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https://www.readbyqxmd.com/read/28334603/the-cb1-receptor-as-the-cornerstone-of-exostasis
#1
REVIEW
Pier Vincenzo Piazza, Daniela Cota, Giovanni Marsicano
The type-1 cannabinoid receptor (CB1) is the main effector of the endocannabinoid system (ECS), which is involved in most brain and body functions. In this Perspective, we provide evidence indicating that CB1 receptor functions are key determinants of bodily coordinated exostatic processes. First, we will introduce the concepts of endostasis and exostasis as compensation or accumulation for immediate or future energy needs and discuss how exostasis has been necessary for the survival of species during evolution...
March 22, 2017: Neuron
https://www.readbyqxmd.com/read/28326930/effects-of-jwh015-in-cytokine-secretion-in-primary-human-keratinocytes-and-fibroblasts-and-its-suitability-for-topical-transdermal-delivery
#2
Alicia Bort, Perla A Alvarado-Vazquez, Carolina Moracho-Vilrriales, Kristopher G Virga, Giuseppe Gumina, Alfonso Romero-Sandoval, Scott Asbill
Background JWH015 is a cannabinoid (CB) receptor type 2 agonist that produces immunomodulatory effects. Since skin cells play a key role in inflammatory conditions and tissue repair, we investigated the ability of JWH015 to promote an anti-inflammatory and pro-wound healing phenotype in human primary skin cells. Methods Human primary keratinocytes and fibroblasts were stimulated with lipopolysaccharide. The mRNA expression of cannabinoid receptors was determined using RT-PCR. The effects of JWH015 (0.05, 0...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28322830/antidiabetic-antidyslipidemic-and-toxicity-profile-of-env-2-a-potent-pyrazole-derivative-against-diabetes-and-related-diseases
#3
Eduardo Hernández-Vázquez, Hugo Ocampo-Montalban, Litzia Cerón-Romero, Miguel Cruz, Jaime Gomez-Zamudio, Guadalupe Hiriart-Valencia, Rafael Villalobos-Molina, Angelica Flores-Flores, Samuel Estrada-Soto
Diabetes is a major health problem and a predisposition factor for further degenerative complications and, therefore, novel therapies are urgently needed. Currently, cannabinoid receptor 1 (CB1 receptor) antagonists have been considered as promissory entities for metabolic disorders treatment. Accordingly, the purpose of this work was the evaluation of the sub-acute antidiabetic, anti-hyperglycemic, antidyslipidemic and toxicological profile of ENV-2, a potent hypoglycemic and antioxidant CB1 receptor antagonist...
March 17, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28320859/2-arachidonoylglycerol-ameliorates-inflammatory-stress-induced-insulin-resistance-in-cardiomyocytes
#4
Dipanjan Chanda, Yvonne Oligschlaeger, Ilvy Geraets, Yilin Liu, Xiaoqing Zhu, Jieyi Li, Miranda Nabben, Will Coumans, Joost J F P Luiken, Jan F C Glatz, Dietbert Neumann
Several studies have linked impaired glucose uptake and insulin resistance (IR) to functional impairment of the heart. Recently, endocannabinoids have been implicated in cardiovascular disease. However, the mechanisms involving endocannabinoid signaling, glucose uptake and IR in cardiomyocytes are understudied. Here, we report the endocannabinoid 2-Arachidonoylglycerol (2-AG) via stimulation of cannabinoid type-1 (CB1) receptor and Ca2+/Calmodulin-dependent protein kinase β (CaMKKβ) activates AMPK leading to increased glucose uptake...
March 20, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28315398/hepatic-expressions-of-cannabinoid-receptors-cb1-and-cb2-correlate-with-the-fibrogenesis-in-patients-with-chronic-hepatitis-b
#5
Erhei Dai, Lianshan Zhang, Lihong Ye, Shiqing Wan, Lulu Feng, Qi Qi, Fang Yao, Zhen Li
AIM: The endocannabinoid system is involved in the pathogenesis of liver fibrosis. However, most of the findings come from experiment researches on animal model or clinical trial on chronic hepatitis C. The roles of cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2) in hepatofibrosis on patients with chronic hepatitis B(CHB) have not been studied universally. This study aimed to explore the relationship between liver fibrosis and expressions of CB1 and CB2 on patients with CHB...
