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Synthetic cannabinoids

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https://www.readbyqxmd.com/read/29668081/lipocalin-type-prostaglandin-d-synthase-is-a-novel-phytocannabinoid-binding-protein
#1
Matthew W Elmes, Anthony D Volpe, Simon d'Oelsnitz, Joseph M Sweeney, Martin Kaczocha
Lipocalin-type prostaglandin D synthase (L-PGDS; EC:5.3.99.2) is an enzyme with dual functional roles as a prostaglandin D2 -synthesizing enzyme and as an extracellular transporter for diverse lipophilic compounds in the cerebrospinal fluid (CSF). Transport of hydrophobic endocannabinoids is mediated by serum albumin in the blood and intracellularly by the fatty acid binding proteins, but no analogous transport mechanism has yet been described in CSF. L-PGDS has been reported to promiscuously bind a wide variety of lipophilic ligands and is among the most abundant proteins found in the CSF...
April 18, 2018: Lipids
https://www.readbyqxmd.com/read/29659506/in-vitro-inhibitory-effects-of-synthetic-cannabinoid-eam-2201-on-cytochrome-p450-and-udp-glucuronosyltransferase-enzyme-activities-in-human-liver-microsomes
#2
Tae Yeon Kong, Soon-Sang Kwon, Jae Chul Cheong, Hee Seung Kim, Jin Young Kim, Hye Suk Lee
EAM-2201, a synthetic cannabinoid, is a potent agonist of the cannabinoid receptors that is widely abused as an illicit recreational drug in combination with other drugs. To evaluate the potential of EAM-2201 as a perpetrator of drug–drug interactions, the inhibitory effects of EAM-2201 on major drug-metabolizing enzymes, cytochrome P450s (CYPs) and uridine 5′-diphospho-glucuronosyltransferases (UGTs) were evaluated in pooled human liver microsomes using liquid chromatography–tandem mass spectrometry (LC-MS/MS)...
April 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29627825/effect-of-cb1-ligands-on-neurogenic-and-myogenic-contractile-responses-in-the-guinea-pig-ileum
#3
Josef Donnerer, Ingrid Liebmann
This study aimed at investigating whether the synthetic cannabinoid receptor agonist (+)-WIN 55212-2 has neurogenic and myogenic relaxant effects on the longitudinal muscle-myenteric plexus (LMMP) strip of the guinea-pig ileum. (+)-WIN 55212-2, 1-1,000 nmol/L, concentration-dependently inhibited both the electrical stimulation-induced cholinergic twitch responses as well as the myogenic smooth muscle contractions in the LMMP preparation. SR-141716A (rimonabant) 1-1,000 nmol/L, the cannabinoid CB1 receptor antagonist, being without effect on its own, antagonized the (+)-WIN 55212-2-induced effects...
April 6, 2018: Pharmacology
https://www.readbyqxmd.com/read/29609727/medical-cannabis-and-the-treatment-of-obstructive-sleep-apnea-an-american-academy-of-sleep-medicine-position-statement
#4
Kannan Ramar, Ilene M Rosen, Douglas B Kirsch, Ronald D Chervin, Kelly A Carden, R Nisha Aurora, David A Kristo, Raman K Malhotra, Jennifer L Martin, Eric J Olson, Carol L Rosen, James A Rowley
The diagnosis and effective treatment of obstructive sleep apnea (OSA) in adults is an urgent health priority. Positive airway pressure (PAP) therapy remains the most effective treatment for OSA, although other treatment options continue to be explored. Limited evidence citing small pilot or proof of concept studies suggest that the synthetic medical cannabis extract dronabinol may improve respiratory stability and provide benefit to treat OSA. However, side effects such as somnolence related to treatment were reported in most patients, and the long-term effects on other sleep quality measures, tolerability, and safety are still unknown...
March 30, 2018: Journal of Clinical Sleep Medicine: JCSM: Official Publication of the American Academy of Sleep Medicine
https://www.readbyqxmd.com/read/29608249/targeted-and-non-targeted-metabolite-identification-of-mam-2201-in-human-mouse-and-rat-hepatocytes
#5
Ju-Hyun Kim, Tae Yeon Kong, Ju-Yeon Moon, Kyung Ho Choi, Yong-Yeon Cho, Han Chang Kang, Joo Young Lee, Hye Suk Lee
MAM-2201 is a fluorinated naphthoylindole synthetic cannabinoid with potent psychoactive properties that has been detected as an active ingredient in herbal incense blends. To gain a greater understanding of MAM-2201 metabolism and to compare the metabolic fate in humans with those in animals, the metabolism of MAM-2201 in human, mouse, and rat hepatocytes was investigated using liquid chromatography-high-resolution mass spectrometry combined with targeted and non-targeted metabolite profiling approaches. Nineteen phase I metabolites (M1-M19) reported previously in human liver microsomes and 13 novel metabolites were identified in human, mouse, and rat hepatocytes: one phase I metabolite (M20) and 12 phase II metabolites including six glucuronides (G1-G6), one sulfate (S1), and five glutathione (GSH) conjugates (GS1-GS5) of MAM-2201 metabolites...
