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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 60minutes post treatment...
October 20, 2016: Toxicology Letters
Sandra Nordmann, Thomas Nefau, Joëlle Micallef, Catherine Duplessy, Jean-Christophe Catusse, Elisabeth Frauger
OBJECTIVE: The aim of this study is to analyze the residual content of used syringes. METHODS: Used syringes were collected in March 2014 at 9 sites in Marseille (automatic injection kit dispensers, streets, drug-user risk reduction centers [Centres d'accueil et d'accompagnement à la réduction de risques pour usagers de drogues [CAARUD]). Several substances (n=28) were investigated using liquid chromatography and mass spectrometry method. RESULTS: On average, 2±1 substances in each syringe were found among 254 syringes analyzed...
October 19, 2016: Thérapie
Hussein M Ageely, Ahmed E Agag, Syam Mohan, Atef Shehata
BACKGROUND: Khat (Catha edulis) is a controversial plant having a euphoretic effect, at the same time part of culture in many countries such as Africa and Arabian Peninsula. The presence of amphetamine-like substance, cathinone and cathine make this plant banned in many countries. Many neurological and other system related studies have been carried out in this plant, but the lack of toxicity studies are there especially the mechanism. OBJECTIVE: In this study, Madin-Darby Bovine Kidney cell line was used as an in vitro model to study the cell death mechanism...
July 2016: Pharmacognosy Magazine
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
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
The recreational use of synthetic cathinones has grown rapidly which prompted concerns from legal authorities and health care providers. However, in response to legislative regulations, synthesis of novel synthetic cathinones by introducing substituents in cathinone molecule has dramatically increased the diversity of these substances. Based on current trends, the aromatic ring is one of the popular sites in cathinone molecule being explored by designer-type modifications. In this study, we designed and synthesized a novel synthetic cathinone, 2-(methylamino)-1-(naphthalen-2-yl) propan-1-one (BMAPN), which has a naphthalene substituent on the aromatic ring...
October 11, 2016: Behavioural Brain Research
Jadwiga Nędza, Renata Polaniak, Rafał J Bułdak, Milena Majchrzak, Joanna Margasiń-Ska, Marcin Rojkiewicz, Rafał Celiński, Elżbieta Grochowska-Niedworok
Recently, there has been an increase in the consumption of designer drugs, substances aimed at producing psychoactive, energizing, euphoric or anesthetic effects. Designer drugs are substitutes of actual narcotics, whose possession is banned under Polish law according to the Act of 29 July 2005. The latest reports suggest that the number of synthetic psychoactive substances is increasing. In the span of 2012, a total of 28 new synthetic cannabinoids were discovered in member states of the European Union. Synthetic psychoactive substances appear in different forms on the market: tablets (often very colourful and interestingly-shaped), seeds, dried product (sprayed with synthetic substance and redried), crystals or powder...
July 29, 2016: Polski Merkuriusz Lekarski: Organ Polskiego Towarzystwa Lekarskiego
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
G Jeanne, D Purper-Ouakil, H Rigole, N Franc
AIM: There have been significant changes in adolescent consumption habits over the past fifteen years. New molecules have been synthesized, new devices created and a number of products have increased in popularity; and as a result clinicians sometimes lack information. We chose to focus on this population because of its vulnerability, as adolescents show low sensitivity to long-term outcomes of their actions and may be easily influenced by peers as regards experimentation of new drugs...
October 6, 2016: L'Encéphale
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 blood pressure (BP) and heart rate (HR). On test days, rats were placed individually in standard isolation cubicles...
October 7, 2016: British Journal of Pharmacology
Douglas A Smith, Bruce E Blough, Matthew L Banks
RATIONALE: Synthetic cathinones have emerged as the newest class of abused monoamine transporter substrates. Structurally, these compounds are all beta-ketone amphetamine (cathinone) analogs. Whether synthetic cathinone analogs produce differential behavioral effects from their amphetamine analog counterparts has not been systematically examined. Preclinical drug discrimination procedures have been useful for determining the structure activity relationships (SARs) of abused drugs; however, direct comparisons between amphetamine and cathinone analogs are lacking and, in particular, in non-human primate models...