March 14, 2017: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/28295323/crip1a-inhibits-endocytosis-of-g-protein-coupled-receptors-activated-by-endocannabinoids-and-glutamate-by-a-common-molecular-mechanism
#6
Fabrizio Mascia, Lisa Klotz, Judith Lerch, Mostafa A Ahmed, Yan Zhang, Ralf Enz
The excitability of the central nervous system depends largely on the surface density of neurotransmitter receptors. The endocannabinoid receptor CB1 R and the metabotropic glutamate receptor mGlu8 R are expressed presynaptically where they reduce glutamate release into the synaptic cleft. Recently, the CB1 R interacting protein CRIP1a was identified and characterized to regulate CB1 R activity in neurons. However, underlying molecular mechanisms are largely unknown. Here, we identified a common mechanism used by CRIP1a to regulate the cell surface density of two different types of G-protein coupled receptors, CB1 R and mGlu8a R...
March 15, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28293172/ethanol-modulates-the-spontaneous-complex-spike-waveform-of-cerebellar-purkinje-cells-recorded-in-vivo-in-mice
#7
Guang-Jian Zhang, Mao-Cheng Wu, Jin-Di Shi, Yin-Hua Xu, Chun-Ping Chu, Song-Biao Cui, De-Lai Qiu
Cerebellar Purkinje cells (PCs) are sensitive to ethanol, but the effect of ethanol on spontaneous complex spike (CS) activity in these cells in vivo is currently unknown. Here, we investigated the effect of ethanol on spontaneous CS activity in PCs in urethane-anesthetized mice using in vivo patch-clamp recordings and pharmacological manipulation. Ethanol (300 mM) induced a decrease in the CS-evoked pause in simple spike (SS) firing and in the amplitude of the afterhyperpolarization (AHP) under current clamp conditions...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28289947/in-vivo-and-in-vitro-identification-of-endocannabinoid-signaling-in-periodontal-tissues-and-their-potential-role-in-local-pathophysiology
#8
Anna Konermann, Andreas Jäger, Stefanie A E Held, P Brossart, Anne Schmöle
The endocannabinoid system (ECS) with its binding receptors CB1 and CB2 impacts multiple pathophysiologies not only limited to neuronal psychoactivity. CB1 is assigned to cerebral neuron action, whereas CB2 is mainly expressed in different non-neuronal tissues and associated with immunosuppressive effects. Based on these tissue-selective CB receptor roles, it was the aim of this study to analyze potential expression in periodontal tissues under physiological conditions and inflammatory states. In vivo, CB receptor expression was investigated on human periodontal biopsies with or without bacterial inflammation and on rat maxillae with or without sterile inflammation...
March 14, 2017: Cellular and Molecular Neurobiology
https://www.readbyqxmd.com/read/28289139/longitudinal-predictors-of-synthetic-cannabinoid-use-in-adolescents
#9
Andrew L Ninnemann, Hye Jeong Choi, Gregory L Stuart, Jeff R Temple
BACKGROUND: Synthetic cannabinoids (SCs) are a large, heterogeneous group of chemicals that are structurally similar to δ-9-tetrahydrocannabinol. Many SCs are high-efficacy full agonists of the CB1 and/or CB2 cannabinoid receptors, resulting in a potent group of chemicals with a variety of negative health effects, including death. SCs are available to adolescents at convenience stores and smoke shops and on the Internet. However, little is known about the risk factors that contribute to eventual use of SCs in adolescents, and no research has examined the psychiatric, personality, and substance-use risk factors that prospectively predict SC use...
March 13, 2017: Pediatrics
https://www.readbyqxmd.com/read/28287814/activation-and-deactivation-of-5-ht1-receptor-of-accumbens-shell-area-does-not-alter-acpa-induced-aversive-memory-deficit-in-male-rat
#10
Marzieh Keramati-Nojedehsadat, Shahrbanoo Oryan, Mohammad Reza Zarrindast, Vahab Babapour
BACKGROUND: Some studies have indicated a close relation between serotonergic and cannabinoidergic systems in several brain regions. Thus, the aim of current study is investigating the effect of 5-HT1 receptors of accumbens shell (Acb shell) on aversive memory deficit induced by ACPA (cannabinoid CB1 receptor agonist) using test-retest protocol of elevated plus-maze (EPM) in male Wistar rats. METHOD: Bilateral guide cannulae were implanted to allow microinjection of ACPA, CP94253 HCL (5-HT1 receptor agonist agonist) or GR127935 HCL (5-HT1 receptor antagonist)...
