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https://www.readbyqxmd.com/read/27871157/synthetic-cannabinoid-induced-immunosuppression-augments-cerebellar-dysfunction-in-tetanus-toxin-treated-mice
#1
Jaesuk Yun, Sun Mi Gu, Tac-Hyung Lee, Yun Jeong Song, Seonhwa Seong, Young-Hoon Kim, Hye Jin Cha, Kyoung Moon Han, Jisoon Shin, Hokyung Oh, Kikyung Jung, Chiyoung Ahn, Hye-Kyung Park, Hyung Soo Kim
Synthetic cannabinoids are one of most abused new psychoactive substances. The recreational use of abused drug has aroused serious concerns about the consequences of these drugs on infection. However, the effects of synthetic cannabinoid on resistance to tetanus toxin are not fully understood yet. In the present study, we aimed to determine if the administration of synthetic cannabinoids increase the susceptibility to tetanus toxin-induced motor behavioral deficit and functional changes in cerebellar neurons in mice...
November 25, 2016: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/27863282/identification-and-quantification-of-synthetic-cannabinoids-in-spice-like-herbal-mixtures-update-of-the-german-situation-for-the-spring-of-2016
#2
Nico Langer, Rainer Lindigkeit, Hans-Martin Schiebel, Uli Papke, Ludger Ernst, Till Beuerle
In February 2016, nine "spice-like" products from German language internet shops were analyzed. In total, eight different synthetic cannabinoids were identified by gas chromatography-mass spectrometry (GC-MS), namely THJ-018, THJ-2201, MAB-CHMINACA, 5F-ADB, 5Cl-AKB48 (syn.: 5C-AKB48), 4-pentenyl-AKB48, MDMB-CHMICA and 5F-AB-PINACA. For the majority of products only one synthetic cannabinoid was identified as the active ingredient, while two products contained 2 and 5 compounds, respectively. For some of the identified cannabinoids (MAB-CHMINACA, 5Cl-AKB48 and 4-pentenyl-AKB48) no or only insufficient physico-chemical data were available in literature...
November 4, 2016: Forensic Science International
https://www.readbyqxmd.com/read/27834143/distribution-of-synthetic-cannabinoids-jwh-210-rcs-4-and-%C3%A2-9-tetrahydrocannabinol-after-intravenous-administration-to-pigs
#3
Nadine Schaefer, Mattias Kettner, Matthias W Laschke, Julia Schlote, Andreas H Ewald, Michael D Menger, Hans H Maurer, Peter H Schmidt
Synthetic cannabinoids (SCs) have become an increasing issue in forensic toxicology. Controlled human studies evaluating pharmacokinetic data of SCs are lacking and only few animal studies have been published. Thus, an interpretation of analytical results found in intoxicated or poisoned individuals is difficult. Therefore, the distribution of two selected SCs, namely 4-ethylnaphthalen-1-yl-(1-pentylindol-3-yl)methanone (JWH-210) and 2-(4-methoxyphenyl)-1-(1-pentyl-indol-3-yl)methanone (RCS-4) as well as ∆9-tetrahydrocannabinol (THC) as reference were examined in pigs...
November 11, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27821642/mother-blame-and-the-just-world-theory-in-child-sexual-abuse-cases
#4
Kelsi Toews, Jorden A Cummings, Jessica L Zagrodney
Mothers are blamed for a variety of negative experiences and outcomes of their children, including child sexual abuse (CSA). According to just world hypothesis (JWH), people have a need to view the world as one where there is no such thing as an innocent victim; that is, the world is fair and just. These beliefs predict victim blaming in situations such as sexual abuse, physical abuse, and robbery. However, JWH has not been applied to the examination of mother blame, a situation in which the blame target did not directly experience the traumatic event...
November 6, 2016: Journal of Interpersonal Violence
https://www.readbyqxmd.com/read/27779402/detection-and-activity-profiling-of-synthetic-cannabinoids-and-metabolites-with-a-newly-developed-bio-assay
#5
Annelies Cannaert, Jolien Storme, Florian Franz, Volker Auwärter, Christophe P Stove
Synthetic cannabinoids (SCs) are the largest group of compounds currently monitored in Europe by the EU Early Warning System on new psychoactive substances. Emerging recreational use of these products has led to multiple cases of adverse health effects and even death. In contrast to marijuana, where Δ9-tetrahydrocannabinol (Δ9THC) is metabolized to only one major active metabolite, it has been reported that several major phase I metabolites of SCs remain biologically active, exerting cannabinoid (CB) receptor affinity, potency and efficacy greater than Δ9THC...
