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Synthetic Cannabinoid

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https://www.readbyqxmd.com/read/28544560/fatal-intoxication-by-5f-adb-and-diphenidine-detection-quantification-and-investigation-of-their-main-metabolic-pathways-in-human-by-lc-ms-ms-and-lc-q-tofms
#1
Maiko Kusano, Kei Zaitsua, Kentaro Taki, Kazuaki Hisatsune, Jun'ichi Nakajima, Takako Moriyasu, Tomomi Asano, Yumi Hayashi, Hitoshi Tsuchihashi, Akira Ishii
Despite the implementation of the new blanket scheduling system in 2013, new psychoactive substance (NPS) abuse remains a serious social concern in Japan. We present a fatal intoxication case involving 5F-ADB (methyl 2-[1-(5-fluoropentyl)-1H-indazole-3-carboxamido]-3,3-dimethylbutanoate) and diphenidine. Postmortem blood screening by liquid chromatography/quadrupole time-of-flight mass spectrometry (LC/Q-TOFMS) in the information dependent acquisition (IDA) mode only detected diphenidine. Further urinary screening using an in-house database containing new NPS and metabolites detected not only diphenidine but also possible 5F-ADB metabolites; subsequent targeted screening by LC/tandem mass spectrometry (LC/MS/MS) allowed for the detection of very low level of unchanged 5F-ADB in postmortem heart blood...
May 21, 2017: Drug Testing and Analysis
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
#2
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/28530077/-the-illegal-synthetic-cannabinoid-drug-market-in-israel-evolution-and-new-challenges
#3
Barak Shapira, Alina Poperno, Ronny Berkovitz
This article represents a short review of the current knowledge on the abuse of synthetic cannabinoids from the perspective of the Division of Enforcement and Inspection of the Israeli Ministry of Health - a body in charge of providing professional assistance to law enforcement bodies in the fields of drug abuse. We describe the principal changes observed in the synthetic cannabinoid market and the Israeli legislators' and enforcement bodies' attempts to cope with these phenomena. These changes relate to the types of synthetic cannabinoids being trafficked, with many structural variations between substances, and a new legal framework which allows for the rapid, temporary scheduling of synthetic cannabinoids using both individual and generic definitions...
September 2016: Harefuah
https://www.readbyqxmd.com/read/28522773/severe-neurological-symptoms-following-synthetic-cannabinoid-intoxication
#4
F van Gorp, L C Wejden, N A Stienstra, E M Kuck, L E M Haas
Synthetic cannabinoids are becoming increasingly popular as substances of abuse. However, in the Netherlands synthetic cannabinoid intoxications are rare. We report a 16-year-old male who became deeply comatose and was admitted to the intensive care unit for invasive mechanical ventilation after a buse of aninitially unknown drug. Routine toxicology screening with an immunoassay only detected tetrahydrocannabinol, but additional tests with liquid chromatography mass spectrometry revealed synthetic cannabinoid use...
May 2017: Netherlands Journal of Medicine
https://www.readbyqxmd.com/read/28517235/new-psychoactive-substances-purchasing-and-supply-patterns-in-australia
#5
Rachel Sutherland, Raimondo Bruno, Amy Peacock, Paul Dietze, Courtney Breen, Lucinda Burns, Monica J Barratt
OBJECTIVE: To examine the purchasing and supply patterns of new psychoactive substance (NPS) consumers in Australia. METHOD: Data were obtained from a self-selected sample of 296 past-year NPS consumers, with comparisons made across dimethyltryptamine (n = 104), 2C-x (n = 59), NBOMe (n = 27), and synthetic cannabinoid (n = 22) users. RESULTS: Most consumers (58%) nominated a friend as their main NPS source, and almost half (46%) reported that they had supplied NPS to others in the past year (predominantly "social supply")...
May 18, 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28503792/synthetic-cannabinoid-use-in-an-acute-psychiatric-inpatient-unit
#6
Richard Vincent Clancy, Robert Charles Hodgson, Arvind Kendurkar, Margarett Ann Terry, Lawrence Dadd, Donna Maria Clancy, Karen Ryan, Maria Hatzistylis, Benjamin Graham Tinman
In the present study, we explored the prevalence of new psychoactive substance use by people admitted into an Australian acute public mental health facility specializing in comorbid mental health and substance use. These substances have since been banned from retail outlets, but the pattern of uptake and reasons people use them is informative in terms of motivations and the management of substance use more generally. A cross-sectional study to explore the use of synthetic cannabis by people admitted to an acute adult mental health unit was undertaken...
