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N-acyl or cannabinoid or NAPE

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https://www.readbyqxmd.com/read/29458190/cannabinoids-prevent-depressive-like-symptoms-and-alterations-in-bdnf-expression-in-a-rat-model-of-ptsd
#1
Or Burstein, Noa Shoshan, Ravid Doron, Irit Akirav
Posttraumatic stress disorder (PTSD) is a debilitating condition highly comorbid with depression. The endocannabinoid (eCB) system and brain-derived neurotrophic factor (BDNF) are suggestively involved in both disorders. We examined whether cannabinoids can prevent the long-term depressive-like symptoms induced by exposure to the shock and situational reminders (SRs) model of PTSD. The CB1/2 receptor agonist WIN55,212-2 (0.5 mg/kg; i.p.), the fatty acid hydrolase (FAAH) inhibitor URB597 (0.3 mg/kg, i.p.) or vehicle were administered 2 h after severe shock...
February 16, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29457829/species-specific-susceptibility-to-cannabis-induced-convulsions
#2
Benjamin J Whalley, Hong Lin, Lynne Bell, Thomas Hill, Amesha Patel, Roy A Gray, C Elizabeth Roberts, Orrin Devinsky, Michael Bazelot, Claire M Williams, Gary J Stephens
BACKGROUND AND PURPOSE: Numerous claims are made for cannabis' therapeutic utility upon human seizures, but concerns persist about risks. A potential confounder is the presence of both Δ9 -tetrahydrocannabinol (Δ9 -THC), variously reported to be pro- and anti-convulsant, and cannabidiol (CBD), widely confirmed as anticonvulsant. Therefore, we investigated effects of prolonged exposure to different Δ9 -THC/CBD cannabis extracts on seizure activity and associated measures of endocannabinoid (eCB) system signalling...
February 19, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29456791/nonacidic-chemotype-possessing-n-acylated-piperidine-moiety-as-potent-farnesoid-x-receptor-fxr-antagonists
#3
Naoki Teno, Yukiko Yamashita, Yusuke Iguchi, Ko Fujimori, Mizuho Une, Tomoko Nishimaki-Mogami, Takie Hiramoto, Keigo Gohda
Farnesoid X receptor (FXR) plays a major role in the control of cholesterol metabolism. Antagonizing transcriptional activity of FXR is an effective means to treat the relevant metabolic syndrome. Some of antagonists so far have the charged functions; however, they may negatively affect the pharmacokinetics. We describe herein a structure-activity relationship (SAR) exploration of nonacidic FXR antagonist 6 focusing on two regions in the structure and biological evaluation of nonacidic 10 with the characteristic N -acylated piperidine group obtained from SAR studies...
February 8, 2018: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29456490/limited-access-to-a-high-fat-diet-alters-endocannabinoid-tone-in-female-rats
#4
Valentina Satta, Maria Scherma, Fabiana Piscitelli, Paolo Usai, M Paola Castelli, Tiziana Bisogno, Walter Fratta, Paola Fadda
Emerging evidence suggest an impaired endocannabinoid activity in the pathophysiology of binge eating disorder (BED). Herein, we investigated whether endocannabinoid tone could be modified as a consequence of dietary-induced binge eating in female rats. For this purpose, brain levels of the endocannabinoids anandamide (AEA) and 2-arachidonoyl glycerol (2-AG), as well as two endocannabinoid-like lipids, oleoylethanolamide (OEA) and palmitoylethanolamide (PEA), were assessed in different brain areas involved in the hedonic feeding (i...
2018: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/29455452/cannabinoids-in-arterial-pulmonary-and-portal-hypertension-mechanisms-of-action-and-potential-therapeutic-significance
#5
REVIEW
Barbara Malinowska, Marek Toczek, Anna Pędzińska-Betiuk, Eberhard Schlicker
The endocannabinoid system is overactivated in arterial, pulmonary and portal hypertension. In this paper, we present limited clinical data concerning the role of cannabinoids in human hypertension including polymorphism of endocannabinoid system components. We underline differences between the acute cannabinoid administration and their potential hypotensive effect after chronic application in experimental hypertension. We discuss pleiotropic effects of cannabinoids on the cardiovascular system mediated via numerous neuronal and non-neuronal mechanisms both in normo- and in hypertension...
February 18, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29454037/melatonin-attenuates-%C3%AE-9-tetrahydrocannabinol-induced-reduction-in-rat-sperm-motility-and-kinematics-in-vitro
#6
Isiaka Abdullateef Alagbonsi, Luqman Aribidesi Olayaki
The use of Cannabis sativa (CS) has been widely demonstrated to have detrimental effect on male reproductive functions. Despite the well-known existence of endocannabinoid and melatonergic systems in semen, the physiological significance of their interaction is not understood. We recently showed that melatonin exacerbates the CS-induced gonadotoxicity in-vivo. To overcome the limitations associated with our in-vivo studies and further understand the role of cannabinoid-melatonin relationship in sperm functions, this study investigated the in-vitro effect of tetrahydrocannabinol (THC) and/or melatonin on motility and kinematics of capacitating rat sperms...