October 25, 2016: Analytical Chemistry
https://www.readbyqxmd.com/read/27769788/cannabinoid-receptor-2-activation-restricts-fibrosis-and-alleviates-hydrocephalus-after-intraventricular-hemorrhage
#6
Qiang Tan, Qianwei Chen, Zhou Feng, Xia Shi, Jun Tang, Yihao Tao, Bing Jiang, Liang Tan, Hua Feng, Gang Zhu, Yunfeng Yang, Zhi Chen
Fibrosis in ventricular system has a role in hydrocephalus following intraventricular hemorrhage (IVH). The cannabinoid receptor 2 (CB2) has been reported to participate in alleviating the fibrosis process of many diseases. However, its role in fibrosis after IVH was unclear so far, and we hypothesized that CB2 activation has potential to attenuate hydrocephalus after IVH via restricting fibrosis. So the present study was designed to investigate this hypothesis in a modified rat IVH model. Autologous non-anticoagulative blood injection model was induced to mimic ventricular extension of hemorrhage in adult Sprague-Dawley rats...
October 18, 2016: Brain Research
https://www.readbyqxmd.com/read/27753007/combination-chemistry-structure-activity-relationships-of-novel-psychoactive-cannabinoids
#7
Jenny L Wiley, Julie A Marusich, Brian F Thomas
Originally developed as research tools for use in structure-activity relationship studies, synthetic cannabinoids contributed to significant scientific advances in the cannabinoid field. Unfortunately, a subset of these compounds was diverted for recreational use beginning in the early 2000s. As these compounds were banned, they were replaced with additional synthetic cannabinoids with increasingly diverse chemical structures. This chapter focuses on integration of recent results with those covered in previous reviews...
October 18, 2016: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/27715709/acute-effects-of-synthetic-cannabinoids-update-2015
#8
Juliana Tournebize, Valérie Gibaja, Jean-Pierre Kahn
BACKGROUND: Cannabis is the most widely used illicit drug in the United States and Europe. In recent years, a range of new substances with cannabis-like effects-known as synthetic cannabinoids (SCs)-have suddenly burst on the drug scene. However, there is limited information about the clinical hazards linked to the use of these emerging substances. This review summarizes the literature to date relating the health effects of SCs. METHOD: A systematic literature review of original case studies was performed using PubMed and Web of Science (January 1980-July 2015)...
August 11, 2016: Substance Abuse
https://www.readbyqxmd.com/read/27695396/vascular-dysfunction-in-a-transgenic-model-of-alzheimer-s-disease-effects-of-cb1r-and-cb2r-cannabinoid-agonists
#9
Jorge Navarro-Dorado, Nuria Villalba, Dolores Prieto, Begoña Brera, Ana M Martín-Moreno, Teresa Tejerina, María L de Ceballos
There is evidence of altered vascular function, including cerebrovascular, in Alzheimer's disease (AD) and transgenic models of the disease. Indeed vasoconstrictor responses are increased, while vasodilation is reduced in both conditions. β-Amyloid (Aβ) appears to be responsible, at least in part, of alterations in vascular function. Cannabinoids, neuroprotective and anti-inflammatory agents, induce vasodilation both in vivo and in vitro. We have demonstrated a beneficial effect of cannabinoids in models of AD by preventing glial activation...
2016: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/27681775/separation-of-isomers-of-jwh-122-on-porous-graphitic-carbon-stationary-phase-with-non-aqueous-mobile-phase-using-intelligent-software
#10
Norbert Rácz, Tibor Veress, Júlia Nagy, Balázs Bobály, Jenő Fekete
Cannabimimetic compounds have gained an increasing attention from the forensic community during the past few years. The present study was aimed to develop a liquid chromatographic separation method for the analysis of JWH-122 and its methyl isomers. In Hungary, JWH-122 is scheduled as a narcotic compound and its methyl isomers fall into the new psychoactive substance category, attracting significantly milder punishment than JWH-122 does. According to our best knowledge, gas chromatography or reversed phase liquid chromatography coupled with mass spectrometry could not be applied for separation and selective determination of methyl-naphthoyl indol isomers...
November 2016: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/27634891/cb2-cannabinoid-receptor-activation-promotes-colon-cancer-progression-via-akt-gsk3%C3%AE-signaling-pathway
#11
Esther Martínez-Martínez, Asunción Martín-Ruiz, Paloma Martín, Virginia Calvo, Mariano Provencio, José M García
The pharmacological activation of the cannabinoid receptor type 2, CB2, has been shown to elicit anti-tumoral mechanisms in different cancer types. However, little is known about its endogenous role in tumor pathophysiology, and different studies have attributed pro-tumorigenic properties to this receptor. In a previous work, we showed that CB2 expression is a poor prognostic factor in colon cancer patients. Here we report that activation of CB2 with low doses of specific agonists induce cell proliferation and favor the acquisition of aggressive molecular features in colon cancer cells...
