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https://www.readbyqxmd.com/read/28611585/role-of-n-arachidonoyl-serotonin-aa-5-ht-in-sleep-wake-cycle-architecture-sleep-homeostasis-and-neurotransmitters-regulation
#1
Eric Murillo-Rodríguez, Vincenzo Di Marzo, Sergio Machado, Nuno B Rocha, André B Veras, Geraldo A M Neto, Henning Budde, Oscar Arias-Carrión, Gloria Arankowsky-Sandoval
The endocannabinoid system comprises several molecular entities such as endogenous ligands [anandamide (AEA) and 2-arachidonoylglycerol (2-AG)], receptors (CB1 and CB2), enzymes such as [fatty acid amide hydrolase (FAHH) and monoacylglycerol lipase (MAGL)], as well as the anandamide membrane transporter. Although the role of this complex neurobiological system in the sleep-wake cycle modulation has been studied, the contribution of the blocker of FAAH/transient receptor potential cation channel subfamily V member 1 (TRPV1), N-arachidonoyl-serotonin (AA-5-HT) in sleep has not been investigated...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28606623/the-interaction-between-alpha-7-nicotinic-acetylcholine-receptor-and-nuclear-peroxisome-proliferator-activated-receptor-%C3%AE-represents-a-new-antinociceptive-signaling-pathway-in-mice
#2
Giulia Donvito, Deniz Bagdas, Wisam Toma, Elnaz Rahimpour, Asti Jackson, Julie A Meade, Shakir AlSharari, Abhijit R Kulkarni, F Ivy Carroll, Aron H Lichtman, Roger L Papke, Ganesh A Thakur, M Imad Damaj
Recently, α7 nicotinic acetylcholine receptors (nAChRs), primarily activated by binding of orthosteric agonists, represent a target for anti-inflammatory and analgesic drug development. These receptors may also be modulated by positive allosteric modulators (PAMs), ago-allosteric ligands (ago-PAMs), and α7-silent agonists. Activation of α7 nAChRs has been reported to increase the brain levels of endogenous ligands for nuclear peroxisome proliferator-activated receptors type-α (PPAR-α), palmitoylethanolamide (PEA) and oleoylethanolamide (OEA), in a Ca(2+)-dependent manner...
June 9, 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28601556/cannabidiol-upregulates-melanogenesis-through-cb1-dependent-pathway-by-activating-p38-mapk-and-p42-44-mapk
#3
Young Sun Hwang, Youn-Jung Kim, Mi Ok Kim, Mingyeong Kang, Sae Woong Oh, Youn Hwa Nho, See-Hyoung Park, Jongsung Lee
Melanogenesis plays a critical role in the protection of skin against external stresses such as ultraviolet irradiation and oxidative stressors. This study was aimed to investigate the effects of cannabidiol on melanogenesis and its mechanisms of action in human epidermal melanocytes. We found that cannabidiol increased both melanin content and tyrosinase activity. The mRNA levels of microphthalmia-associated transcription factor (MITF), tyrosinase, tyrosinase-related protein (TRP) 1, and TRP2 were increased following cannabidiol treatment...
June 7, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28597570/pharmaco-toxicological-effects-of-the-novel-third-generation-fluorinate-synthetic-cannabinoids-5f-adbinaca-ab-fubinaca-and-sts-135-in-mice-in-vitro-and-in-vivo-studies
#4
Isabella Canazza, Andrea Ossato, Fabrizio Vincenzi, Adolfo Gregori, Fabiana Di Rosa, Federica Nigro, Alessandro Rimessi, Paolo Pinton, Katia Varani, Pier Andrea Borea, Matteo Marti
INTRODUCTION: 5F-ADBINACA, AB-FUBINACA, and STS-135 are 3 novel third-generation fluorinate synthetic cannabinoids that are illegally marketed as incense, herbal preparations, or research chemicals for their psychoactive cannabis-like effects. METHODS: The present study aims at investigating the in vitro and in vivo pharmacological activity of 5F-ADBINACA, AB-FUBINACA, and STS-135 in male CD-1 mice, comparing their in vivo effects with those caused by the administration of Δ(9) -THC and JWH-018...