March 2017: Archives of Iranian Medicine
https://www.readbyqxmd.com/read/28284861/biological-evaluation-of-pyridone-alkaloids-on-the-endocannabinoid-system
#11
Andrea Chicca, Regina Berg, Henning J Jessen, Nicolas Marck, Fabian Schmid, Patrick Burch, Jürg Gertsch, Karl Gademann
Naturally occurring pyridone alkaloids as well as synthetic derivatives were previously shown to induce neurite outgrowth. However, the molecular basis for this biological effect remains poorly understood. In this work, we have prepared new pyridones, and tested the effect of thirteen 4-hydroxy-2-pyridone derivatives on the components of the endocannabinoid system. Investigation of binding affinities towards CB1 and CB2 receptors led to the identification of a compound binding selectively to CB1 (12). Compound 12 and a closely related derivative (11) also inhibited anandamide (AEA) hydrolysis by fatty acid amide hydrolase...
February 17, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28283967/exercise-training-and-high-fat-diet-elicit-endocannabinoid-system-modifications-in-the-rat-hypothalamus-and-hippocampus
#12
François-Xavier Gamelin, Julien Aucouturier, Fabio Arturo Iannotti, Fabiana Piscitelli, Enrico Mazzarella, Teresa Aveta, Melissa Leriche, Erwan Dupont, Caroline Cieniewski-Bernard, Erwan Leclair, Bruno Bastide, Vincenzo Di Marzo, Elsa Heyman
The purpose of the present study was to examine the effect of chronic exercise on the hypothalamus and hippocampus levels of the endocannabinoids (eCBs) anandamide (AEA) and 2-arachidonoylglycerol (2-AG) and of two AEA congeners and on the expression of genes coding for CB1, CB2 receptors (Cnr1 and Cnr2, respectively), and the enzymes responsible for eCB biosynthesis and degradation, in rats fed with a standard or high-fat diet. Male Wistar rats (n = 28) were placed on a 12-week high-fat (HFD) or standard diet period, followed by 12 weeks of exercise training for half of each group...
March 10, 2017: Journal of Physiology and Biochemistry
https://www.readbyqxmd.com/read/28265242/the-ratio-of-2-ag-to-its-isomer-1-ag-as-an-intrinsic-fine-tuning-mechanism-of-cb1-receptor-activation
#13
Klaudia Dócs, Zoltán Mészár, Sándor Gonda, Attila Kiss-Szikszai, Krisztina Holló, Miklós Antal, Zoltán Hegyi
Endocannabinoids are pleiotropic lipid messengers that play pro-homeostatic role in cellular physiology by strongly influencing intracellular Ca(2+) concentration through the activation of cannabinoid receptors. One of the best-known endocannabinoid '2-AG' is chemically unstable in aqueous solutions, thus its molecular rearrangement, resulting in the formation of 1-AG, may influence 2-AG-mediated signaling depending on the relative concentration and potency of the two isomers. To predict whether this molecular rearrangement may be relevant in physiological processes and in experiments with 2-AG, here we studied if isomerization of 2-AG has an impact on 2-AG-induced, CB1-mediated Ca(2+) signaling in vitro...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28261100/endocannabinoids-a-promising-impact-for-traumatic-brain-injury
#14
REVIEW
Lesley D Schurman, Aron H Lichtman
The endogenous cannabinoid (endocannabinoid) system regulates a diverse array of physiological processes and unsurprisingly possesses considerable potential targets for the potential treatment of numerous disease states, including two receptors (i.e., CB1 and CB2 receptors) and enzymes regulating their endogenous ligands N-arachidonoylethanolamine (anandamide) and 2-arachidonyl glycerol (2-AG). Increases in brain levels of endocannabinoids to pathogenic events suggest this system plays a role in compensatory repair mechanisms...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28254562/cb1-receptor-mediated-respiratory-depression-by-endocannabinoids
#15
András Iring, László Hricisák, Zoltán Benyó
Endocannabinoids (ECs) are bioactive lipid mediators acting on two distinct cannabinoid receptors (CB1 and CB2), which are ubiquitously expressed in many tissues including the respiratory system. Despite numerous experimental data showing that cannabinomimetics influence respiration, the role of endogenously produced ECs in respiratory control has not been verified yet. Pulse oximetry was used in the present study to directly measure changes in respiratory parameters during elevation of EC levels. The cannabinoid reuptake inhibitor AM-404 (10mgkg(-1), i...
