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https://www.readbyqxmd.com/read/28637216/qualitative-analysis-and-detection-of-the-pyrolytic-products-of-jwh-018-and-11-additional-synthetic-cannabinoids-in-the-presence-of-common-herbal-smoking-substrates
#1
Stephen Raso, Suzanne Bell
Synthetic cannabinoids have become a ubiquitous challenge in forensic toxicology and seized drug analysis. Thermal degradation products have yet to be identified and evaluated for toxicity in comparison to parent and metabolic compounds. An investigation into these pyrolytic products, as the major route of ingestion is inhalation, may produce additional insight to understand the toxicity of synthetic cannabinoids. The pyrolysis of JWH-018 and 11 additional synthetic cannabinoids and six herbal plant substrates were conducted using an in-house constructed smoking simulator...
June 20, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28601726/identification-and-quantification-of-synthetic-cannabinoids-in-spice-like-herbal-mixtures-update-of-the-german-situation-in-early-2017
#2
Ludger Ernst, Kai Brandhorst, Uli Papke, Anna Altrogge, Simone Zodel, Nico Langer, Till Beuerle
In February 2017, eleven "Spice-like" products (14 individual packages including replicates) from German language internet shops were analyzed. In total, three different synthetic cannabinoids (SCs) were identified by gas-chromatography-mass spectrometry (GC-MS), namely MDMB-CHMICA and two, so far only partially described compounds, 5F-Cumyl-P7AICA and Cumyl-PeGACLONE. All analyzed products contained only one synthetic cannabinoid as active ingredient. 5F-Cumyl-P7AICA and Cumyl-PeGACLONE were subject to an in-depth characterization by nuclear magnetic resonance spectroscopy (NMR), electron ionization mass spectrometry (EI-MS), electrospray ionization tandem mass spectrometry (ESI-MS/MS), infrared and ultraviolet-visible spectroscopy (IR and UV/Vis)...
May 26, 2017: Forensic Science International
https://www.readbyqxmd.com/read/28597943/identification-of-eight-synthetic-cannabinoids-including-5f-akb48-in-seized-herbal-products-using-dart-tof-ms-and-lc-qtof-ms-as-nontargeted-screening-methods
#3
Katherine N Moore, Demetra Garvin, Brian F Thomas, Megan Grabenauer
Synthetic cannabinoids are sprayed onto plant material and smoked for their marijuana-like effects. Clandestine manufacturers modify synthetic cannabinoid structures by creating closely related analogs. Forensic laboratories are tasked with detection of these analog compounds, but targeted analytical methods are often thwarted by the structural modifications. Here, direct analysis in real time coupled to accurate mass time-of-flight mass spectrometry (DART-TOF-MS) in combination with liquid chromatography quadruple time-of-flight mass spectrometry (LC-QTOF-MS) are presented as a screening and nontargeted confirmation method, respectively...
June 9, 2017: Journal of Forensic Sciences
https://www.readbyqxmd.com/read/28597570/pharmaco-toxicological-effects-of-the-novel-third-generation-fluorinate-synthetic-cannabinoids-5f-adbinaca-ab-fubinaca-and-sts-135-in-mice-in-vitro-and-in-vivo-studies
#4
Isabella Canazza, Andrea Ossato, Fabrizio Vincenzi, Adolfo Gregori, Fabiana Di Rosa, Federica Nigro, Alessandro Rimessi, Paolo Pinton, Katia Varani, Pier Andrea Borea, Matteo Marti
INTRODUCTION: 5F-ADBINACA, AB-FUBINACA, and STS-135 are 3 novel third-generation fluorinate synthetic cannabinoids that are illegally marketed as incense, herbal preparations, or research chemicals for their psychoactive cannabis-like effects. METHODS: The present study aims at investigating the in vitro and in vivo pharmacological activity of 5F-ADBINACA, AB-FUBINACA, and STS-135 in male CD-1 mice, comparing their in vivo effects with those caused by the administration of Δ(9) -THC and JWH-018...
June 9, 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28533288/apparent-affinity-estimates-and-reversal-of-the-effects-of-synthetic-cannabinoids-am-2201-cp-47-497-jwh-122-and-jwh-250-by-rimonabant-in-rhesus-monkeys
#5
Lenka Hruba, Lance R McMahon
Synthetic cannabinoids have been prohibited due to abuse liability and toxicity. Four such synthetic cannabinoids, AM-2201, CP-47,497, JWH-122, and JWH-250, were tested for their capacity to produce CB1 receptor-mediated discriminative stimulus effects in two groups of rhesus monkeys. One group (n=4) discriminated ∆9-THC (0.1 mg/kg i.v.) and a second group (n=4) discriminated the cannabinoid antagonist rimonabant (1 mg/kg i.v.) while receiving 1 mg/kg/12 h of ∆9-THC. AM-2201, JWH-122, CP-47,497, JWH-250, and ∆9-THC increased ∆9-THC-lever responding...
