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https://www.readbyqxmd.com/read/29353373/disturbance-of-metabotropic-glutamate-receptor-mediated-long-term-depression-mglu-ltd-of-excitatory-synaptic-transmission-in-the-rat-hippocampus-after-prenatal-immune-challenge
#1
Mélanie Cavalier, Azza Ben Sedrine, Lea Thevenet, Nadine Crouzin, Janique Guiramand, Marie-Céleste de Jésus Ferreira, Catherine Cohen-Solal, Gérard Barbanel, Michel Vignes
Maternal immune challenge has proved to induce moderate to severe behavioral disabilities in the offspring. Cognitive/behavioral deficits are supported by changes in synaptic plasticity in different brain areas. We have reported previously that prenatal exposure to bacterial LPS could induce inhibition of hippocampal long-term potentiation (LTP) in the CA1 area of the juvenile/adult male offspring associated with spatial learning inabilities. Nevertheless, deficits in plasticity could be observed at earlier stages as shown by the early loss of long-term depression (LTD) in immature animals...
January 20, 2018: Neurochemical Research
https://www.readbyqxmd.com/read/29352424/cannabinoid-cb1-and-cb2%C3%A2-receptors-and-monoacylglycerol-lipase-gene-expression-alterations-in-the-basal-ganglia-of-patients-with-parkinson-s-disease
#2
Francisco Navarrete, M Salud García-Gutiérrez, Auxiliadora Aracil-Fernández, José L Lanciego, Jorge Manzanares
Previous studies suggest that the endocannabinoid system plays an important role in the neuropathological basis of Parkinson's disease (PD). This study was designed to detect potential alterations in the cannabinoid receptors CB1 (CB1r) and CB2 (A isoform, CB2Ar), and in monoacylglycerol lipase (MAGL) gene expression in the substantia nigra (SN) and putamen (PUT) of patients with PD. Immunohistochemical studies were performed to identify precise CB2r cellular localization in the SN of control and PD patients...
January 19, 2018: Neurotherapeutics: the Journal of the American Society for Experimental NeuroTherapeutics
https://www.readbyqxmd.com/read/29350472/the-chemistry-and-pharmacology-of-synthetic-cannabinoid-sdb-006-and-its-regioisomeric-fluorinated-and-methoxylated-analogues
#3
Samuel D Banister, Alexander Olson, Matthew Winchester, Jordyn Stuart, Amelia R Edington, Richard C Kevin, Mitchell Longworth, Marco Herrera, Mark Connor, Iain S McGregor, Roy R Gerona, Michael Kassiou
Synthetic cannabinoids are the largest and most structurally diverse class of new psychoactive substances, with manufacturers often using isomerism to evade detection and circumvent legal restriction. The regioisomeric methoxy- and fluorine-substituted analogues of SDB-006 (N-benzyl-1-pentyl-1H-indole-3-carboxamide) were synthesized and could not be differentiated by gas chromatography-mass spectrometry (GC-MS), but were distinguishable by liquid chromatography-quadrupole time-of-flight-MS (LC-QTOF-MS). In a fluorescence-based plate reader membrane potential assay, SDB-006 acted as a potent agonist at human cannabinoid receptors (CB1 EC50 = 19 nM)...
January 19, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29342943/the-peptide-pnpp-19-a-spider-toxin-derivative-activates-%C3%AE-opioid-receptors-and-modulates-calcium-channels
#4
Ana C N Freitas, Steve Peigneur, Flávio H P Macedo, José E Menezes-Filho, Paul Millns, Liciane F Medeiros, Maria A Arruda, Jader Cruz, Nicholas D Holliday, Jan Tytgat, Gareth Hathway, Maria E de Lima
The synthetic peptide PnPP-19 comprehends 19 amino acid residues and it represents part of the primary structure of the toxin δ-CNTX-Pn1c (PnTx2-6), isolated from the venom of the spider Phoneutria nigriventer. Behavioural tests suggest that PnPP-19 induces antinociception by activation of CB1, μ and δ opioid receptors. Since the peripheral and central antinociception induced by PnPP-19 involves opioid activation, the aim of this work was to identify whether this synthetic peptide could directly activate opioid receptors and investigate the subtype selectivity for μ-, δ- and/or κ-opioid receptors...
January 15, 2018: Toxins
https://www.readbyqxmd.com/read/29340966/cannabinomimetric-lipids-from-natural-extract-to-artificial-synthesis
#5
REVIEW
Ya-Ru Gao, Yong-Qiang Wang
Endocannabinoid system is related with various physiological and cognitive processes including fertility, pregnancy, during pre- and postnatal development, pain-sensation, mood, appetite, and memory. In the latest decades, an important milestone concerning the endocannabinoid system was the discovery of the existence of the cannabinoid receptors CB1 and CB2. Anandamide was the first reported endogenous metabolite, which adjusted the release of some neurotransmitters through binding to the CB1 or CB2 receptors...
