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Synthetic cannabinoids

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https://www.readbyqxmd.com/read/28821542/human-hepatocyte-metabolism-of-novel-synthetic-cannabinoids-mn-18-and-its-5-fluoro-analog-5f-mn-18
#1
Xingxing Diao, Jeremy Carlier, Mingshe Zhu, Marilyn A Huestis
BACKGROUND: In 2014, 2 novel synthetic cannabinoids, MN-18 and its 5-fluoro analog, 5F-MN-18, were first identified in an ongoing survey of novel psychoactive substances in Japan. In vitro pharmacological assays revealed that MN-18 and 5F-MN-18 displayed high binding affinities to human CB1 and CB2 receptors, with Ki being 1.65-3.86 nmol/L. MN-18 and 5F-MN-18 were scheduled in Japan and some other countries in 2014. Despite increasing prevalence, no human metabolism data are currently available, making it challenging for forensic laboratories to confirm intake of MN-18 or 5F-MN-18...
August 18, 2017: Clinical Chemistry
https://www.readbyqxmd.com/read/28815938/optimization-of-recombinant-%C3%AE-glucuronidase-hydrolysis-and-quantification-of-eight-urinary-cannabinoids-and-metabolites-by-liquid-chromatography-tandem-mass-spectrometry
#2
Cristina Sempio, Karl B Scheidweiler, Allan J Barnes, Marilyn A Huestis
Prolonged urinary cannabinoid excretion in chronic frequent cannabis users confounds identification of recent cannabis intake that may be important in treatment, workplace, clinical, and forensic testing programs. In addition, differentiation of synthetic Δ9-tetrahydrocannabinol (THC) intake from cannabis plant products might be an important interpretive issue. THC, 11-hydroxy-THC (11-OH-THC) and 11-nor-9-carboxy-THC (THCCOOH) urine concentrations were evaluated during previous controlled cannabis administration studies following tandem alkaline/E...
June 14, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28813207/examination-of-synthetic-cannabinoid-and-cathinone-use-among-a-drug-using-offender-sample-2013-2015
#3
Kirsten Elin Smith, Amanda M Bunting, Michele Staton, Robert Walker, Sara Shalash, Erin Winston, Kevin Pangburn
Use of novel psychoactive substances (NPS) such as synthetic cannabinoids (e.g., "Spice," "Serenity") and cathinones (e.g., "bath salts") has proliferated in recent years; however, there is a gap in research examining prevalence among offender samples. This study examined demographics, drug use, mental health characteristics, and criminal histories of NPS users compared to non-NPS users within an offender sample entering drug treatment. Using logistic regression analysis, combined 2013-2015 assessment data were examined (N = 8,791)...
August 16, 2017: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/28800377/antidote-to-cannabinoid-intoxication-inverse-cannabinoid-receptor-one-cb1-agonism-by-n-piperidin-1-yl-5-4-iodophenyl-1-2-4-dichlorophenyl-4-methyl-1h-pyrazole-3-carboxamidse-am251-reverses-the-hypothermic-effects-of-cannabinoid-receptor-one-agonism-by-1-naphthalenyl
#4
Gareth Pryce, David Baker
BACKGROUND & PURPOSE: Cannabis is a recreational drug leading to intoxication, due to cannabinoid receptor one (CB1 ) stimulation. However, more recently herbs mixed with synthetic cannabinoids sometimes known as "Spice" and "Black Mamba" have been increasing used and their high CB1 receptor affinity means not only marked intoxication, but life-threatening complications and an increasing number of deaths. Whilst many studies have indicated that prophylactic CB1 receptor antagonism can block cannabimimetic effects in animals and humans...
August 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28799775/a-review-of-the-therapeutic-antitumor-potential-of-cannabinoids
#5
Višnja Bogdanović, Jasminka Mrdjanović, Ivana Borišev
OBJECTIVES: The aim of this review is to discuss cannabinoids from a preclinical and clinical oncological perspective and provide the audience with a concise, retrospective overview of the most significant findings concerning the potential use of cannabinoids in cancer treatment. METHODS: A literature survey of medical and scientific databases was conducted with a focus on the biological and medical potential of cannabinoids in cancer treatment. RESULTS: Cannabis sativa is a plant rich in more than 100 types of cannabinoids...