May 15, 2017: International Journal of Mental Health Nursing
https://www.readbyqxmd.com/read/28497982/neuroprotection-in-oxidative-stress-related-neurodegenerative-diseases-role-of-endocannabinoid-system-modulation
#7
Janos Paloczi, Zoltan V Varga, George Hasko, Pal Pacher
SIGNIFICANCE: Redox imbalance may lead to overproduction of reactive oxygen and nitrogen species (ROS/RNS) and subsequent oxidative tissue damage which is a critical event in the course of neurodegenerative diseases. It is still not fully elucidated, however, whether oxidative stress is the primary trigger or a consequence in process of neurodegeneration. Recent Advances: Increasing evidence suggests that oxidative stress is involved in the propagation of neuronal injury and consequent inflammatory response, which in concert promote development of pathological alterations characteristic of most common neurodegenerative diseases...
May 12, 2017: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/28496039/pyrolysis-of-ur-144-a-synthetic-cannabinoid-augments-an-affinity-to-human-cb1-receptor-and-cannabimimetic-effects-in-mice
#8
Asuka Kaizaki-Mitsumoto, Kyoko Hataoka, Masahiko Funada, Yuki Odanaka, Hiroki Kumamoto, Satoshi Numazawa
Drug abusers most often smoke 'herbal incense' as a cigarette or inhale it using a smoking tool. Smoking may cause pyrolysis of the drug and produce decomposed products of which biological effect has never been investigated. The synthetic cannabinoid UR-144 is known to undergo thermal degradation, giving a ring-opened isomer, so-called UR-144 degradant. The present study demonstrates by using UR-144 as a model drug that the smoke of burned UR-144 contains the UR-144 degradant. The UR-144 degradant showed approximately four fold higher agonist activity to human CB1 receptor and augmented hypothermic and akinetic actions in mice compared to UR-144...
2017: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/28495606/the-synthetic-cannabinoid-win-55-212-induced-apoptosis-in-cytotrophoblasts-cells-by-a-mechanism-dependent-on-cb1-receptor
#9
Marta Almada, Lia Costa, Bruno Miguel Fonseca, Cristina Amaral, Natércia Teixeira, Georgina Correia-da-Silva
The endocannabinoid system has evolved as a key regulator in several pathological and physiological processes, including placentation, decidualization and implantation. In addition, it is known that Cannabis and cannabinoids negatively affect female reproduction. Although, the biological action of synthetic cannabinoids, such as WIN-55,212, in human fertility and pregnancy outcome remain to be unveiled. A tight balance between proliferation, differentiation and apoptosis of trophoblast cells is required for placental development and pregnancy outcome...
May 8, 2017: Toxicology
https://www.readbyqxmd.com/read/28492462/synthetic-cannabinoids-use-in-elderly-patients
#10
Nahla Mahgoub, Robert C Young
Synthetic cannabinoids are becoming a public health concern. No data are apparently available concerning use of synthetic cannabinoids in the elderly. We report two cases of elderly individuals who used synthetic cannabinoids and were admitted to a psychiatric hospital.
May 2017: Journal of Psychiatric Practice
https://www.readbyqxmd.com/read/28488989/spice-y-kidney-failure-a-case-report-and-systematic-review-of-acute-kidney-injury-attributable-to-the-use-of-synthetic-cannabis
#11
REVIEW
Ceyda Zarifi, Shuchi Vyas
INTRODUCTION: Spice is a synthetic cannabinoid that is readily available for purchase in smoke shops at relatively low cost. Spice is not detectable upon routine drug screening, making it an increasingly popular new street drug. CASE REPORT: A 21-year-old man presented with new-onset seizures. During the next 2 days, he developed uncontrollable hypertension, agitation, respiratory failure requiring intubation, pulmonary hypertension, and acute kidney injury (AKI) with a maximum blood urea nitrogen/creatinine level of 54/7...
2017: Permanente Journal
https://www.readbyqxmd.com/read/28487743/delirium-and-high-creatine-kinase-and-myoglobin-levels-related-to-synthetic-cannabinoid-withdrawal
#12
Ahmet Bulent Yazici, Esra Yazici, Atila Erol
Synthetic cannabinoids (SCs) are included in a group of drugs called new psychoactive substances. Effects of SCs on the central nervous system are similar to other cannabinoids, but 2-100 times more potent than marijuana. Thus, addiction and withdrawal symptoms are more severe than natural cannabinoids. Withdrawal symptoms of SCs were reported in the literature previously. But there is no report about SC withdrawal delirium and its treatment. Several studies reported that agonists of CB1 receptors play a role in GABA and glutamatergic neurotransmission, which is similar to the effects of alcohol on GABA and glutamatergic receptors...