January 16, 2018: Natural Products and Bioprospecting
https://www.readbyqxmd.com/read/29338068/single-and-combined-effects-of-plant-derived-thc-cbd-and-synthetic-win-55-212-cannabinoids-on-cognition-and-cannabinoid-associated-withdrawal-signs-in-mice
#6
Alyssa M Myers, Patrick B Siegele, Jeffrey D Foss, Ronald F Tuma, Sara Jane Ward
BACKGROUND AND PURPOSE: It has been suggested that the non-euphorogenic phytocannabinoid cannabidiol (CBD) can ameliorate adverse effects of delta-9-tetrahydrocannabinol (THC). We determined whether CBD ameliorates cognitive deficits and withdrawal signs induced by cannabinoid CB1/CB2 receptor agonists or produces these pharmacological effects on its own. EXPERIMENTAL APPROACH: The effects of THC or the CB1/CB2 receptor full agonist WIN55212 (WIN) alone, CBD alone, or their combination were tested across a range of doses...
January 16, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29336868/the-therapeutic-potential-of-targeting-the-peripheral-endocannabinoid-cb1-receptor-system
#7
REVIEW
Joseph Tam, Liad Hinden, Adi Drori, Shiran Udi, Shahar Azar, Saja Baraghithy
Endocannabinoids (eCBs) are internal lipid mediators recognized by the cannabinoid-1 and -2 receptors (CB1R and CB2R, respectively), which also mediate the different physiological effects of marijuana. The endocannabinoid system, consisting of eCBs, their receptors, and the enzymes involved in their biosynthesis and degradation, is present in a vast number of peripheral organs. In this review we describe the role of the eCB/CB1R system in modulating the metabolism in several peripheral organs. We assess how eCBs, via activating the CB1R, contribute to obesity and regulate food intake...
January 11, 2018: European Journal of Internal Medicine
https://www.readbyqxmd.com/read/29335158/arvanil-olvanil-am-1172-and-ly-2183240-various-cannabinoid-cb1-receptor-agonists-increase-the-threshold-for-maximal-electroshock-induced-seizures-in-mice
#8
Piotr Tutka, Aleksandra Wlaź, Magdalena Florek-Łuszczki, Patrycjusz Kołodziejczyk, Dorota Bartusik-Aebisher, Jarogniew J Łuszczki
BACKGROUND: Recent evidence reveals therapeutic potential for cannabinoids to reduce seizure frequency, severity and duration. Animal models are useful tools to determine the potential antiseizure or antiepileptic effects of cannabinoids. The objective of this study was evaluation of the effect of arvanil, olvanil, AM 1172 and LY 2183240, the compounds interacted with endocannabinoid and/or endovanilloid systems, on convulsions in the commonly used model of convulsions in mice. METHODS: Arvanil and olvanil were injected intraperitoneally (ip) 30 min and AM 1172 and LY 2183240 were administered ip 60 min before the maximal electroshock seizure threshold (MEST) test...
August 24, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29334787/analysis-of-endocannabinoid-receptors-and-enzymes-in-the-post-mortem-motor-cortex-and-spinal-cord-of-amyotrophic-lateral-sclerosis-patients
#9
Francisco Espejo-Porras, Javier Fernández-Ruiz, Eva de Lago
OBJECTIVE: We have investigated the endocannabinoid system in the motor cortex of motor neuron disease (MND) patients. METHODS: Post-mortem samples from MND patients and controls were used for immunostaining and/or Western blotting analysis of endocannabinoid elements. RESULTS: We did not find any evidence of neuronal losses in the motor cortex of MND patients, but elevations in glial markers Iba-1 and GFAP were evident. We found no changes in FAAH and MAGL enzymes and in the CB1 receptor, which correlated with the lack of cortical neuron death...
January 15, 2018: Amyotrophic Lateral Sclerosis and Frontotemporal Degeneration
https://www.readbyqxmd.com/read/29331500/peripheral-modulation-of-the-endocannabinoid-system-in-metabolic-disease
#10
REVIEW
Nirajan Shrestha, James S M Cuffe, Dana S Hutchinson, John P Headrick, Anthony V Perkins, Andrew J McAinch, Deanne H Hryciw
Dysfunction of the endocannabinoid system (ECS) has been identified in metabolic disease. Cannabinoid receptor 1 (CB1) is abundantly expressed in the brain but also expressed in the periphery. Cannabinoid receptor 2 (CB2) is more abundant in the periphery, including the immune cells. In obesity, global antagonism of overexpressed CB1 reduces bodyweight but leads to centrally mediated adverse psychological outcomes. Emerging research in isolated cultured cells or tissues has demonstrated that targeting the endocannabinoid system in the periphery alleviates the pathologies associated with metabolic disease...