April 2, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29607523/a-new-cause-of-ischaemic-priapism-synthetic-cannabinoids
#6
M Ortac, Y Pazır, A Kadıoğlu
Priapism is a urological emergency that needs early intervention and may lead to irreversible cavernosal damage. Ischaemic priapism is the most common type, which is frequently idiopathic and commonly associated with haematological diseases, medications or recreational drugs. Synthetic cannabinoids (SCs) have been increasingly used all over the world, particularly among young-adult population. SCs can cause severe adverse effects on several organ systems. However, there are no studies in the literature which have stated the possible relationship between using of SCs and priapism...
April 1, 2018: Andrologia
https://www.readbyqxmd.com/read/29605179/development-of-a-micro-solid-phase-extraction-molecularly-imprinted-polymer-technique-for-synthetic-cannabinoids-assessment-in-urine-followed-by-liquid-chromatography-tandem-mass-spectrometry
#7
Juan Sánchez-González, Sara Odoardi, Ana María Bermejo, Pilar Bermejo-Barrera, Francesco Saverio Romolo, Antonio Moreda-Piñeiro, Sabina Strano-Rossi
Several molecularly imprinted polymers (MIPs) have been synthesized for the first time using various synthetic cannabinoids (JWH007, JWH015 and JWH098) as template molecules. Ethylene dimethacrylate (EDMA) was used as a functional monomer for all cases. Similarly, divinylbenzene (DVB) and 2,2'-azobisisobutyronitrile (AIBN) were used as cross-linker and initiator, respectively. The prepared MIPs have been fully characterized and evaluated as new selective adsorbents for micro-solid phase extraction (μ-SPE) of synthetic cannabinoids in urine...
March 26, 2018: Journal of Chromatography. A
https://www.readbyqxmd.com/read/29601658/chromatographic-characterisation-of-11-phytocannabinoids-quantitative-and-fit-to-purpose-performance-as-a-function-of-extra-column-variance
#8
Matthew Noestheden, Gareth Friedlander, Jason Anspach, Scott Krepich, K C Hyland, Wesley F Zandberg
INTRODUCTION: Cannabis sativa L. (cannabis) is utilised as a therapeutic and recreational drug. With the legalisation of cannabis in many countries and the anticipated regulation of potency that will accompany legalisation, analytical testing facilities will require a broadly applicable, quantitative, high throughput method to meet increased demand. Current analytical methods for the biologically active components of cannabis (phytocannabinoids) suffer from low throughput and/or an incomplete complement of relevant phytocannabinoids...
March 30, 2018: Phytochemical Analysis: PCA
https://www.readbyqxmd.com/read/29601300/cannabinoids-in-health-and-disease-pharmacological-potential-in-metabolic-syndrome-and-neuroinflammation
#9
REVIEW
Andrea Mastinu, Marika Premoli, Giulia Ferrari-Toninelli, Simone Tambaro, Giuseppina Maccarinelli, Maurizio Memo, Sara Anna Bonini
The use of different natural and/or synthetic preparations of Cannabis sativa is associated with therapeutic strategies for many diseases. Indeed, thanks to the widespread diffusion of the cannabinoidergic system in the brain and in the peripheral districts, its stimulation, or inhibition, regulates many pathophysiological phenomena. In particular, central activation of the cannabinoidergic system modulates the limbic and mesolimbic response which leads to food craving. Moreover, cannabinoid agonists are able to reduce inflammatory response...