August 11, 2017: Journal of Alternative and Complementary Medicine: Research on Paradigm, Practice, and Policy
https://www.readbyqxmd.com/read/28794966/synthetic-cannabinoid-induced-acute-respiratory-depression-case-series-and-literature-review
#6
Mark Henry Alon, Margaret Olibrice Saint-Fleur
Synthetic Cannabinoids are a street drug that is widely attainable and cheap compared to natural cannabis, and has variable potency and unpredictable effects with no commercially available diagnostic test to confirm its presence. Similar to natural cannabis, Synthetic Cannabinoid intoxication can present in several ways with the most common emergency room presentations to be of neurologic and psychiatric manifestation. The respiratory depressive effect of Synthetic Cannabinoids has not been well documented in medical literature...
2017: Respiratory Medicine Case Reports
https://www.readbyqxmd.com/read/28792725/pharmacology-of-cumyl-carboxamide-synthetic-cannabinoid-new-psychoactive-substances-nps-cumyl-bica-cumyl-pica-cumyl-5f-pica-cumyl-5f-pinaca-and-their-analogues
#7
Mitchell Longworth, Samuel D Banister, Rochelle Boyd, Richard C Kevin, Mark Connor, Iain S McGregor, Michael Kassiou
Synthetic cannabinoids (SC) are the largest class of new psychoactive substances (NPS), and are increasingly associated with serious adverse effects. The majority of SC NPS are 1,3-disubstituted indoles and indazoles featuring a diversity of subunits at the 1- and 3-positions. Most recently, cumyl-derived indole- and indazole-3-carboxamides have been detected by law enforcement agencies and by emergency departments. Herein we describe the synthesis, characterization, and pharmacology of SCs CUMYL-BICA, CUMYL-PICA, CUMYL-5F-PICA, CUMYL-PINACA, CUMYL-5F-PINACA, and related analogues...
August 11, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28777688/attitudes-and-beliefs-about-new-psychoactive-substance-use-among-electronic-dance-music-party-attendees
#8
Joseph J Palamar, Patricia Acosta, Charles M Cleland
BACKGROUND: Attitudes and beliefs about drug use have been shown to be robust correlates of use of drugs such as alcohol, marijuana, and cocaine; however, little is known regarding attitudes or beliefs about new psychoactive substances (NPS). We sought to examine attitudes and beliefs about NPS and how they relate to self-reported use in a high-risk population-electronic dance music (EDM) party attendees. METHOD: 1,048 individuals (age 18-40) were surveyed entering EDM parties in New York City in 2016...
August 4, 2017: Substance Use & Misuse
https://www.readbyqxmd.com/read/28771321/activity-based-detection-of-consumption-of-synthetic-cannabinoids-in-authentic-urine-samples-using-a-stable-cannabinoid-reporter-system
#9
Annelies Cannaert, Florian Franz, Volker Auwärter, Christophe P Stove
Synthetic cannabinoids (SCs) continue to be the largest group of new psychoactive substances (NPS) monitored by the European Monitoring Center of Drugs and Drugs of Abuse (EMCDDA). The identification and subsequent prohibition of single SCs has driven clandestine chemists to produce analogues of increasing structural diversity, intended to evade legislation. That structural diversity, combined with the mostly unknown metabolic profiles of these new SCs, poses a big challenge for the conventional targeted analytical assays, as it is difficult to screen for 'unknown' compounds...
August 3, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28768940/inhalation-exposure-method-for-illegal-drugs
#10
Akiko Inomata, Akio Ogata, Yukie Tada, Akemichi Nagasawa, Katsuhiro Yuzawa, Hiroshi Ando, Yoshikazu Kubo, Hiroshi Takahashi, Fujifumi Kaihoko, Kazuyoshi Tanaka, Jun'ichi Nakajima, Atsuko Suzuki, Nozomi Uemura, Takako Moriyasu, Daisuke Watanabe, Kei Ishihara, Takashi Usami, Satoru Kamei, Yasuaki Kohno
 We developed a new inhalation exposure method to evaluate effects of synthetic cannabimimetics that are being distributed as new, unregulated drugs in the Tokyo area. We selected the commercial product "SOUTOU" containing AB-CHMINACA and 5F-AMB as the test drug and dried marshmallow (Althaea officinalis) leaves as the negative control. A half cigarette packed with dried marshmallow leaves or SOUTOU was ignited, then mainstream smoke from each was delivered to five mice in an exposure box. After the cigarettes were fully consumed, neurobehavioral observations and a catalepsy test were performed at 15, 30 and 60 min after exposure...