February 14, 2018: Reproductive Toxicology
https://www.readbyqxmd.com/read/29454025/early-alteration-of-distribution-and-activity-of-hippocampal-type-1-cannabinoid-receptor-in-alzheimer-s-disease-like-mice-overexpressing-the-human-mutant-amyloid-precursor-protein
#7
Mauro Maccarrone, Antonio Totaro, Alessandro Leuti, Giacomo Giacovazzo, Lucia Scipioni, Dalila Mango, Roberto Coccurello, Robert Nisticò, Sergio Oddi
Besides its involvement in Alzheimer's disease (AD) as precursor of the neurotoxic amyloid peptides, the pathophysiological impact of brain accumulation of amyloid precursor protein (APP) is not yet well understood. Recent studies reported that APP interacts with other membrane proteins, including G protein coupled receptors, affecting their biological functions. Here, we focused on the study of the potential impact of human mutant APP on expression, distribution and activity of type-1 cannabinoid (CB 1 ) receptor in the hippocampus of Tg2576 mice, an AD-like mice model...
February 14, 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29453495/comparison-of-concentrations-of-drugs-between-blood-samples-with-and-without-fluoride-additive-important-findings-for-%C3%AE-9-tetrahydrocannabinol-and-amphetamine
#8
Christopher Wiedfeld, Julia Krueger, Gisela Skopp, Frank Musshoff
Fluoride is a common stabilizing agent in forensic toxicology to avoid the frequent problem of degradation of drugs in blood samples especially described for cocaine. In cases only samples with addition of fluoride are available, it is a crucial question if also concentrations of common drugs other than cocaine (amphetamines, opiates and cannabinoids) are affected by fluoride. So far, there are only rare literature data available on discrepant results especially for Δ 9 -tetrahydrocannabinol (THC). In this study, comparative analysis of positive tested paired routine plasma/serum samples (n = 375), collected at the same time point (one device with and one without fluoride), was carried out with special focus on cannabinoids...
February 17, 2018: International Journal of Legal Medicine
https://www.readbyqxmd.com/read/29453460/development-and-initial-characterization-of-a-novel-ghrelin-receptor-crispr-cas9-knockout-wistar-rat-model
#9
L J Zallar, B J Tunstall, C T Richie, Y J Zhang, Z B You, E L Gardner, M Heilig, J Pickel, G F Koob, L F Vendruscolo, B K Harvey, L Leggio
BACKGROUND/OBJECTIVES: Ghrelin, a stomach-derived hormone implicated in numerous behaviors including feeding, reward, stress, and addictive behaviors, acts by binding to the growth hormone secretagogue receptor (GHSR). Here, we present the development, verification, and initial characterization of a novel GHSR knockout (KO) Wistar rat model created with CRISPR genome editing. METHODS: Using CRISPR/Cas9, we developed a GHSR KO in a Wistar background. Loss of GHSR mRNA expression was histologically verified using RNAscope in wild-type (WT; n = 2) and KO (n = 2) rats...
January 30, 2018: International Journal of Obesity: Journal of the International Association for the Study of Obesity
https://www.readbyqxmd.com/read/29453228/targeted-profiling-of-a-thaliana-sub-proteomes-illuminates-new-co-and-post-translationally-n-terminal-myristoylated-proteins
#10
Wojciech Majeran, Jean-Pierre Le Caer, Lalit Ponnala, Thierry Meinnel, Carmela Giglione
N-terminal myristoylation (MYR) is a biologically important co-translational protein lipidation. MYR is difficult to detect in vivo and challenging to predict in silico. We developed a targeted proteomics strategy to identify the Arabidopsis thaliana myristoylated (MYRed) proteome in specific sub-cellular compartments. This global profiling approach allowed us to: (i) identify one third of all open reading frames of the A. thaliana proteome including 54% of the predicted myristoylome; and (ii) establish the first comprehensive plant myristoylome, featuring direct evidence of MYR in 72 proteins...
February 16, 2018: Plant Cell
https://www.readbyqxmd.com/read/29453097/self-assembled-vertically-aligned-au-nanorod-arrays-for-surface-enhanced-raman-scattering-sers-detection-of-cannabinol
#11
Sarah Milliken, Jeff Fraser, Shawn Poirier, John Hulse, Li-Lin Tay
Self-assembled multi-layered vertically aligned gold nanorod (AuNR) arrays have been fabricated by a simple preparation process that requires a balance between the particle concentration and the ionic strength of the solvent. An experimentally determined critical AuNR concentration of 2.0nM and 50mM NaCl produces well-ordered vertically aligned hexagonally close-packed AuNR arrays. We demonstrate surface treatment via UV Ozone cleaning of such samples to allow introduction of analyte molecules (benzenethiol and cannabinol) for effective surface enhanced Raman scattering detection...
