarding properties of these agents have not yet been evaluated. In this study, we investigated the abuse potential of buphedrone [2-(methylamino)-1-phenylbutan-1-one, α-methylamino-butyrophenone] and its effects on the mesolimbic dopaminergic system in mice using conditioned place preference (CPP) analysis, a self-administration test, a locomotor activity test, a behavioral sensitization test and Western blot analysis...
October 27, 2016: Addiction Biology
https://www.readbyqxmd.com/read/27790150/excited-delirium-and-sudden-death-a-syndromal-disorder-at-the-extreme-end-of-the-neuropsychiatric-continuum
#18
REVIEW
Deborah C Mash
Over the past decade, the excited delirium syndrome (ExDS) has raised continued controversy regarding the cause and manner of death of some highly agitated persons held in police custody, restrained or incapacitated by electrical devices. At autopsy, medical examiners have difficulty in identifying an anatomic cause of death, but frequently cite psychostimulant intoxication as a contributing factor. The characteristic symptoms of ExDS include bizarre and aggressive behavior, shouting, paranoia, panic, violence toward others, unexpected physical strength, and hyperthermia...
2016: Frontiers in Physiology
https://www.readbyqxmd.com/read/27784226/evidence-of-2-populations-of-mephedrone-abusers-by-hair-testing-application-to-4-forensic-expertises
#19
Pascal Kintz
New psychoactive substances are conquering the drug scene. Among these substances, cathinone derivatives have been observed since late in the year 2000. At that time, an increasing use of the synthetic cathinone mephedrone (4-methylmethcathinone) started to be observed, particularly among night clubbers. Although these new psychoactive drugs showed an appearance of safety, a growing amount of experiences on their secondary effects has been reported. Mephedrone for example is known to induce psychosis. Given the potential negative effects of mephedrone, the laboratory was asked to test for the drug in hair, a cumulative matrix that can document single, occasional or repetitive abuse of xenobiotics...
October 26, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27773724/cooling-down-the-bath-salts-carvedilol-attenuation-of-methylone-and-mephedrone-mediated-hyperthermia
#20
Luke C Zona, Gregory G Grecco, Jon E Sprague
The use of the synthetic cathinones ("bath salts"), methylone and mephedrone, has been associated with the development of life-threatening hyperthermia. To date, no direct pharmacological intervention to mitigate the hyperthermia induced by synthetic cathinones has been identified. Here, we investigated the effects of the non-selective α1 and β adrenergic receptor antagonist carvedilol (5mg/kg ip) on established hyperthermia mediated by methylone and mephedrone (30mg/kg sc) in Sprague-Dawley rats. Methylone and mephedrone induced a hyperthermic response that peaked 60min post treatment...
October 20, 2016: Toxicology Letters
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