March 30, 2018: Hormone Molecular Biology and Clinical Investigation
https://www.readbyqxmd.com/read/29577658/metabolism-study-for-cumyl-4cn-binaca-in-human-hepatocytes-and-authentic-urine-specimens-free-cyanide-is-formed-during-the-main-metabolic-pathway
#10
Anna Åstrand, Svante Vikingsson, Daniel Lindstedt, Gunilla Thelander, Henrik Green, Robert Kronstrand, Ariane Wohlfarth
To further elucidate the metabolism of CUMYL-4CN-BINACA, a new synthetic cannabinoid with a cyano group, and to evaluate biomarkers, we incubated the substance in human hepatocytes and analysed nine authentic urine specimens. We also quantified CUMYL-4CN-BINACA and cyanide in blood and provide comprehensive data on the seven autopsy cases, five determined CUMYL-4CN-BINACA intoxications. For metabolite elucidation, CUMYL-4CN-BINACA was incubated with pooled human hepatocytes up to 5 h, urine samples were analysed with and without enzymatic hydrolysis...
March 25, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29575721/synthesis-pharmacological-evaluation-and-docking-studies-of-novel-pyridazinone-based-cannabinoid-receptor-type-2-ligands
#11
Gabriele Murineddu, Patricia Reggio, Stefania Gessi
In the last years cannabinoid type 2 receptors (CB2R) have emerged as promising therapeutic targets in a wide variety of diseases. Selective ligands of CB2R are devoid of psychoactive effect typically observed for CB1R ligands. Taking advantage of our recent studies on a class of pyridazinone 4-carboxamides, further structural modifications on pyridazinone core were explored to better investigate the structure-activity relationships for this promising scaffold with the aim to develop potent CB2R ligands. In binding assays two of the new synthetized compounds (2 and 22) showed high CB2R affinity, with Ki values of 2...
March 25, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29562280/the-use-of-cannabinoids-in-colitis-a-systematic-review-and-meta-analysis
#12
Daniel G Couch, Henry Maudslay, Brett Doleman, Jonathan N Lund, Saoirse E O'Sullivan
Background: Clinical trials investigating the use of cannabinoid drugs for the treatment of intestinal inflammation are anticipated secondary to preclinical literature demonstrating efficacy in reducing inflammation. Methods: We systematically reviewed publications on the benefit of drugs targeting the endo-cannabinoid system in intestinal inflammation. We collated studies examining outcomes for meta-analysis from EMBASE, MEDLINE and Pubmed until March 2017. Quality was assessed according to mSTAIR and SRYCLE score...
March 19, 2018: Inflammatory Bowel Diseases
https://www.readbyqxmd.com/read/29559524/activity-based-detection-of-cannabinoids-in-serum-and-plasma-samples
#13
Annelies Cannaert, Jolien Storme, Cornelius Hess, Volker Auwärter, Sarah M R Wille, Christophe P Stove
BACKGROUND: Synthetic cannabinoids are the largest group of new psychoactive substances monitored by the European Monitoring Center of Drugs and Drug Addiction. The rapid proliferation of novel analogs makes the detection of these new derivatives challenging and has initiated considerable interest in the development of so-called "untargeted" screening strategies to detect these compounds. METHODS: We developed new, stable bioassays in which cannabinoid receptor activation by cannabinoids led to recruitment of truncated β-arrestin 2 (βarr2) to the cannabinoid receptors, resulting in functional complementation of a split luciferase, allowing readout via bioluminescence...
March 20, 2018: Clinical Chemistry
https://www.readbyqxmd.com/read/29557759/cannabis-and-psychosis-what-do-we-know-and-what-should-we-do
#14
Marco Colizzi, Robin Murray
It is now incontrovertible that heavy use of cannabis increases the risk of psychosis. There is a dose-response relationship and high potency preparations and synthetic cannabinoids carry the greatest risk. It would be wise to await the outcome of the different models of legalisation that are being introduced in North America, before deciding whether or not to follow suit. Declaration of interest None.
April 2018: British Journal of Psychiatry: the Journal of Mental Science
https://www.readbyqxmd.com/read/29549742/metabolism-of-the-synthetic-cannabinoids-amb-chmica-and-5c-akb48-in-pooled-human-hepatocytes-and-rat-hepatocytes-analyzed-by-uhplc-ims-hr-ms-e
#15
Marie Mardal, Petur Weihe Dalsgaard, Bing Qi, Christian Brinch Mollerup, Pieter Annaert, Kristian Linnet
The main analytical targets of synthetic cannabinoids are often metabolites. With the high number of new psychoactive substances entering the market, suitable workflows are needed for analytical target identification in biological samples. The aims of this study were to identify the main metabolites of the synthetic cannabinoids, AMB-CHMICA and 5C-AKB48, using an in silico-assisted workflow with analytical data acquired using ultra-high-performance liquid chromatography-(ion mobility spectroscopy)-high resolution-mass spectrometry in data-independent acquisition mode (UHPLC-(IMS)-HR-MSE )...