May 22, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28469427/vaping-synthetic-cannabinoids-a-novel-preclinical-model-of-e-cigarette-use-in-mice
#6
Timothy W Lefever, Julie A Marusich, Brian F Thomas, Daniel G Barrus, Nicholas C Peiper, Richard C Kevin, Jenny L Wiley
Smoking is the most common route of administration for cannabis; however, vaping cannabis extracts and synthetic cannabinoids ("fake marijuana") in electronic cigarette devices has become increasingly popular. Yet, most animal models used to investigate biological mechanisms underlying cannabis use employ injection as the route of administration. This study evaluated a novel e-cigarette device that delivers aerosolized cannabinoids to mice. The effects of aerosolized and injected synthetic cannabinoids (CP 55,940, AB-CHMINACA, XLR-11, and JWH-018) in mice were compared in a battery of bioassays in which psychoactive cannabinoids produce characteristic effects...
2017: Substance Abuse: Research and Treatment
https://www.readbyqxmd.com/read/28467971/anti-proliferative-pro-apoptotic-and-anti-invasive-effect-of-ec-ev-system-in-human-osteosarcoma
#7
Francesca Punzo, Chiara Tortora, Daniela Di Pinto, Iolanda Manzo, Giulia Bellini, Fiorina Casale, Francesca Rossi
Osteosarcoma is the most common and aggressive bone tumor in children. The Endocannabinoid/Endovanilloid system has been proposed as anticancer target in tumor of different origins. This system is composed of two receptors (CB1 and CB2), the Transient Potential Vanilloid 1 (TRPV1) channel and their ligands and enzymes. CB1 is expressed mainly in central nervous system while CB2 predominantly on immune and peripheral cells. We investigated the effects of JWH-133 (CB2 agonist) and RTX (TRPV1 agonist) in six human Osteosarcoma cell lines: MG-63, U-2OS, MNNG/HOS, Saos-2, KHOS/NP, Hs888Lu, by Apoptosis and Migration-Assay...
April 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/28442584/apparent-cb1-receptor-rimonabant-affinity-estimates-combination-with-thc-and-synthetic-cannabinoids-in-the-mouse-in-vivo-triad-model
#8
Travis W Grim, Anthony J Morales, Brian F Thomas, Jenny L Wiley, Gregory W Endres, Sidney S Negus, Aron H Lichtman
Synthetic cannabinoids (SCs) represent an emerging class of abused drugs associated with psychiatric complications and other substantial health risks. These ligands are largely sold over the internet for human consumption presumably because of their high cannabinoid 1 receptor (CB1R) affinity and potency in eliciting similar pharmacological effects as Δ9-tetrahydrocannabinol (THC), while circumventing laws illegalizing this plant. Factors potentially contributing to the increased prevalence of SC abuse and related hospitalizations, such as increased CB1R efficacy and non-CB1R targets, highlight the need for quantitative pharmacological analyses to determine receptor mediation of the pharmacological effects of cannabinoids...
April 25, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28441106/jwh-122-consumption-adverse-effects-a-case-of-hallucinogen-persisting-perception-disorder-five-year-follow-up
#9
Maurizio Coppola, Raffaella Mondola
Synthetic cannabinoid receptor agonists are a heterogeneous group of psychotropic drugs functionally related to Δ9-tetrahydrocannabinol. These substances, marketed as cannabis substitutes, have been associated with numerous cases of severe intoxication and death across the world. In our article, we describe a case of hallucinogen persisting perception disorder developing in a natural cannabis user after consumption of JWH-122, a naphthoylindole largely used since 2010. Clinical symptomatology persisted for about four years and was alleviated through treatment with clonazepam...
April 25, 2017: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/28406320/underestimated-impact-of-novel-psychoactive-substances-laboratory-confirmation-of-recreational-drug-toxicity-in-oslo-norway
#10
Odd Martin Vallersnes, Per Sverre Persett, Elisabeth Leere Øiestad, Ritva Karinen, Fridtjof Heyerdahl, Knut Erik Hovda
CONTEXT: Recreational drug toxicity is frequent. Availability of new psychoactive substances is steadily increasing. However, data with verified analyses from clinical settings are limited. To evaluate the impact of novel psychoactive substances (NPS) on recreational drug toxicity in Oslo, Norway, we analysed samples from a selection of patients. METHODS: All the patients presenting with recreational drug toxicity at the Oslo Accident and Emergency Outpatient Clinic (OAEOC) and at the Oslo University Hospital (OUH) were registered from April through September 2014...
