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https://www.readbyqxmd.com/read/27896377/self-administration-and-behavioral-economics-of-second-generation-synthetic-cathinones-in-male-rats
#1
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/27418996/flakka-induced-prolonged-psychosis
#2
Craig Crespi
In South Florida, there has been a highly addictive new synthetic drug flooding the streets for people looking for a cheap high. Alpha-PVP, better known as Flakka, is an illegal substance that sells on the streets for as little as $5 a hit and delivers an instant high that can last from hours to days with lingering effects for weeks after it has been ingested. Although people use Flakka for its potential euphoric high, symptoms are known to easily escalate into frightening delusions, paranoid psychosis, extreme agitation, and a multitude of other altered mental states...
2016: Case Reports in Psychiatry
https://www.readbyqxmd.com/read/27237056/pharmacological-effects-of-methamphetamine-and-alpha-pvp-vapor-and-injection
#3
Julie A Marusich, Timothy W Lefever, Bruce E Blough, Brian F Thomas, Jenny L Wiley
Vaporizing drugs in e-cigarettes is becoming a common method of administration for synthetic cathinones and classical stimulants. Heating during vaporization can expose the user to a cocktail of parent compound and thermolytic degradants, which could lead to different toxicological and pharmacological effects compared to ingesting the parent compound alone via injection or nasal inhalation. This study examined the in vivo toxicological and pharmacological effects of vaporized and injected methamphetamine (METH) and α-pyrrolidinopentiophenone (α-PVP)...
July 2016: Neurotoxicology
https://www.readbyqxmd.com/read/27179320/temporal-trends-in-drug-use-in-adelaide-south-australia-by-wastewater-analysis
#4
Benjamin J Tscharke, Chang Chen, Jacobus P Gerber, Jason M White
Analysis of municipal wastewater for drug metabolites can reveal the scale of drug use within communities. An Australian city with a population of 1.2million inhabitants was assessed for 4 stimulants: cocaine, methamphetamine, 3.4-methylenedioxymethamphetamine (MDMA) and amphetamine; 6 opioids: codeine, morphine, heroin, fentanyl, oxycodone and methadone; 11 new psychoactive substances (NPS); benzylpiperazine (BZP), trifluoromethylphenylpiperazine (TFMPP), methcathinone, methylone, mephedrone, methylenedioxypyrovalerone (MDPV), alpha pyrrolidinopentiophenone (alpha-PVP), paramethoxyamphetamine (PMA), 25C-NBOMe, 25B-NBOMe, 25I-NBOMe; and cannabis, for up to four years between December 2011 and December 2015...
September 15, 2016: Science of the Total Environment
https://www.readbyqxmd.com/read/27060605/cocaine-like-discriminative-stimulus-effects-of-alpha-pyrrolidinovalerophenone-methcathinone-and-their-3-4-methylenedioxy-or-4-methyl-analogs-in-rhesus-monkeys
#5
Douglas A Smith, S Stevens Negus, Justin L Poklis, Bruce E Blough, Matthew L Banks
Synthetic cathinones are beta-ketone amphetamine analogs that have emerged as a heterogeneous class of abused compounds that function as either monoamine transporter substrates or inhibitors. Pre-clinical drug discrimination procedures are useful for interrogating structure-activity relationships of abuse-related drug effects; however, in vivo structure-activity relationship comparisons between synthetic cathinones with different mechanisms of action are lacking. The aim of the present study was to determine whether the cocaine-like discriminative stimulus effects of the monoamine transporter inhibitor alpha-pyrrolidinovalerophenone (alpha-PVP) and the monoamine transporter substrate methcathinone were differentially sensitive to 3,4-methylenedioxy and 4-methyl substitutions...