January 12, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/29450995/n-acyl-glutarimides-resonance-and-proton-affinities-of-rotationally-inverted-twisted-amides-relevant-to-n-c-o-cross-coupling
#12
Roman Szostak, Michal Szostak
Resonance energies and proton affinities of N-acyl-glutarimides, compared with related twisted acyclic amides of relevance to N-C(O) cross-coupling, are reported. The data demonstrate that amidic resonance in N-acyl-glutarimides practically disappears (E R < 2.8 kcal/mol), while, intriguingly, these amides favor O-protonation despite significant twist. In some cases, N-acyl-glutarimides undergo intramolecular N- to O-acyl migration, indicative of high capacity as acylating reagents. The understanding provided for the high reactivity of N-acyl-glutarimides should facilitate the development of a broadly general N-C(O) amide activation platform...
February 16, 2018: Organic Letters
https://www.readbyqxmd.com/read/29450258/the-cannabinoids-%C3%AE-8-thc-cbd-and-hu-308-act-via-distinct-receptors-to-reduce-corneal-pain-and-inflammation
#13
Dinesh Thapa, Elizabeth A Cairns, Anna-Maria Szczesniak, James T Toguri, Meggie D Caldwell, Melanie E M Kelly
Background and Purpose: Corneal injury can result in dysfunction of corneal nociceptive signaling and corneal sensitization. Activation of the endocannabinoid system has been reported to be analgesic and anti-inflammatory. The purpose of this research was to investigate the antinociceptive and anti-inflammatory effects of cannabinoids with reported actions at cannabinoid 1 (CB 1 R) and cannabinoid 2 (CB 2 R) receptors and/or noncannabinoid receptors in an experimental model of corneal hyperalgesia. Methods: Corneal hyperalgesia (increased pain response) was generated using chemical cauterization of the corneal epithelium in wild-type (WT) and CB 2 R knockout (CB 2 R -/- ) mice...
2018: Cannabis and Cannabinoid Research
https://www.readbyqxmd.com/read/29449262/systematic-review-of-systematic-reviews-for-medical-cannabinoids-pain-nausea-and-vomiting-spasticity-and-harms
#14
G Michael Allan, Caitlin R Finley, Joey Ton, Danielle Perry, Jamil Ramji, Karyn Crawford, Adrienne J Lindblad, Christina Korownyk, Michael R Kolber
OBJECTIVE: To determine the effects of medical cannabinoids on pain, spasticity, and nausea and vomiting, and to identify adverse events. DATA SOURCES: MEDLINE, the Cochrane Database, and the references of included studies were searched. STUDY SELECTION: Systematic reviews with 2 or more randomized controlled trials (RCTs) that focused on medical cannabinoids for pain, spasticity, or nausea and vomiting were included. For adverse events, any meta-analysis for the conditions listed or of adverse events of cannabinoids was included...
February 2018: Canadian Family Physician Médecin de Famille Canadien
https://www.readbyqxmd.com/read/29449241/simplified-guideline-for-prescribing-medical-cannabinoids-in-primary-care
#15
G Michael Allan, Jamil Ramji, Danielle Perry, Joey Ton, Nathan P Beahm, Nicole Crisp, Beverly Dockrill, Ruth E Dubin, Ted Findlay, Jessica Kirkwood, Michael Fleming, Ken Makus, Xiaofu Zhu, Christina Korownyk, Michael R Kolber, James McCormack, Sharon Nickel, Guillermina Noël, Adrienne J Lindblad
OBJECTIVE: To develop a clinical practice guideline for a simplified approach to medical cannabinoid use in primary care; the focus was on primary care application, with a strong emphasis on best available evidence and a promotion of shared, informed decision making. METHODS: The Evidence Review Group performed a detailed systematic review of 4 clinical areas with the best evidence around cannabinoids: pain, nausea and vomiting, spasticity, and adverse events. Nine health professionals (2 generalist family physicians, 2 pain management-focused family physicians, 1 inner-city family physician, 1 neurologist, 1 oncologist, 1 nurse practitioner, and 1 pharmacist) and a patient representative comprised the Prescribing Guideline Committee (PGC), along with 2 nonvoting members (pharmacist project managers)...