January 10, 2018: Drug Discovery Today
https://www.readbyqxmd.com/read/29325907/corrigendum-to-cannabinoid-cb1-receptor-inverse-agonist-mj08-stimulates-glucose-production-via-hepatic-sympathetic-innervation-in-rats-european-journal-of-pharmacology-814-2017-232-239
#11
Wei Chen, Hongying Liu, Hua Guan, Nina Xue, Lili Wang
No abstract text is available yet for this article.
January 15, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29325757/the-role-of-fatty-acids-and-their-endocannabinoid-like-derivatives-in-the-molecular-regulation-of-appetite
#12
REVIEW
Renger F Witkamp
Intake, absorption and synthesis of fatty acids, including those produced by the intestinal microbiota are tightly monitored via specific receptors and, indirectly through their conversion into a variety of signalling molecules. The resulting information is integrated and translated to different physiological processes, including the regulation of appetite and satiation. Direct chemosensing of fatty acids takes place via interaction with free fatty acid (FFA) and other receptors. These are present in the oronasal cavity and along the entire gastrointestinal tract, in various other tissues, and, for some receptors also in brain...
January 8, 2018: Molecular Aspects of Medicine
https://www.readbyqxmd.com/read/29314831/a-fluorescent-probe-to-unravel-functional-features-of-cannabinoid-receptor-cb1-in-human-blood-and-tonsil-immune-system-cells
#13
Mar Martín-Fontecha, Alba Angelina, Beate Rückert, Ainoa Rueda-Zubiaurre, Leticia Martin-Cruz, Willem van de Veen, Mübeccel Akdis, Silvia Ortega-Gutierrez, María L López-Rodrí Guez, Cezmi Akdis, Oscar Palomares
The human endogenous cannabinoid system (ECS) regulates key physiological processes and alterations in its signalling pathways and endocannabinoid levels are associated to diseases such as neurological and neuropsychiatric conditions, cancer, pain and inflammation, obesity, metabolic and different immune related disorders. Immune system cells express the G-protein coupled cannabinoid receptor 1 (CB1) but its functional role has not been fully understood, likely due to the lack of appropriate tools. The availability of novel tools to investigate the role of CB1 in immune regulation might contribute to identify CB1 as a potential novel therapeutic target or biomarker for many diseases...
January 9, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29314474/multiple-binding-sites-contribute-to-the-mechanism-of-the-2-phenylindole-mixed-orthosteric-agonistic-and-pam-action-on-the-cannabinoid-cb1-receptor
#14
Noureldin Saleh, Oliver Hucke, Florian Montel, Gert Kramer, Boris Ferger, Esther Schmidt, Timothy Clark, Peter Hildebrand, Christofer Tautermann, Radoslaw Lipinski
The cannabinoid CB1 receptor (CB1R) is an abundant metabotropic G-protein coupled receptor that has been difficult to address therapeutically because of CNS side effects exerted by orthosteric ligands. Recent efforts have focused on developing allosteric modulators that target CB1R. Compounds from a recently discovered of 2-phenylindoles mixed agonist and positive allosteric modulators (Ago-PAMs), have shown promising properties for CB1R. Here, we identify binding modes of both the CP 55,940 agonist and GAT228 a 2-phenylindole allosteric modulator using a metadynamics simulation, and quantify their affinity and cooperativity...
January 3, 2018: Angewandte Chemie
https://www.readbyqxmd.com/read/29311110/long-lasting-in-vivo-effects-of-the-cannabinoid-cb1-antagonist-am6538
#15
Carol A Paronis, Girish R Chopda, Kiran Vemuri, Ani S Zakarian, Alexandros Makriyannis, Jack Bergman
AM6538 is a cannabinoid antagonist that binds CB1 receptors expressed in HEK-293 cells in a wash-resistant manner. The effects of AM6538 in live animals has not previously been established. We characterized the antagonist effects of AM6538 in male mice, using a warm-water tail-withdrawal assay, and in male squirrel monkeys trained to discriminate the CB1 agonist AM4054 from vehicle. The cannabinoid agonists WIN 55,212, Δ9-tetrahydrocannabinol (THC), and AM4054 all produced 100% maximum possible antinociceptive effects in mice following vehicle pretreatment...