April 6, 2016: Addiction Biology
https://www.readbyqxmd.com/read/26964151/schedules-of-controlled-substances-extension-of-temporary-placement-of-10-synthetic-cathinones-in-schedule-i-of-the-controlled-substances-act-final-order
#6
(no author information available yet)
The Administrator of the Drug Enforcement Administration is issuing this final order to extend the temporary schedule I status of 10 synthetic cathinones pursuant to the temporary scheduling provisions of the Controlled Substances Act. The 10 substances are: 4-methyl-N-ethylcathinone (4-MEC); 4-methyl-alpha-pyrrolidinopropiophenone (4-MePPP); alpha-pyrrolidinopentiophenone ([alpha]-PVP); 1-(1,3-benzodioxol-5-yl)-2-(methylamino)butan-1-one (butylone); 2-(methylamino)-1-phenylpentan-1-one (pentedrone); 1-(1,3-benzodioxol-5-yl)-2-(methylamino)pentan-1-one (pentylone); 4-fluoro-N-methylcathinone (4-FMC); 3-fluoro-N-methylcathinone (3-FMC); 1-(naphthalen-2-yl)-2-(pyrrolidin-1-yl)pentan-1-one (naphyrone); and alpha-pyrrolidinobutiophenone ([alpha]-PBP) [hereinafter 4-MEC, 4-MePPP, [alpha]-PVP, butylone, pentedrone, pentylone, 4-FMC, 3-FMC, naphyrone, and [alpha]-PBP, respectively], including their optical, positional, and geometric isomers, salts, and salts of isomers...
March 4, 2016: Federal Register
https://www.readbyqxmd.com/read/26890319/suicide-attempt-with-a-mix-of-synthetic-cannabinoids-and-synthetic-cathinones-case-report-of-non-fatal-intoxication-with-ab-chminaca-ab-fubinaca-alpha-php-alpha-pvp-and-4-cmc
#7
Janez Klavž, Maksimiljan Gorenjak, Martin Marinšek
We report on a case of intoxication with a mix of new psychoactive substances. A 38-year-old male was brought to the emergency department (ED) following the ingestion of an unknown drug in a suicide attempt. During the transport, he became progressively more somnolent and unresponsive to painful stimuli. Urine and stomach content were collected on admission to be screened for drugs of abuse and medicinal drugs. After admission, the patient's next of kin presented five small grip seal plastic bags containing different powders/crystals, and they were sent for analysis along with urine and stomach content to the toxicology laboratory...
August 2016: Forensic Science International
https://www.readbyqxmd.com/read/26883685/detection-of-bath-salts-and-other-novel-psychoactive-substances-in-hair-samples-of-ecstasy-mdma-molly-users
#8
Joseph J Palamar, Alberto Salomone, Marco Vincenti, Charles M Cleland
BACKGROUND: Ecstasy (MDMA) in the US is commonly adulterated with other drugs, but research has not focused on purity of ecstasy since the phenomenon of "Molly" (ecstasy marketed as pure MDMA) arose in the US. METHODS: We piloted a rapid electronic survey in 2015 to assess use of novel psychoactive substances (NPS) and other drugs among 679 nightclub/festival-attending young adults (age 18-25) in New York City. A quarter (26.1%) of the sample provided a hair sample to be analyzed for the presence of select synthetic cathinones ("bath salts") and some other NPS...
April 1, 2016: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/25925780/in-vivo-potency-and-efficacy-of-the-novel-cathinone-%C3%AE-pyrrolidinopentiophenone-and-3-4-methylenedioxypyrovalerone-self-administration-and-locomotor-stimulation-in-male-rats
#9
Shawn M Aarde, Kevin M Creehan, Sophia A Vandewater, Tobin J Dickerson, Michael A Taffe
RATIONALE: Numerous substituted cathinone drugs have appeared in recreational use. This variety is often a response to legal actions; the scheduling of 3,4-methylenedioxypyrovalerone (MDPV; "bath salts") in the USA was followed by the appearance of the closely related drug α-pyrrolidinopentiophenone (alpha-PVP; "flakka"). OBJECTIVES: This study aimed to directly compare the efficacy and potency of alpha-PVP with that of MDPV. METHODS: Groups of male Wistar rats were trained in the intravenous self-administration (IVSA) alpha-PVP or MDPV under a fixed-ratio 1 schedule of reinforcement...