2017: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/28764574/designer-drugs-review-and-implications-for-emergency-management
#11
A Pourmand, M Mazer-Amirshahi, S Chistov, A Li, M Park
In the past 10 years, "designer drugs" such as synthetic cannabinoids and cathinones have emerged and come into widespread use, resulting in more overdose cases involving these new drugs in the United States. Emergency departments regularly treat a diverse array of drug intoxications, and providers must be cognizant of novel drugs of abuse and the associated clinical presentations in order to provide the most appropriate care. This review aims to describe the epidemiology, mechanism of action, clinical presentation, and treatment of intoxication for both the common and newest drugs of abuse...
January 1, 2017: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/28756090/single-oral-dose-of-cannabinoid-derivate-loaded-plga-nanocarriers-relieves-neuropathic-pain-for-eleven-days
#12
E Berrocoso, R Rey-Brea, M Fernández-Arévalo, J A Micó, Lucía Martín-Banderas
Neuropathic pain, resistant to opiates and other drugs, is a chronic/persistent state with a complex treatment and often poor efficacy. In this scenario, cannabinoids are increasingly regarded as a genuine alternative. In this paper, and in an experimental animal model of neuropathic pain, we studied the efficacy of three kinds of PLGA nanoparticles containing synthetic cannabinoid CB13: (i) plain nanoparticles (PLGA); (ii) particles coated with PEG chains (PLGA+PEG) and (iii) particles possessing hydrophilic surfaces obtained by covalently binding PEG chains (PLGA-PEG)...
July 26, 2017: Nanomedicine: Nanotechnology, Biology, and Medicine
https://www.readbyqxmd.com/read/28750809/assessing-allosteric-modulation-of-cb1-at-the-receptor-and-cellular-levels
#13
Caitlin E Scott, Debra A Kendall
The cannabinoid CB1 receptor is abundant in the central nervous system and regulates neuronal transmission and other key physiological processes including those leading to pain, inflammation, memory, and feeding behavior. CB1 is activated by the endogenous ligands, arachidonoyl ethanolamine and 2-arachidonoyl glycerol, by various synthetic ligands (e.g., CP55940), and by Δ(9)-tetrahydrocannabinol, the psychoactive component of Cannabis sativa. These CB1 ligands are orthosteric and transduce downstream signals by binding CB1 and primarily inducing Gi coupling, but Gs and β-arrestin coupling are also possible...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28750806/new-methods-for-the-synthesis-of-cannabidiol-derivatives
#14
Ana Lago-Fernandez, Vanessa Redondo, Laura Hernandez-Folgado, Laura Figuerola-Asencio, Nadine Jagerovic
Cannabidiol (CBD) is one of the most abundant components isolated from Cannabis sativa. However, CBD is a nonpsychotropic phytocannabinoid. In the last decade, there has been a growing interest in its therapeutic effects. This is why this natural product represents a lead structure for the development of new cannabinoid compounds. Even though chemistry of CBD has been explored for more than 30 years, the synthesis of only a few derivatives has been described. This chapter first reviews the synthetic methods for the preparation of CBD and derivatives...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28747489/a-novel-selective-inverse-agonist-of-the-cb2-receptor-as-a-radiolabeled-tool-compound-for-kinetic-binding-studies
#15
Andrea Martella, Huub Sijben, Arne Rufer, Juergen Fingerle, Uwe Grether, Christoph Ullmer, Thomas Hartung, Ad IJzerman, Mario van der Stelt, Laura Heitman
The endocannabinoid system (ECS) and in particular the cannabinoid receptor 2 (CB2R), raised the interest of many medicinal chemistry programs for its therapeutic relevance in several (patho)physiological processes. However, the the physico-chemical properties of tool compounds for CB2R (e.g. the radioligand [(3)H]CP55,940) are not optimal, despite the research efforts in developing effective drugs to target this system. At the same time, the importance of drug-target binding kinetics is growing, as the kinetic binding profile of a ligand may provide important insights for the resulting in vivo efficacy...