April 13, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28371432/determination-of-cannabinoid-and-synthetic-cannabinoid-metabolites-in-wastewater-by-liquid-liquid-extraction-and-ultrahigh-performance-supercritical-fluid-chromatography-tandem-mass-spectrometry
#11
Iria González-Mariño, Kevin V Thomas, Malcolm J Reid
For the first time, ultrahigh performance supercritical fluid chromatography (UHPSFC) coupled to tandem mass spectrometry has been used to determine cannabinoid and synthetic cannabinoid residues in wastewater. Combined with a downscaled version of the classical liquid-liquid extraction, the proposed method allows for the quantification of ∆9-tetrahydrocannabinol, three of its major metabolites (the monohydroxylated, the dihydroxylated and the carboxylated species) and four synthetic cannabinoid metabolites (from the JWH-series) at low ng L(-1) levels...
March 31, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28365515/pharmacokinetic-properties-of-the-synthetic-cannabinoid-jwh-018-and-of-its-metabolites-in-serum-after-inhalation
#12
Stefan W Toennes, Anna Geraths, Werner Pogoda, Alexander Paulke, Cora Wunder, Eef L Theunissen, Johannes G Ramaekers
Each year, synthetic cannabinoids are occurring in high numbers in the illicit drug market, but data on their pharmacology and toxicology are scarcely available. Therefore, a pilot study was performed to assess adverse effects of JWH-018, which is one of the oldest and best known synthetic cannabinoids. Six subjects inhaled smoke from 2 and 3mg JWH-018. The drug and nine of its metabolites were analyzed in their blood samples taken during the following 12h by liquid chromatography-mass spectrometry (LC-MSMS)...
June 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28340730/identification-and-determination-of-synthetic-cannabinoids-in-herbal-products-by-dry-film-attenuated-total-reflectance-infrared-spectroscopy
#13
Victor de la Asunción-Nadal, Sergio Armenta, Salvador Garrigues, Miguel de la Guardia
A new procedure has been developed for the identification and quantitative determination of synthetic cannabinoids in illicit herbal preparations. The methodology is based on the use of attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR) measurement of sample extracts with 2-propanol drying 5µL of the extracts onto the ATR crystal. The qualitative identification was carried out on the 2-propanol extract after identification of the herbal matrix, followed by its subtraction and using a cut-off criterion of 75%...
May 15, 2017: Talanta
https://www.readbyqxmd.com/read/28340702/selective-solid-phase-extraction-of-jwh-synthetic-cannabinoids-by-using-computationally-designed-peptides
#14
Marcello Mascini, Camilla Montesano, German Perez, Joseph Wang, Dario Compagnone, Manuel Sergi
The objective of the present work is to demonstrate a rational way to prepare selective sorbents able to extract simultaneously several structural analogs. For this purpose the binding specificity of two hexapeptides computationally designed (VYWLVW and YYIGGF) versus four synthetic cannabinoids Naphthalen-1-yl-(1-pentylindol-3-yl)methanone (JWH 018), naphthalen-1-yl-(1-butylindol-3-yl)methanone (JWH 073), (R)-(1-((1-methylpiperidin-2-yl)methyl)-1H-indol-3-yl)(naphthalen-1-yl)methanone (AM 1220) and (R)-(+)-[2,3-Dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1,2,3-de]-1,4-benzoxazin-6-yl]-1-napthalenylmethanone (WIN 55) was computationally studied and then experimentally tested by solid-phase extraction (SPE) clean-up and ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) analysis...
May 15, 2017: Talanta
https://www.readbyqxmd.com/read/28295787/an-exploratory-wastewater-analysis-study-of-drug-use-in-auckland-new-zealand
#15
Foon Yin Lai, Chris Wilkins, Phong Thai, Jochen F Mueller
INTRODUCTION AND AIMS: New Zealand is considered to have unusual drug use patterns by international standards. However, this understanding has largely been obtained from social surveys where respondents self-report use. The aim of this paper is to conduct the first wastewater study of drug use in Auckland. DESIGN AND METHODS: Wastewater sampling was completed from 2 May to 18 July 2014 at 2 Auckland wastewater treatment plants which service 1.3 million people. Samples were analysed for 17 drug residues by using liquid chromatography-tandem mass spectrometry...