2017: Case Reports in Medicine
https://www.readbyqxmd.com/read/28484907/inhibition-of-cytochrome-p450-and-uridine-5-diphospho-glucuronosyltransferases-by-mam-2201-in-human-liver-microsomes
#13
Tae Yeon Kong, Ju-Hyun Kim, Soon-Sang Kwon, Jae Chul Cheong, Hee Seung Kim, Moon Kyo In, Hye Suk Lee
MAM-2201, a synthetic cannabinoid, is a potent agonist of the cannabinoid receptors and is increasingly used as an illicit recreational drug. The inhibitory effects of MAM-2201 on major drug-metabolizing enzymes such as cytochrome P450s (CYPs) and uridine 5'-diphospho-glucuronosyltransferases (UGTs) have not yet been investigated although it is widely abused, sometimes in combination with other drugs. We evaluated the inhibitory effects of MAM-2201 on eight major human CYPs (CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4) and six UGTs (UGTs 1A1, 1A3, 1A4, 1A6, 1A9, and 2B7) of pooled human liver microsomes; we thus explored potential MAM-2201-induced drug interactions...
May 8, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28472731/online-test-purchased-new-psychoactive-substances-in-5-different-european-countries-a-snapshot-study-of-chemical-composition-and-price
#14
Tibor Markus Brunt, Amanda Marie Atkinson, Thomas Nefau, Magali Martinez, Emmanuel Lahaie, Artur Malzcewski, Martin Pazitny, Vendula Belackova, Simon D Brandt
BACKGROUND: New psychoactive substances (NPS) are on offer worldwide online, in order to shed light on the purity and price of these substances in the European Union, a research collaboration was set up involving France, United Kingdom (UK), the Netherlands, Czech Republic and Poland. METHODS: Per country, around 10 different NPS were test purchased from different webshops. Then, chemical analysis of NPS was done with according reference standards to identify and quantify the contents...
May 1, 2017: International Journal on Drug Policy
https://www.readbyqxmd.com/read/28469427/vaping-synthetic-cannabinoids-a-novel-preclinical-model-of-e-cigarette-use-in-mice
#15
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/28457767/clinical-and-financial-implications-of-emergency-department-visits-for-synthetic-marijuana
#16
Eric Rowley, David Benson, Aaron Tiffee, Adam Hockensmith, Henry Zeng, Glenn N Jones, Mandi W Musso
BACKGROUND: Many users believe that synthetic cannabinoids offer a safe and legal means of getting high. However, spikes in emergency department visits have been associated with use of synthetic cannabinoids. The purpose of the current study was to document emergency department visits from three large hospitals in one metropolitan area over a two month period. METHOD: This was a retrospective chart review examining 218 patients presenting to three inner city emergency departments between March and April 2014...
April 23, 2017: American Journal of Emergency Medicine
https://www.readbyqxmd.com/read/28455676/metabolic-profile-of-synthetic-cannabinoids-5f-pb-22-pb-22-xlr-11-and-ur-144-by-cunninghamella-elegans
#17
Shimpei Watanabe, Unnikrishnan Kuzhiumparambil, My Ann Nguyen, Jane Cameron, Shanlin Fu
The knowledge of metabolic profile of synthetic cannabinoids is important for the detection of drugs in urinalysis due to the typical absence or low abundance of parent cannabinoids in human urine. The fungus Cunninghamella elegans has been reported to be a useful tool for metabolism study and thus applicability to synthetic cannabinoid metabolism was examined. In this study, 8-quinolinyl 1-(5-fluoropentyl)-1H-indole-3-carboxylate (5F-PB-22), 8-quinolinyl 1-pentyl-1H-indole-3-carboxylate (PB-22), [1-(5-fluoropentyl)-1H-indol-3-yl](2,2,3,3-tetramethylcyclopropyl)methanone (XLR-11) and (1-pentyl-1H-indol-3-yl)(2,2,3,3-tetramethylcyclopropyl)methanone (UR-144) were incubated with C...
April 28, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28446875/cannabinoid-modulation-of-memory-consolidation-in-rats-beyond-the-role-of-cannabinoid-receptor-subtype-1
#18
Patrizia Ratano, Maura Palmery, Viviana Trezza, Patrizia Campolongo
The effects induced by exogenous manipulation of endocannabinoid neurotransmission on emotion and memory are often contradictory. Among the different factors involved, of particular interest is the binding affinity of endocannabinoids, and their analogs, for other receptor families beyond cannabinoid receptors, such as the peroxisome proliferator-activated receptors (PPARs), and the transient receptor potential cation channel subfamily V member 1 (TRPV1). The aim of this study was to investigate which receptor subtype mediates cannabinoid effects on memory consolidation for emotionally arousing experiences...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28444659/new-psychoactive-substances-nps-a-challenge-for-the-addiction-treatment-services
#19
Norbert Scherbaum, F Schifano, Udo Bonnet
Over the last few years, hundreds of new psychoactive substances (NPS) have been identified in Europe. Apart from some herbal compounds, NPS mainly include synthetic cannabinoids and a range of new synthetic stimulants (e. g., cathinones). Synthetic NPS are often developed whilst modifying the basic chemical (e. g., phenethylamine or tryptamine) structure. Although the pharmacology and toxicology of most NPS are hardly known, they are being offered, especially online, as "bath salts," as "incense mixtures," or under other misleading labels...
May 2017: Pharmacopsychiatry
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
#20
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
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