October 5, 2016: Psychopharmacology
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
S Stevens Negus, Matthew L Banks
Many cathinone analogs act as substrates or inhibitors at dopamine, norepinephrine, and serotonin transporters (DAT, NET, SERT, respectively). Drug selectivity at DAT vs. SERT is a key determinant of abuse potential for monoamine transporter substrates and inhibitors, such that potency at DAT > SERT is associated with high abuse potential, whereas potency at DAT < SERT is associated with low abuse potential. Quantitative structure-activity relationship (QSAR) studies with a series of 4-substituted methcathinone analogs identified volume of the 4-position substituent on the methcathinone phenyl ring as one structural determinant of both DAT vs...
October 1, 2016: Current Topics in Behavioral Neurosciences
Lisham Ashrafioun, Francis A Bonadio, Kyoung Deok Baik, Stacey L Bradbury, Victoria L Carhart, Nicole A Cross, Alan K Davis, Margaret Feuille, Anna R Harper, Jennifer H Lackey, Brent Lang, Kirstin J Lauritsen, Jaclyn Leith, Lawrence A Osborn, Harold Rosenberg, Jacob Stock, Mariya Zaturenskaya
Given the variety and potential toxicity of synthetic cathinones, clinicians and educators would benefit from information about patterns of and motivations for use, frequency of psychosocial consequences, and experience of acute subjective effects. We administered a comprehensive, web-based survey to 104 recreational users of synthetic cathinones. Sixty percent of respondents consumed synthetic cathinones once or more per month, usually snorting or swallowing these drugs, typically at home, usually with others, customarily during the evening and nighttime hours, and often in combination with another drug such as alcohol or marijuana...
September 28, 2016: Journal of Psychoactive Drugs
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
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
Ling-Yi Feng, Wen-Jing Yu, Wei-Ting Chang, Eunyoung Han, Heesun Chung, Jih-Heng Li
BACKGROUND: Illegal drug use has long been a global concern. Taiwan and Korea are geographically adjacent and both countries have experienced the illegal use problems of methamphetamine, a predominant prototype of New Psychoactive Substances (NPS). NPS, a term coined by the United Nations Office on Drugs and Crime (UNODC) in recent years, have not been scrutinized for their safety and may become a new threat to public health and security worldwide. To conduct evidence-based drug policy, it is imperative to estimate the trend and pattern of illegal drug use...
2016: Substance Abuse Treatment, Prevention, and Policy
Joseph J Palamar, Patricia Acosta, Danielle C Ompad, Charles M Cleland
BACKGROUND: Ecstasy (MDMA) use has regained popularity in the United States, particularly in the form of "Molly," which is often marketed as pure MDMA. Surveys have generally not included "Molly" in the definition of ecstasy, so rates of use may be underestimated. As popularity of ecstasy increases, research is needed to examine use among those at highest risk for use-nightlife attendees. METHODS: We surveyed 679 young adults (age 18-25) entering nightclubs and festivals holding electronic dance music (EDM) parties in New York City in 2015...
September 23, 2016: Substance Use & Misuse
Dalton T Snyder, Patrick W Fedick, R Graham Cooks
There are many cases in which limited information is obtained from a single stage of tandem mass spectrometry (MS(2) or MS/MS). For example, isomeric cathinones give similar product ion MS(2) spectra, but they can be differentiated by their unique MS(3) fragments. Other drugs such as oxycodone and noroxycodone lose water in a single-stage tandem mass spectrometry experiment but give rich structural information in subsequent stages, as do many peptides. Here we utilize multigenerational collision-induced dissociation (CID) on a miniature mass spectrometer and emphasize useful applications...
October 4, 2016: Analytical Chemistry
Minaleshewa Atlabachew, Sandra Combrinck, Alvaro M Viljoen, Josias H Hamman, Chrisna Gouws
ETHNOPHARMACOLOGICAL RELEVANCE: Khat, the leaves of Catha edulis, is used as a "natural amphetamine-like" stimulant in eastern and southern Africa, as well as in the Arabian Peninsula. Leaves are masticated to elicit a state of euphoria. Although the psychostimulatory effects of the leaves are attributed to the presence of phenylpropylamino alkaloids (i.e. cathinone, cathine and norephedrine) the extent of permeation of these alkaloids across the oral and intestinal mucosa has not been established...
September 8, 2016: Journal of Ethnopharmacology
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
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