February 2018: Canadian Family Physician Médecin de Famille Canadien
https://www.readbyqxmd.com/read/29447909/phosphatidylserine-stimulated-production-of-n-acyl-phosphatidylethanolamines-by-ca-2-dependent-n-acyltransferase
#16
Zahir Hussain, Toru Uyama, Katsuhisa Kawai, Smriti Sultana Binte Mustafiz, Kazuhito Tsuboi, Nobukazu Araki, Natsuo Ueda
N-Acyl-phosphatidylethanolamine (NAPE) is known to be a precursor for various bioactive N-acylethanolamines including the endocannabinoid anandamide. NAPE is produced in mammals through the transfer of an acyl chain from certain glycerophospholipids to phosphatidylethanolamine (PE) by Ca 2+ -dependent or -independent N-acyltransferases. The Ɛ isoform of mouse cytosolic phospholipase A 2 (cPLA 2 Ɛ) was recently identified as a Ca 2+ -dependent N-acyltransferase (Ca-NAT). In the present study, we first showed that two isoforms of human cPLA 2 Ɛ function as Ca-NAT...
February 12, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29446742/development-of-an-in-vitro-drug-delivery-efficiency-test-for-a-pulmonary-toxicokinetic-pig-study
#17
Nadine Schaefer, Ann-Katrin Kroll, Matthias W Laschke, Michael D Menger, Hans H Maurer, Markus R Meyer, Peter H Schmidt
BACKGROUND: Since their appearance on the drugs of abuse market, synthetic cannabinoids (SCs) are gaining increasing toxicological relevance. They are consumed without knowledge of their toxicokinetic (TK) and toxicodynamic properties and human studies are not allowed due to ethical reasons. A controlled animal TK study following nebulization of 4-ethylnaphthalene-1-yl-(1-pentylindole-3-yl)methanone (JWH-210), 2-(4-methoxyphenyl)-1-(1-pentyl-indole-3-yl)methanone (RCS-4) as well as Δ9-tetrahydrocannabinol (THC) to pigs should be helpful for better interpretation of analytical results in cases of misuse or poisoning...
February 14, 2018: Current Drug Delivery
https://www.readbyqxmd.com/read/29445868/induction-of-systemic-resistance-in-tomato-against-botrytis-cinerea-by-n-decanoyl-homoserine-lactone-via-jasmonic-acid-signaling
#18
Zhangjian Hu, Shujun Shao, Chenfei Zheng, Zenghui Sun, Junying Shi, Jingquan Yu, Zhenyu Qi, Kai Shi
N-decanoyl-homoserine lactone activates plant systemic resistance against Botrytis cinerea in tomato plants, which is largely dependent on jasmonic acid biosynthesis and signal transduction pathways. Rhizosphere bacteria secrete N-acylated-homoserine lactones (AHLs), a type of specialized quorum-sensing signal molecule, to coordinate their population density during communication with their eukaryotic hosts. AHLs behave as low molecular weight ligands that are sensed by plants and promote the host's resistance against foliar pathogens...
February 14, 2018: Planta
https://www.readbyqxmd.com/read/29444596/activation-of-the-cannabinoid-receptor-1-by-acea-suppresses-senescence-in-human-primary-chondrocytes-through-sirt1-activation
#19
Dawei Zhang, Gang Zhang, Zongyu Li, Bingsheng Li
Senescence of chondrocytes and cartilage degeneration induced by the proinflammatory cytokine interleukin-1β is associated with the pathogenesis of osteoarthritis. The cannabinoid receptor 1 has been involved in the pathological development of various diseases. Here, we evaluated whether activation of cannabinoid receptor 1 using its selective agonist arachidonyl-2-chloroethylamide had an influence on cellular senescence induced by interleukin-1βin human chondrocytes. Our findings demonstrate that agonist arachidonyl-2-chloroethylamidedecreased senescence-associated β-galactosidase activity and cell cycle arrest in the G0/G1 phase induced by interleukin-1β...
January 1, 2018: Experimental Biology and Medicine
https://www.readbyqxmd.com/read/29442178/the-use-of-cannabis-and-cannabinoids-in-treating-symptoms-of-multiple-sclerosis-a-systematic-review-of-reviews
#20
REVIEW
Suzanne Nielsen, Rada Germanos, Megan Weier, John Pollard, Louisa Degenhardt, Wayne Hall, Nicholas Buckley, Michael Farrell
PURPOSE OF REVIEW: Pharmaceutical cannabinoids such as nabiximols, nabilone and dronabinol, and plant-based cannabinoids have been investigated for their therapeutic potential in treating multiple sclerosis (MS) symptoms. This review of reviews aimed to synthesise findings from high quality systematic reviews that examined the safety and effectiveness of cannabinoids in multiple sclerosis. We examined the outcomes of disability and disability progression, pain, spasticity, bladder function, tremor/ataxia, quality of life and adverse effects...
February 13, 2018: Current Neurology and Neuroscience Reports
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