August 2015: Psychopharmacology
https://www.readbyqxmd.com/read/25707704/discriminative-stimulus-effects-of-second-generation-synthetic-cathinones-in-methamphetamine-trained-rats
#10
Jennifer E Naylor, Kevin B Freeman, Bruce E Blough, William L Woolverton, Sally L Huskinson
BACKGROUND: Synthetic cathinones are beta-ketophenethylamine analogs manufactured to avoid legal restrictions placed on illicit stimulants like methamphetamine. Regulating these "emerging" designer drugs require scientific evidence of abuse potential. METHODS: The present study evaluated the discriminative-stimulus effects of three synthetic cathinones, recently identified in commercial and confiscated products, in male Sprague-Dawley rats trained to discriminate methamphetamine (1...
April 1, 2015: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/25645132/fatal-poisoning-in-drug-addicts-in-the-nordic-countries-in-2012
#11
K Wiese Simonsen, H M E Edvardsen, G Thelander, I Ojanperä, S Thordardottir, L V Andersen, P Kriikku, V Vindenes, D Christoffersen, G J M Delaveris, J Frost
This report is a follow-up to a study on fatal poisoning in drug addicts conducted in 2012 by a Nordic working group. Here we analyse data from the five Nordic countries: Denmark, Finland, Iceland, Norway and Sweden. Data on sex, number of deaths, places of death, age, main intoxicants and other drugs detected in the blood were recorded. National data are presented and compared between the Nordic countries and with data from similar studies conducted in 1991, 1997, 2002 and 2007. The death rates (number of deaths per 100,000 inhabitants) increased in drug addicts in Finland, Iceland and Sweden but decreased in Norway compared to the rates in earlier studies...
March 2015: Forensic Science International
https://www.readbyqxmd.com/read/24418703/new-recreational-drug-1-phenyl-2-1-pyrrolidinyl-1-pentanone-alpha-pvp-activates-central-nervous-system-via-dopaminergic-neuron
#12
Asuka Kaizaki, Sachiko Tanaka, Satoshi Numazawa
1-phenyl-2-(1-pyrrolidinyl)-1-pentanone (α-PVP) is a new designer drug of the cathinone type. People who have taken drugs containing α-PVP or other synthetic cathinone reportedly lose consciousness, develop difficulty breathing, and at worst case, die. However, the mechanism underlying α-PVP-induced neurotoxicity is unknown. The objective of the present study was to investigate the effect of α-PVP on the central nervous system (CNS) and compare its neurotoxicity with that of methamphetamine (METH) in mice...
February 2014: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/23361867/analysis-of-synthetic-cathinones-commonly-found-in-bath-salts-in-human-performance-and-postmortem-toxicology-method-development-drug-distribution-and-interpretation-of-results
#13
Laureen J Marinetti, Heather M Antonides
To date, the Toxicology Section of the Montgomery County Coroner's Office/Miami Valley Regional Crime Laboratory has identified six synthetic cathinones, commonly found in bath salt products, in 43 cases. Thirty-two cases will be reviewed here, including all of the postmortem cases, all of the human performance cases that had blood specimens submitted, and one urine-only human performance case. The following compounds have been confirmed: 3,4-methylenedioxypyrovalerone (MDPV), 3,4-methylenedioxymethcathinone (methylone), pyrovalerone, pentylone, alpha-pyrrolidinopentiophenone (alpha-PVP) and methedrone...