March 12, 2017: Drug and Alcohol Review
https://www.readbyqxmd.com/read/28138895/the-impact-of-cb2-receptor-ligands-on-the-mk-801-induced-hyperactivity-in-mice
#16
Marta Kruk-Slomka, Izabela Banaszkiewicz, Grazyna Biala
It has been known that there is a relationship between cannabis use and schizophrenia-related symptoms; however, it can be a subject of controversy. The involvement of CB1 receptor ligands in the schizophrenia has already been revealed and confirmed. However, there is still lack of information concerning the role of CB2 receptors in the psychosis-like effects in mice and the further studies are needed.The aim of the present research was to study the role of the CB2 receptor ligands in the symptoms typical for schizophrenia...
April 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28130989/comparison-of-the-discriminative-stimulus-and-response-rate-effects-of-%C3%AE-9-tetrahydrocannabinol-and-synthetic-cannabinoids-in-female-and-male-rats
#17
Jenny L Wiley, Timothy W Lefever, Julie A Marusich, Rebecca M Craft
BACKGROUND: Women report greater sensitivity to the subjective effects of Δ(9)-tetrahydrocannabinol (THC). Similarly, female rodents tend to be more sensitive to some pharmacological effects of THC and synthetic cannabinoids. This study examined sex differences in discriminative stimulus and response rate effects of THC and synthetic cannabinoids in rats. METHODS: A cumulative dosing THC discrimination procedure was utilized to evaluate sex differences in the discriminative stimulus effects of THC and three synthetic cannabinoids: CP47,497, WIN55,212-2, and JWH-018...
March 1, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28130957/immunoassay-screening-in-urine-for-synthetic-cannabinoids-an-evaluation-of-the-diagnostic-efficiency
#18
Florian Franz, Verena Angerer, Hanna Jechle, Melanie Pegoro, Harald Ertl, Georg Weinfurtner, David Janele, Christian Schlögl, Matthias Friedl, Stefan Gerl, Reinhard Mielke, Ralf Zehnle, Matthias Wagner, Bjoern Moosmann, Volker Auwärter
BACKGROUND: The abuse of synthetic cannabinoids (SCs) as presumed legal alternative to cannabis poses a great risk to public health. For economic reasons many laboratories use immunoassays (IAs) to screen for these substances in urine. However, the structural diversity and high potency of these designer drugs places high demands on IAs regarding cross-reactivity of the antibodies used and detection limits. METHODS: Two retrospective studies were carried out in order to evaluate the capability of two homogenous enzyme IAs for the detection of currently prevalent SCs in authentic urine samples...
January 28, 2017: Clinical Chemistry and Laboratory Medicine: CCLM
https://www.readbyqxmd.com/read/28110689/cannabinoids-possible-agents-for-treatment-of-psoriasis-via-suppression-of-angiogenesis-and-inflammation
#19
Amir Hossein Norooznezhad, Fatemeh Norooznezhad
Psoriasis is a chronic skin disease also affecting other sites such as joints. This disease highly depends on inflammation and angiogenesis as well as other pathways. At each step of the psoriasis molecular pathway, different inflammatory cytokines and angiogenic growth factors are involved such as hypoxia inducible factor-1 α (HIF-1 α), vascular endothelial growth factor (VEGF), matrix metalo proteinases (MMPs), basic fibroblast growth factor (bFGF), Angiopoitin-2, interleukin-8 (IL-8), IL-17, and IL-2. Beside the mentioned growth factors and cytokines, cellular adhesion molecule 1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) which play roles in both angiogenesis and inflammation are also involved in the pathogenesis...
February 2017: Medical Hypotheses
https://www.readbyqxmd.com/read/28087785/thermolytic-degradation-of-synthetic-cannabinoids-chemical-exposures-and-pharmacological-consequences
#20
Brian F Thomas, Timothy W Lefever, Ricardo A Cortes, Megan Grabenauer, Alexander L Kovach, Anderson O Cox, Purvi R Patel, Gerald T Pollard, Julie A Marusich, Richard C Kevin, Thomas F Gamage, Jenny L Wiley
Synthetic cannabinoids are manufactured clandestinely with little quality control and are distributed as herbal "spice" for smoking or as bulk compound for mixing with a solvent and inhalation via electronic vaporizers. Intoxication with synthetic cannabinoids has been associated with seizure, excited delirium, coma, kidney damage, and other disorders. The chemical alterations produced by heating these structurally novel compounds for consumption are largely unknown. Here, we show that heating synthetic cannabinoids containing tetramethylcyclopropyl-ring substituents produced thermal degradants with pharmacological activity that varied considerably from their parent compounds...
April 2017: Journal of Pharmacology and Experimental Therapeutics
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