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Synthetic cannabinoids

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https://www.readbyqxmd.com/read/27924364/metabolic-characterization-of-1-5-fluoropentyl-1h-indol-3-yl-4-methyl-1-naphthalenyl-methanone-mam-2201-using-human-liver-microsomes-and-cdna-overexpressed-cytochrome-p450-enzymes
#1
Tae Yeon Kong, Ju-Hyun Kim, Won Gu Choi, Joo Young Lee, Hee Seung Kim, Jin Young Kim, Moon Kyo In, Hye Suk Lee
MAM-2201 is a synthetic cannabinoid that is increasingly found in recreational drug abusers and cases of severe intoxication. Thus, characterization of the metabolic pathways of MAM-2201 is necessary to predict individual pharmacokinetics and toxicity differences, and to avoid toxic drug-drug interactions. Collectively, 19 phase 1 metabolites of MAM-2201 were identified using liquid chromatography-Orbitrap mass spectrometry following human liver microsomal incubations in the presence of NADPH: 7 hydroxy-MAM-2201 (M1-M7), 4 dihydroxy-MAM-2201 (M8-M11), dihydrodiol-MAM-2201 (M12), N-(5-hydroxypentyl)-MAM-2201 (M13), hydroxy-M13 (M14), N-dealkyl-MAM-2201 (M15), 2 hydroxy-M15 (M16, M17), MAM-2201 N-pentanoic acid (M18), and hydroxy-M18 (M19)...
December 6, 2016: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/27903642/behavioral-characterization-of-kappa-opioid-receptor-agonist-spiradoline-and-cannabinoid-receptor-agonist-cp55940-mixtures-in-rats
#2
Vanessa Minervini, Sujata S Dahal, Charles France
Pain is a significant clinical problem and there is a need for more effective treatments with reduced adverse effects that currently limit the use of mu opioid receptor agonists. Synthetic kappa opioid receptor agonists have no abuse liability and well-documented antinociceptive effects; however, adverse effects (diuresis, dysphoria) preclude their use in the clinic. Combining kappa opioids with non-opioid drugs (cannabinoid receptor agonists) allows for smaller doses of each drug to produce antinociception...
November 30, 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27896322/effectiveness-of-the-synthetic-cannabinoids-seminar
#3
Murat Seyit, Mert Ozen, Alten Oskay, Emine Kadioglu
OBJECTIVES: Synthetic cannabinoid or "Bonzai" use is a public health issue as its use has increased in Turkey as well as all over the world. The aim of this study is to evaluate the effectiveness of the "Synthetic Cannabinoids Seminar" that was provided to physicians who work in emergency services, using multiple choice questionnaires before and after the seminar as a tool for evaluation. MATERIAL AND METHOD: Synthetic cannabinoids seminars were provided to physicians who work in emergency services in two different cities, with the participation of 20 physicians in each scheduled seminar...
June 2016: Turkish Journal of Emergency Medicine
https://www.readbyqxmd.com/read/27894904/from-niche-to-stigma-headshops-to-prison-exploring-the-rise-and-fall-of-synthetic-cannabinoid-use-among-young-adults
#4
Shane Blackman, Rick Bradley
The aim of this paper will be to consider the rise and subsequent fall in NPS use at national and local level with a focus on synthetic cannabinoid products in Kent. We will examine the local practice and policy responses by Kent's Young Persons' Drug and Alcohol Service towards a possible change in patterns of NPS drug consumption. The county has seen an expansion in the number of Headshops and we present local media coverage on NPS, and the Trading Standards and Kent Police intervention Operation Lantern to regulate Headshops...
November 25, 2016: International Journal on Drug Policy
https://www.readbyqxmd.com/read/27884725/endocannabinoid-system-in-sexual-motivational-processes-is-it-a-novel-therapeutic-horizon
#5
REVIEW
Renata Androvicova, Jiri Horacek, Tibor Stark, Filippo Drago, Vincenzo Micale
The endocannabinoid system (ECS), which is composed of the cannabinoid receptors types 1 and 2 (CB1 and CB2) for marijuana's psychoactive ingredient Δ(9)-tetrahydrocannabinol (Δ(9)-THC), the endogenous ligands (AEA and 2-AG) and the enzymatic systems involved in their biosynthesis and degradation, recently emerged as important modulator of emotional and non-emotional behaviors. For centuries, in addition to its recreational actions, several contradictory claims regarding the effects of Cannabis use in sexual functioning and behavior (e...