April 2013: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/11103807/antitumor-activity-of-tumor-necrosis-factor-alpha-conjugated-with-polyvinylpyrrolidone-on-solid-tumors-in-mice
#14
COMPARATIVE STUDY
H Kamada, Y Tsutsumi, Y Yamamoto, T Kihira, Y Kaneda, Y Mu, H Kodaira, S I Tsunoda, S Nakagawa, T Mayumi
We attempted the development of a novel polymer conjugation to further improve the therapeutic potency of antitumor cytokines compared with PEGylation for clinical application. Compared with native tumor necrosis factor (TNF)-alpha in vitro, specific bioactivities of polyvinyl-pyrrolidone (PVP)-modified TNF-alphas (PVP-TNF-alphas) were decreased by increasing the degree of PVP attachment. PVP-TNF-alpha fraction 3, Mr 101,000, had the most effective antitumor activity of the various PVP-TNF-alphas in vivo. PVP-TNF-alpha fraction 3 had >200-fold higher antitumor effect than native TNF-alpha, and the antitumor activity of PVP-TNF-alpha fraction 3 was >2-fold higher than that of MPEG-TNF-alpha (Mr 108,000), which had the highest antitumor activity among the polyethylene glycol (PEG)-conjugated TNF-alphas...
November 15, 2000: Cancer Research
https://www.readbyqxmd.com/read/10198233/molecular-design-of-conjugated-tumor-necrosis-factor-alpha-synthesis-and-characteristics-of-polyvinyl-pyrrolidone-modified-tumor-necrosis-factor-alpha
#15
H Kamada, Y Tsutsumi, S Tsunoda, T Kihira, Y Kaneda, Y Yamamoto, S Nakagawa, Y Horisawa, T Mayumi
We conjugated tumor necrosis factor-alpha (TNF-alpha) with the synthetic polymeric modifier polyvinyl pyrrolidone (PVP) to facilitate its clinical use for anti-tumor therapy. TNF-alpha was chemically conjugated with the terminal carboxyl-bearing PVP at one end of its main chain, which was radically polymerized via the formation of an amide bond between the lysine amino groups of TNF-alpha and carboxyl group of PVP. In vitro specific bioactivity of PVP-conjugated TNF-alpha (PVP-TNF-alpha) relative to that of native TNF-alpha gradually decreased with increases in the degree of PVP attachment...
April 13, 1999: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/9794206/nonviral-interferon-alpha-gene-therapy-inhibits-growth-of-established-tumors-by-eliciting-a-systemic-immune-response
#16
M Coleman, S Muller, A Quezada, S K Mendiratta, J Wang, N M Thull, J Bishop, M Matar, J Mester, F Pericle
A plasmid expression system encoding murine IFN-alpha4 and complexed with a protective interactive noncondensing polymeric (PINC) delivery system was used for in vivo immunotherapy treatment of an immunogenic murine renal cell carcinoma, Renca, and a nonimmunogenic mammary adenocarcinoma, TS/A. Mice bearing established tumors were treated with IFN-alpha/polyvinylpyrrolidone (PVP) expression complexes via direct intratumoral injection. Up to 100% inhibition of tumor growth was observed in the treated mice. By using an optimal dose of 96 and 48 microg of formulated IFN-alpha plasmid for the treatment of Renca and TS/A, respectively, 30% (Renca) and 10% (TS/A) of the treated animals remained tumor free...
October 10, 1998: Human Gene Therapy
https://www.readbyqxmd.com/read/3819864/macrophage-function-as-studied-by-the-clearance-of-125i-labeled-polyvinylpyrrolidone-in-iron-deficient-and-iron-replete-mice
#17
S Kuvibidila, S Wade
This study evaluated the effects of iron deficiency and iron repletion on in vivo macrophage function determined by the clearance of 125I-labeled polyvinylpyrrolidone (PVP). Two experiments were done. There were four groups of C57BL/6 female mice in experiment 1: the iron-deficient (ID), pair-fed (PF), control (C) and the high iron (HI) groups. In experiment 2, there were three ID groups (severe to moderate anemia), three PF, one C and four ID groups that were fed adequate iron for 14 (R-14), 7 (R-7), 3 (R-3) days before or on the day of PVP injection (R-0)...
January 1987: Journal of Nutrition
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