January 8, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29306760/effect-of-acetaminophen-on-osteoblastic-differentiation-and-migration-of-mc3t3-e1-cells
#16
Yoshihiro Nakatsu, Fumio Nakagawa, Sen Higashi, Tomoko Ohsumi, Shunji Shiiba, Seiji Watanabe, Hiroshi Takeuchi
BACKGROUND: N-acetyl-p-aminophenol (APAP, acetaminophen, paracetamol) is a widely used analgesic/antipyretic with weak inhibitory effects on cyclooxygenase (COX) compared to non-steroidal anti-inflammatory drugs (NSAIDs). The mechanism of action of APAP is mediated by its metabolite that activates transient receptor potential channels, including transient receptor potential vanilloid 1 (TRPV1) and TRP ankyrin 1 (TRPA1) or the cannabinoid receptor type 1 (CB1). However, the exact molecular mechanism and target underlying the cellular actions of APAP remain unclear...
July 15, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29288767/surprising-outcomes-in-cannabinoid-cb1-cb2-receptor-double-knockout-mice-in-two-models-of-ischemia
#17
Sara Jane Ward, Francesca Castelli, Zachary W Reichenbach, Ronald F Tuma
AIMS: We tested the hypothesis that CB1/CB2 receptor double knockout would produce significant increases in infarct size and volume and significant worsening in clinical score, using two mouse models, one of permanent ischemia and one of ischemia/reperfusion. MAIN METHODS: Focal cerebral infarcts were created using either photo induced permanent injury or transient middle cerebral artery occlusion. Infarct volume and motor function were evaluated in cannabinoid receptor 1/cannabinoid receptor 2 double knockout mice...
December 27, 2017: Life Sciences
https://www.readbyqxmd.com/read/29288688/neuroprotective-activity-of-macamides-on-manganese-induced-mitochondrial-disruption-in-u-87-mg-glioblastoma-cells
#18
Kuljeet S Gugnani, Nguyen Vu, Alejandro N Rondón-Ortiz, Mark Böhlke, Timothy J Maher, Alejandro J Pino-Figueroa
Macamides are a distinct class of secondary metabolites, benzylamides of long chain fatty acids, which were isolated from the Peruvian plant Lepidium meyenii (Maca). As structural analogues of the endocannabinoid anandamide (AEA), they have demonstrated neuroprotective effects in vitro and in vivo. The purpose of this study was to demonstrate the neuroprotective activity of the macamides: N-(3-methoxybenzyl)oleamide (MAC 18:1), N-(3-methoxybenzyl)linoleamide (MAC 18:2) and N-(3-methoxybenzyl)linolenamide (MAC 18:3) in a neurotoxic environment caused by exposure of U-87 MG glioblastoma cells to manganese chloride (MnCl2)...
December 27, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29285308/decisive-role-of-p42-44-mitogen-activated-protein-kinase-in-%C3%AE-9-tetrahydrocannabinol-induced-migration-of-human-mesenchymal-stem-cells
#19
Ellen Lüder, Robert Ramer, Kirsten Peters, Burkhard Hinz
In past years, medical interest in Δ9-tetrahydrocannabinol (THC), the major psychoactive ingredient of the Cannabis plant, has been renewed due to the elucidation of the endocannabinoid system and diverse other receptor targets involved in biological cannabinoid effects. The present study therefore investigates the impact of THC on the migration of mesenchymal stem cells (MSCs) which are known to be involved in various regenerative processes such as bone healing. Using Boyden chamber assays, THC was found to increase the migration of adipose-derived MSCs...
December 1, 2017: Oncotarget
https://www.readbyqxmd.com/read/29284441/expression-of-cannabinoid-1-and-2-receptors-and-the-effects-of-cannabinoid-1-and-2-receptor-agonists-on-detrusor-overactivity-associated-with-bladder-outlet-obstruction-in-rats
#20
Sung Dae Kim, Kang Jun Cho, Joon Chul Kim
BACKGROUND: This study investigated changes in the expression of cannabinoid (CB) receptors and the effects of CB1 and CB2 agonists on detrusor overactivity (DO) associated with bladder outlet obstruction (BOO) in rats. METHODS: Male Sprague Dawley rats were randomly assigned to four groups (n = 10) in each group. The control group comprised sham-operated rats. A animals in the BOO, CB1 agonist and CB2 agonist groups all underwent BOO surgery. Three weeks postoperatively, cystometrography (CMG) was performed on all rats...
December 29, 2017: BMC Urology
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