March 10, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29549157/molecular-and-behavioral-pharmacological-characterization-of-abused-synthetic-cannabinoids-mmb-and-mdmb-fubinaca-mn-18-nnei-cumyl-pica-and-5-fluoro-cumyl-pica
#16
Thomas F Gamage, Charlotte E Farquhar, Timothy W Lefever, Julie A Marusich, Richard C Kevin, Iain S McGregor, Jenny L Wiley, Brian F Thomas
Synthetic cannabinoids are a class of novel psychoactive substances that exhibit high affinity at the cannabinoid type-1 (CB1) receptor and produce effects similar to those of THC, the primary psychoactive constituent of cannabis. Illicit drug manufacturers are continually circumventing laws banning the sale of synthetic cannabinoids by synthesizing novel structures and doing so with little regard for their potential impact on pharmacological and toxicological effects. Synthetic cannabinoids produce a wide range of effects including cardiotoxicity, seizure activity, and kidney damage and can result in death...
March 16, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29538266/synthetic-cannabinoid-exposure-in-adolescents-presenting-for-emergency-care
#17
Meghan Gilley, Jeffrey Brent, Diane P Calello, Paul Wax, Yaron Finkelstein
OBJECTIVE: The objective of this study was to characterize the clinical picture and management of synthetic cannabinoid exposure in a cohort of adolescents. METHODS: Using the 45 participating sites of the Toxicology Investigators Consortium Registry, a North American database, we conducted an observational study of a prospectively collected cohort. We identified all adolescent (12-19 years) cases of synthetic cannabinoid exposure who have received medical toxicology consultation between January 2012 and December 2016...
March 12, 2018: Pediatric Emergency Care
https://www.readbyqxmd.com/read/29535650/repeated-exposure-to-the-spice-cannabinoid-jwh-018-induces-tolerance-and-enhances-responsiveness-to-5-ht-1a-receptor-stimulation-in-male-rats
#18
Joshua S Elmore, Michael H Baumann
Naphthalen-1-yl-(1-pentylindol-3-yl)methanone (JWH-018) is a synthetic compound found in psychoactive "spice" products that activates cannabinoid receptors. Preclinical evidence suggests that exposure to synthetic cannabinoids increases 5-HT2A/2C receptor function in the brain, an effect which might contribute to psychotic symptoms. Here, we hypothesized that repeated exposures to JWH-018 would enhance behavioral responsiveness to the 5-HT2A/2C receptor agonist DOI. Male Sprague-Dawley rats fitted with subcutaneously (sc) temperature transponders received daily injections of JWH-018 (1...
2018: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/29534614/annals-express-analytical-evidence-to-show-letters-impregnated-with-novel-psychoactive-substances-nps-are-a-means-of-getting-drugs-to-inmates-within-the-uk-prison-service
#19
Loretta Theresa Ford, Jonathan David Berg
Novel psychotropic substances (NPS) also known as legal highs are a major concern in UK prisons, fuelling violence and putting a strain on resources for inmates requiring medical treatment for adverse effects. We provide a clinical toxicology service including routine screening for NPS. In 2015 we were approached by Her Majesty Prison Service (HMPS) search dog training team to advise on which NPS to target, and again in 2016 to further provide analytical support to test five letters which the dogs positively identified for NPS during routine searches of prison mail rooms...
January 1, 2018: Annals of Clinical Biochemistry
https://www.readbyqxmd.com/read/29522717/altered-metabolism-of-synthetic-cannabinoid-jwh-018-by-human-cytochrome-p450-2c9-and-variants
#20
Amy L Patton, Kathryn A Seely, Azure L Yarbrough, William Fantegrossi, Laura P James, Keith R McCain, Ryoichi Fujiwara, Paul L Prather, Jeffery H Moran, Anna Radominska-Pandya
Synthetic cannabinoids (SCBs), synonymous with 'K2', 'Spice' or 'synthetic marijuana', are psychoactive drugs of abuse that frequently result in clinical effects and toxicity more severe than those classically associated with Δ9 -tetrahydrocannabinol such as extreme agitation, hallucinations, supraventricular tachycardia, syncope, and seizures. JWH-018 is one of the earliest compounds identified in various SCB products, and our laboratory previously demonstrated that JWH-018 undergoes extensive metabolism by cytochromes P450 (P450), binds to, and activates cannabinoid receptors (CBRs)...
March 6, 2018: Biochemical and Biophysical Research Communications
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