September 12, 2016: Oncotarget
https://www.readbyqxmd.com/read/27535976/stratification-of-cannabinoid-1-receptor-cb1r-agonist-efficacy-manipulation-of-cb1r-density-through-use-of-transgenic-mice-reveals-congruence-between-in-vivo-and-in-vitro-assays
#12
T W Grim, A J Morales, M M Gonek, J L Wiley, B F Thomas, G W Endres, L J Sim-Selley, D E Selley, S S Negus, A H Lichtman
Synthetic cannabinoids (SCs) are an emerging class of abused drugs that differ from each other and the phytocannabinoid ∆(9)-tetrahydrocannabinol (THC) in their safety and cannabinoid-1 receptor (CB1R) pharmacology. As efficacy represents a critical parameter to understanding drug action, the present study investigated this metric by assessing in vivo and in vitro actions of THC, two well-characterized SCs (WIN55,212-2 and CP55,940), and three abused SCs (JWH-073, CP47,497, and A-834,735-D) in CB1 (+/+), (+/-), and (-/-) mice...
November 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27534533/cb2-receptor-activation-prevents-glial-derived-neurotoxic-mediator-production-bbb-leakage-and-peripheral-immune-cell-infiltration-and-rescues-dopamine-neurons-in-the-mptp-model-of-parkinson-s-disease
#13
Young C Chung, Won-Ho Shin, Jeong Y Baek, Eun J Cho, Hyung H Baik, Sang R Kim, So-Yoon Won, Byung K Jin
The cannabinoid (CB2) receptor type 2 has been proposed to prevent the degeneration of dopamine neurons in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated mice. However, the mechanisms underlying CB2 receptor-mediated neuroprotection in MPTP mice have not been elucidated. The mechanisms underlying CB2 receptor-mediated neuroprotection of dopamine neurons in the substantia nigra (SN) were evaluated in the MPTP mouse model of Parkinson's disease (PD) by immunohistochemical staining (tyrosine hydroxylase, macrophage Ag complex-1, glial fibrillary acidic protein, myeloperoxidase (MPO), and CD3 and CD68), real-time PCR and a fluorescein isothiocyanate-labeled albumin assay...
2016: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/27527584/effect-of-the-novel-synthetic-cannabinoids-akb48-and-5f-akb48-on-tetrad-sensorimotor-neurological-and-neurochemical-responses-in-mice-in-vitro-and-in-vivo-pharmacological-studies
#14
Isabella Canazza, Andrea Ossato, Claudio Trapella, Anna Fantinati, Maria Antonietta De Luca, Giulia Margiani, Fabrizio Vincenzi, Claudia Rimondo, Fabiana Di Rosa, Adolfo Gregori, Katia Varani, Pier Andrea Borea, Giovanni Serpelloni, Matteo Marti
RATIONALE: AKB48 and its fluorinate derivate 5F-AKB48 are two novel synthetic cannabinoids belonging to a structural class with an indazole core structure. They are marketed as incense, herbal preparations or chemical supply for their psychoactive Cannabis-like effects. OBJECTIVES: The present study was aimed at investigating the in vitro and in vivo pharmacological activity of AKB48 and 5F-AKB48 in male CD-1 mice and comparing their in vivo effects with those caused by the administration of Δ(9)-THC and JWH-018...
October 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27521533/simultaneous-determination-of-major-phytocannabinoids-their-main-metabolites-and-common-synthetic-cannabinoids-in-urine-samples-by-lc-ms-ms
#15
Xiaoru Dong, Liliang Li, Yonghong Ye, Lixing Zheng, Yan Jiang
Simultaneous determination of major phytocannabinoids (THC, CBD, CBN), their main metabolites (11-OH-THC, THC-COOH, THC-COOH-glucuronide) and common synthetic cannabinoids (HU-210, JWH-018, JWH-073, JWH-250) remains an issue in forensic toxicology. The present study has developed a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to simultaneously detect the above 10 analytes in human urine samples. The chromatographic separation was performed on an ACQUITY UPLC(®)BEH Phenyl 1.7μm (2.1×100mm) column, using a mobile phase consisting of 0...