July 26, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28730896/cannabinoid-hyperemesis-syndrome-potential-mechanisms-for-the-benefit-of-capsaicin-and-hot-water-hydrotherapy-in-treatment
#16
John R Richards, Jeff M Lapoint, Guillermo Burillo-Putze
INTRODUCTION: Cannabinoid hyperemesis syndrome is a clinical disorder that has become more prevalent with increasing use of cannabis and synthetic cannabinoids, and which is difficult to treat. Standard antiemetics commonly fail to alleviate the severe nausea and vomiting characteristic of the syndrome. Curiously, cannabinoid hyperemesis syndrome patients often report dramatic relief of symptoms with hot showers and baths, and topical capsaicin. OBJECTIVES: In this review, we detail the pharmacokinetics and pharmacodynamics of capsaicin and explore possible mechanisms for its beneficial effect, including activation of transient receptor potential vanilloid 1 and neurohumoral regulation...
July 21, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28716633/the-synthetic-cannabinoid-win55212-2-ameliorates-traumatic-spinal-cord-injury-via-inhibition-of-gapdh-siah1-in-a-cb2-receptor-dependent-manner
#17
Bin-Xiao Su, Xin Chen, Jia Huo, Shu-Yun Guo, Rui Ma, Yan-Wu Liu
The essential role of GAPDH/Siah1 signaling pathway in the pathogenesis of various injurious conditions such as traumatic spinal cord injury (SCI) has been gradually recognized. However, the drugs targeting this signaling pathway are still lacking. The endocannabinoid system, including its receptors (CB1 and CB2), act as neuroprotective and immunomodulatory modulators in SCI. WIN55212-2, an agonist for CB1 and CB2 receptors, has been demonstrated with anti-inflammatory and anti-apoptotic effects in multiple neurological diseases...
July 14, 2017: Brain Research
https://www.readbyqxmd.com/read/28713291/an-expanding-world-of-novel-psychoactive-substances-opioids
#18
REVIEW
Jolanta B Zawilska
The abuse of novel psychoactive substances (NPS) has been increasing dramatically worldwide since late 2000s. By the end of 2015, more than 560 NPS had been reported to the European Monitoring Centre for Drugs and Drug Addiction. Although the most popular compounds are synthetic cannabinoids and psychostimulatory derivatives of cathinone (so-called β-keto-amphetamines), novel synthetic opioids have recently emerged on the recreational drug market. They include fentanyl (a potent narcotic analgesic) and its analogs (e...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/28707493/ab-chminaca-induced-sudden-death-from-non-cardiogenic-pulmonary-edema
#19
Hideyuki Maeda, Ruri Kikura-Hanajiri, Maiko Kawamura, Erika Nagashima, Ken-Ichi Yoshida
CONTEXT: Despite widespread use of diverse synthetic cannabinoid (sCB) compounds, the pathophysiology associated with intoxication with many sCB compounds, including AB-CHMINACA, is poorly understood, as is their metabolism and distribution into blood and organs. CASE DETAILS: A young man died shortly after ingesting an herb product containing sCB compounds. Toxicological analyses of blood samples revealed high levels of AB-CHMINACA (7.61 ± 0.59 ng/mL) and its metabolites (M2, 56...
July 14, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28706566/motor-vehicle-collisions-caused-by-the-super-strength-synthetic-cannabinoids-mam-2201-5f-pb-22-5f-ab-pinaca-5f-amb-and-5f-adb-in-japan-experienced-from-2012-to-2014
#20
REVIEW
Shuji Kaneko
From 2012 to 2014 in Japan, 214 cases of motor vehicle collisions were attributed to the use of illegal drugs. In 93 out of 96 investigated cases, the causative agents were a variety of synthetic cannabinoids (SCs). These SCs can be classified into three groups according to the lineage of the chemical structures: (1) naphthoyl indoles, such as MAM-2201, (2) quinolinyl ester indoles, such as 5F-PB-22, and (3) indazole carboxamides, such as 5F-AB-PINACA, 5F-AMB, and 5F-ADB. These SCs became available sequentially with increasing cannabinoid CB1 agonist potencies and reached a nationwide outbreak in the summer of 2014...
2017: Forensic Toxicology
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