November 21, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27879006/allosteric-modulation-an-alternate-approach-targeting-the-cannabinoid-cb1-receptor
#6
REVIEW
Thuy Nguyen, Jun-Xu Li, Brian F Thomas, Jenny L Wiley, Terry P Kenakin, Yanan Zhang
The cannabinoid CB1 receptor is a G protein coupled receptor and plays an important role in many biological processes and physiological functions. A variety of CB1 receptor agonists and antagonists, including endocannabinoids, phytocannabinoids, and synthetic cannabinoids, have been discovered or developed over the past 20 years. In 2005, it was discovered that the CB1 receptor contains allosteric site(s) that can be recognized by small molecules or allosteric modulators. A number of CB1 receptor allosteric modulators, both positive and negative, have since been reported and importantly, they display pharmacological characteristics that are distinct from those of orthosteric agonists and antagonists...
November 23, 2016: Medicinal Research Reviews
https://www.readbyqxmd.com/read/27876485/cannabinoid-receptors-and-trpa1-on-neuroprotection-in-a-model-of-retinal-ischemia
#7
D S M Araújo, V S Miya-Coreixas, P Pandolfo, K C Calaza
Retinal ischemia is a pathological event present in several retinopathies such as diabetic retinopathy and glaucoma, leading to partial or full blindness with no effective treatment available. Since synthetic and endogenous cannabinoids have been studied as modulators of ischemic events in the central nervous system (CNS), the present study aimed to investigate the involvement of cannabinoid system in the cell death induced by ischemia in an avascular (chick) retina. We observed that chick retinal treatment with a combination of WIN 55212-2 and cannabinoid receptor antagonists (either AM251/O-2050 or AM630) decreased the release of lactate dehydrogenase (LDH) induced by retinal ischemia in an oxygen and glucose deprivation (OGD) model...
November 19, 2016: Experimental Eye Research
https://www.readbyqxmd.com/read/27875961/editorial-thematic-issue-from-old-cannabinoids-to-emerging-new-synthetic-derivatives-with-potential-therapeutic-application-in-neurological-disorders
#8
EDITORIAL
Anna M Malfitano
No abstract text is available yet for this article.
2016: Recent Patents on CNS Drug Discovery
https://www.readbyqxmd.com/read/27871157/synthetic-cannabinoid-induced-immunosuppression-augments-cerebellar-dysfunction-in-tetanus-toxin-treated-mice
#9
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/27866061/patterns-of-drugs-poisons-in-southern-area-of-south-korea-in-2014
#10
Eunmi Kim, Yonghoon Park, Hongil Ha, Heesun Chung
The southern area of South Korea consists of three parts; Busan, Ulsan and Gyeongsangnam-do. Busan Institute of National Forensic Service (NFS) performed about 50,000 cases throughout the southern area in 2014, occupying over 15% of total cases covered by NFS. In this study, patterns of drugs and poisons in the southern area of South Korea were investigated. The investigation was carried out by the laboratory information management system of NFS between January and December of 2014. As results, a total of 606 autopsy cases were performed by Busan Institute of NFS in 2014...
December 2016: Forensic Science International
https://www.readbyqxmd.com/read/27865819/buzz-juice-neurological-sequelae-of-synthetic-cannabinoids
#11
Manisha Kak, Fadi Mikhail, Sho T Yano, Rui Guan, Rimas V Lukas
The use of synthetic cannabinoids is becoming more widespread. Familiarity with the potential toxicities associated with these agents will grow in importance. We present a case of a woman who developed onset of confusion, visual hallucinations, and ataxia after vaporizing synthetic cannabinoids. MRI imaging demonstrated restricted diffusion and increased T2/FLAIR signal in the corpus callosum and cerebellar peduncles.
November 16, 2016: Journal of Clinical Neuroscience: Official Journal of the Neurosurgical Society of Australasia
https://www.readbyqxmd.com/read/27864947/determining-the-toxicological-significance-of-pregabalin-in-fatalities
#12
Simon P Elliott, Timothy Burke, Christopher Smith
Pregabalin has become more widely prescribed and abused in recent years but is still not always included in laboratory analysis. An LC-MS-MS method has been developed and applied to measure pregabalin in 93 postmortem cases, including drug-related deaths, alternative causes of death, and fatalities where pregabalin was likely to have contributed to death. Other drugs or alcohol was detected, and the most common drug types (in decreasing frequency) were antidepressants, opioids, benzodiazepines, opiates, alcohol, antipsychotics, cocaine, cardiac drugs, amphetamines, cannabis, anticonvulsants, and antihistamines...
November 16, 2016: Journal of Forensic Sciences
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
#13
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...