October 15, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/27504865/the-effect-of-muscarinic-receptor-modulators-on-the-antinociception-induced-by-cb2-receptor-agonist-jwh133-in-mice
#16
M Alipour, F Fekrmandi, S Onsori, P Tabrizian, M R Jafari
There is no published study regarding the interaction between muscarinic receptor modulators and antinociception induced by cannabinoid receptor (CB2) agonist. The effect of pilocarpine (a muscarinic agonist) and atropine (a muscarinic antagonist) on JWH-133 (a CB2 agonist) induced analgesia in mice was studied. First the analgesic effect of JWH-133 (0.001-1 mg/Kg) or pilocarpine (2.5-20 mg/kg) or atropine (0.2-5 mg/kg) was evaluated. Subsequently, the effect of co-administration of pilocarpine (2.5 mg/kg) or atropine (5 mg/kg) and JWH-133 (0...
August 9, 2016: Drug Research
https://www.readbyqxmd.com/read/27474129/selective-activation-of-cb2-receptor-improves-efferocytosis-in-cultured-macrophages
#17
Lisheng Jiang, Yingmin Chen, Xiaojing Huang, Ancai Yuan, Qin Shao, Jun Pu, Ben He
AIMS: Recent evidence indicates that the defective ability to clear apoptotic cells by macrophages (efferocytosis) and the resultant apoptotic cells accumulation in atherosclerotic plaques play an important role during the progression of unstable plaques. The cannabinoid type 2 receptor (CB2), has recently been emerging as a new target to reduce vulnerability and promote stability of plaques, however, the underlying mechanisms have not been studied in detail. In the present study, we investigated whether selective activation of CB2 improves efferocytosis of macrophages...
September 15, 2016: Life Sciences
https://www.readbyqxmd.com/read/27471991/chemical-characterization-of-synthetic-cannabinoids-by-electrospray-ionization-ft-icr-mass-spectrometry
#18
Jade B Kill, Izabela F Oliveira, Lilian V Tose, Helber B Costa, Ricardo M Kuster, Leandro F Machado, Radigya M Correia, Rayza R T Rodrigues, Géssica A Vasconcellos, Boniek G Vaz, Wanderson Romão
The synthetic cannabinoids (SCs) represent the most recent advent of the new psychotropic substances (NPS) and has become popularly known to mitigate the effects of the Δ(9)-THC. The SCs are dissolved in organic solvents and sprayed in a dry herbal blend. However, little information is reported on active ingredients of SCs as well as the excipients or diluents added to the herbal blend. In this work, the direct infusion electrospray ionization Fourier transform ion cyclotron mass spectrometry technique (ESI-FT-ICR MS) was applied to explore the chemical composition of nine samples of herbal extract blends, where a total of 11 SCs (UR-144, JWH-073, XLR-11, JWH-250, JWH-122, AM-2201, AKB48, JWH-210, JWH-081, MAM-2201 and 5F-AKB48) were identified in the positive ionization mode, ESI(+), and other 44 chemical species (saturated and unsaturated fatty acids, sugars, flavonoids, etc...
September 2016: Forensic Science International
https://www.readbyqxmd.com/read/27449567/evaluation-of-first-generation-synthetic-cannabinoids-on-binding-at-non-cannabinoid-receptors-and-in-a-battery-of-in%C3%A2-vivo-assays-in-mice
#19
Jenny L Wiley, Timothy W Lefever, Julie A Marusich, Megan Grabenauer, Katherine N Moore, John W Huffman, Brian F Thomas
Anecdotal reports suggest that abused synthetic cannabinoids produce cannabis-like "highs," but some of their effects may also differ from traditional cannabinoids such as Δ(9)-tetrahydrocannabinol (THC). This study examined the binding affinities of first-generation indole-derived synthetic cannabinoids at cannabinoid and noncannabinoid receptors and their effects in a functional observational battery (FOB) and drug discrimination in mice. All seven compounds, except JWH-391, had favorable affinity (≤159 nM) for both cannabinoid receptors...
November 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27421777/jwh-018-%C3%AF-oh-a-shared-hydroxy-metabolite-of-the-two-synthetic-cannabinoids-jwh-018-and-am-2201-undergoes-oxidation-by-alcohol-dehydrogenase-and-aldehyde-dehydrogenase-enzymes-in-vitro-forming-the-carboxylic-acid-metabolite
#20
Niels Bjerre Holm, Carolina Noble, Kristian Linnet
Synthetic cannabinoids are new psychoactive substances (NPS) acting as agonists at the cannabinoid receptors. The aminoalkylindole-type synthetic cannabinoid naphthalen-1-yl-(1-pentylindol-3-yl)methanone (JWH-018) was among the first to appear on the illicit drug market and its metabolism has been extensively investigated. The N-pentyl side chain is a major site of human cytochrome P450 (CYP)-mediated oxidative metabolism, and the ω-carboxylic acid metabolite appears to be a major in vivo human urinary metabolite...
September 30, 2016: Toxicology Letters
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