February 22, 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/28252602/-corticosterone-induced-changes-in-the-inhibitory-neurotransmission-in-hippocampal-ca1-synapses-depending-on-the-activity-of-inhibitory-synapses-that-express-cannabinoid-receptors
#16
E P Volkova, G G Nadareishvili, A P Bolshakov
AIM: To study an effect of corticosterone (100 nM) on spontaneous inhibitory postsynaptic currents (sIPSC) in pyramidal neurons of CA1 area and a role of inhibitory CB1-expressing synapses in the development of corticosterone-induced effects. MATERIAL AND METHODS: The experiments were performed on acute slices of the rat ventral hippocampus using whole-cell configuration of the patch-clamp technique. RESULTS AND CONCLUSION: The addition of corticosterone resulted in a small, but significant, increase in the frequency of sIPSCs during the first 10 minutes and then this parameter returned to the basal level...
2017: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
https://www.readbyqxmd.com/read/28247204/changes-in-the-brain-endocannabinoid-system-in-rat-models-of-depression
#17
Irena Smaga, Joanna Jastrzębska, Magdalena Zaniewska, Beata Bystrowska, Dawid Gawliński, Agata Faron-Górecka, Żaneta Broniowska, Joanna Miszkiel, Małgorzata Filip
A growing body of evidence implicates the endocannabinoid (eCB) system in the pathophysiology of depression. The aim of this study was to investigate the influence of changes in the eCB system, such as levels of neuromodulators, eCB synthesizing and degrading enzymes, and cannabinoid (CB) receptors, in different brain structures in animal models of depression using behavioral and biochemical analyses. Both models used, i.e., bulbectomized (OBX) and Wistar Kyoto (WKY) rats, were characterized at the behavioral level by increased immobility time...
April 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28245562/dietary-%C3%AF-3-polyunsaturated-fatty-acids-inhibit-tumor-growth-in-transgenic-apc-min-mice-correlating-with-cb1-receptor-up-regulation
#18
Maria Notarnicola, Valeria Tutino, Valentina De Nunzio, Francesco Dituri, Maria Gabriella Caruso, Gianluigi Giannelli
Mediterranean diet components, such as olive oil and ω-3 polyunsaturated fatty acids (ω-3 PUFAs), can arrest cell growth and promote cell apoptosis. Recently, olive oil has been demonstrated to modulate type-1 cannabinoid (CB1) receptor gene expression in both human colon cancer cells and rat colon. The aim of this study was to investigate a possible link between olive oil and ω-3 PUFAs effects and CB1 receptor expression in both intestinal and adipose tissue of Apc(Min/+) mice. To confirm the role for the CB1 receptor as a negative modulator of cell proliferation in human colon cancer, CB1 receptor gene expression was also detected in tumor tissue and in surrounding normal mucosa of patients with colorectal cancer (CRC)...
February 24, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28245177/%C3%AE-9-tetrahydrocannabinol-decreases-willingness-to-exert-cognitive-effort-in-male-rats
#19
Mason M Silveira, Wendy K Adams, Maria Morena, Matthew N Hill, Catharine A Winstanley
BACKGROUND: Acceptance of cannabis use is growing. However, prolonged use is associated with diminished psychosocial outcomes, potentially mediated by drug-induced cognitive impairments. Δ(9)-Tetrahydrocannabinol (THC) is the main psychoactive ingredient in cannabis, yet other phytocannabinoids in the plant, such as cannabidiol (CBD), have unique properties. Given that CBD can modulate the undesirable effects of THC, therapeutic agents, such as nabiximols, contain higher CBD:THC ratios than illicit marijuana...
March 2017: Journal of Psychiatry & Neuroscience: JPN
https://www.readbyqxmd.com/read/28240187/the-endocannabinoid-system-modulating-levels-of-consciousness-emotions-and-likely-dream-contents
#20
Eric Murillo-Rodriguez, José Carlos Pastrana-Trejo, Mireille Salas-Crisóstomo, Miriel de-la-Cruz
Cannabinoids are derivatives that are either compounds occurring naturally in the plant, Cannabis sativa or synthetic analogs of these molecules. The first and most widely investigated of the cannabinoids is ∆9-tetrahydrocannabinol (Δ9-THC), which is the main psychotropic constituent of cannabis and undergoes significant binding to cannabinoid receptors. These cannabinoid receptors are seven-transmembrane receptors that received their name from the fact that they respond to cannabinoid compounds, including Δ9-THC...
February 23, 2017: CNS & Neurological Disorders Drug Targets
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