December 2016: Forensic Science International
https://www.readbyqxmd.com/read/27863089/freeze-and-thaw-stability-and-long-term-stability-of-84-synthetic-cannabinoids-in-serum
#14
Cornelius Hess, Lynn Krueger, Michael Unger, Burkhard Madea
Information about stability of synthetic cannabinoids is important to give recommendations for storage conditions in cases in which use of synthetic cannabinoids is suspected. In this study freeze and thaw stability (3 cycles at -20 °C at 1.5 ng/ml) and long term stability at room temperature, 4 °C and -20 °C (until 150 days) were tested by a validated liquid chromatographic mass spectrometric method for 80 synthetic cannabinoids. Results demonstrated good freeze and thaw stability for most of the substances...
November 8, 2016: Drug Testing and Analysis
https://www.readbyqxmd.com/read/27861784/focus-on-cannabinoids-and-synthetic-cannabinoids
#15
R Le Boisselier, J Alexandre, V Lelong-Boulouard, D Debruyne
The recent emergence of a multitude of synthetic cannabinoids (SCs) has generated a wealth of new information, suggesting the usefulness of state-of-the-art on lato sensu cannabinoids. By modulating a plurality of neurotransmission pathways, the endocannabinoid system is involved in many physiological processes increasingly explored. SCs desired and adverse effects are considered to be more intense than those observed with cannabis smoking, which is partly explained by the full agonist activity and higher affinity for cannabinoid receptors...
November 9, 2016: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27858284/role-of-cannabinoid-receptor-1-in-human-adipose-tissue-for-lipolysis-regulation-and-insulin-resistance
#16
Cherno O Sidibeh, Maria J Pereira, Joey Lau Börjesson, Prasad G Kamble, Stanko Skrtic, Petros Katsogiannos, Magnus Sundbom, Maria K Svensson, Jan W Eriksson
We recently showed that the peripheral cannabinoid receptor type 1 (CNR1) gene is upregulated by the synthetic glucocorticoid dexamethasone. CNR1 is highly expressed in the central nervous system and has been a drug target for the treatment of obesity. Here we explore the role of peripheral CNR1 in states of insulin resistance in human adipose tissue. Subcutaneous adipose tissue was obtained from well-controlled type 2 diabetes subjects and controls. Subcutaneous adipose tissue gene expression levels of CNR1 and endocannabinoid synthesizing and degrading enzymes were assessed...
November 17, 2016: Endocrine
https://www.readbyqxmd.com/read/27853201/the-effects-of-%C3%AE-9-tetrahydrocannabinol-on-the-dopamine-system
#17
Michael A P Bloomfield, Abhishekh H Ashok, Nora D Volkow, Oliver D Howes
The effects of Δ(9)-tetrahydrocannabinol (THC), the main psychoactive ingredient in cannabis, are a pressing concern for global mental health. Patterns of cannabis use are changing drastically owing to legalization, the availability of synthetic analogues (commonly termed spice), cannavaping and an emphasis on the purported therapeutic effects of cannabis. Many of the reinforcing effects of THC are mediated by the dopamine system. Owing to the complexity of the cannabinoid-dopamine interactions that take place, there is conflicting evidence from human and animal studies concerning the effects of THC on the dopamine system...
November 16, 2016: Nature
https://www.readbyqxmd.com/read/27853110/a-new-designer-drug-5f-adb-activates-midbrain-dopaminergic-neurons-but-not-serotonergic-neurons
#18
Nozomi Asaoka, Hiroyuki Kawai, Naoya Nishitani, Haruko Kinoshita, Norihiro Shibui, Kazuki Nagayasu, Hisashi Shirakawa, Shuji Kaneko
N-[[1-(5-fluoropentyl)-1H-indazol-3-yl]carbonyl]-3-methyl-D-valine methyl ester (5F-ADB) is one of the most potent synthetic cannabinoids and elicits severe psychotic symptoms in humans, sometimes causing death. To investigate the neuronal mechanisms underlying its toxicity, we examined the effects of 5F-ADB on midbrain dopaminergic and serotonergic systems, which modulate various basic brain functions such as those in reward-related behavior. 5F-ADB-induced changes in spontaneous firing activity of dopaminergic and serotonergic neurons were recorded by ex vivo electrophysiological techniques...
2016: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/27850472/834-k2-the-deadly-designer-drug-a-multicenter-case-series-on-synthetic-cannabinoid-complications
#19
Faith Armstrong, Michael McCurdy, Elizabeth Otto
No abstract text is available yet for this article.
December 2016: Critical Care Medicine
https://www.readbyqxmd.com/read/27850172/532-clinical-effects-of-synthetic-cannabinoid-exposure-in-patients-admitted-to-the-intensive-care-unit
#20
Michael Tatusov, Maryann Amirshahi, Aleeza Abbasi, Munish Goyal
No abstract text is available yet for this article.
December 2016: Critical Care Medicine
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