June 9, 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28592614/the-cannabinoid-cb2-agonist-gw405833-suppresses-inflammatory-and-neuropathic-pain-through-a-cb1-mechanism-that-is-independent-of-cb2-receptors-in-mice
#5
Ai-Ling Li, Lawrence M Carey, Ken Mackie, Andrea G Hohmann
GW405833, widely accepted as a cannabinoid CB2 agonist, suppresses pathological pain in preclinical models without unwanted central side effects of CB1 agonists. However, recent in vitro studies suggest that GW405833 may also behave as a non-competitive CB1 antagonist, suggesting that its pharmacology is more complex than initially appreciated. Here, we further investigated the pharmacological specificity of in vivo antinociceptive actions of GW405833 in models of neuropathic (i.e. partial sciatic nerve ligation (PSNL) model) and inflammatory (i...
June 7, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28589628/chemical-tools-to-modulate-2-ag-biosynthesis
#6
Hui Deng, Mario van der Stelt
2-Arachidonoylglycerol (2-AG) as an important endogenous signaling lipid that activates the cannabinoid receptors (CB1 R and CB2 R), thereby regulating a diverse range of physiological processes including anxiety, appetite, inflammation, memory, pain sensation and nociception. Diacylglycerol lipases (DAGLs) are the principle enzymes responsible for 2-AG biosynthesis. Recently, the (patho)physiological functions of DAGLs have been explored by both genetic methods and chemical tools. This review will focus on the recent efforts to develop highly selective and in vivo active DAGLs inhibitors using activity-based protein profiling...
June 6, 2017: Biotechnology and Applied Biochemistry
https://www.readbyqxmd.com/read/28583800/analysis-of-natural-product-regulation-of-cannabinoid-receptors-in-the-treatment-of-human-disease
#7
REVIEW
S Badal, K N Smith, R Rajnarayanan
The organized tightly regulated signaling relays engaged by the cannabinoid receptors (CBs) and their ligands, G proteins and other effectors, together constitute the endocannabinoid system (ECS). This system governs many biological functions including cell proliferation, regulation of ion transport and neuronal messaging. This review will firstly examine the physiology of the ECS, briefly discussing some anomalies in the relay of the ECS signaling as these are consequently linked to maladies of global concern including neurological disorders, cardiovascular disease and cancer...
June 2, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28574245/synthesis-and-pharmacological-profiling-of-the-metabolites-of-synthetic-cannabinoid-drugs-apica-sts-135-adb-pinaca-and-5f-adb-pinaca
#8
Mitchell Longworth, Mark Connor, Samuel D Banister, Michael Kassiou
Synthetic cannabinoids (SCs) containing a 1-pentyl-1-H substituted indole or indazole have found abuse around the world and are associated with an array of serious side effects. These compounds are known to undergo extensive Phase 1 metabolism after ingestion with little understanding whether these metabolites are contributing to the cannabimimetic activity of the drugs. This work presents the synthesis and pharmacological characterization of the major metabolites of two high concern SCs; APICA and ADB-PINACA...
June 2, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28570479/sensitization-of-c-fiber-nociceptors-in-mice-with-sickle-cell-disease-is-decreased-by-local-inhibition-of-anandamide-hydrolysis
#9
Megan L Uhelski, Kalpna Gupta, Donald A Simone
Chronic pain and hyperalgesia, as well as pain resulting from episodes of vasoocclusion, are characteristic features of sickle cell disease (SCD) and are difficult to treat. Since there is growing evidence that increasing local levels of endocannabinoids can decrease hyperalgesia, we examined the effects of URB597, a fatty acid amide hydrolase (FAAH) inhibitor which blocks the hydrolysis of the endogenous cannabinoid anandamide (AEA), on hyperalgesia and sensitization of cutaneous nociceptors in a humanized mouse model of SCD...
May 31, 2017: Pain
https://www.readbyqxmd.com/read/28561272/cannabinoid-cb1-cb2-receptor-agonists-attenuate-hyperactivity-and-body-weight-loss-in-a-rat-model-of-activity-based-anorexia
#10
Maria Scherma, Valentina Satta, Roberto Collu, Maria Francesca Boi, Paolo Usai, Walter Fratta, Paola Fadda
BACKGROUND AND PURPOSE: Anorexia nervosa (AN) is a serious psychiatric condition characterized by excessive body weight loss and disturbed perceptions of body shape and size, often associated with excessive physical activity. There is currently no effective drug-related therapy of this disease and this leads to high relapse rate. Clinical data suggest that a promising therapy to treat and reduce reoccurrence of AN may be based on the use of drugs that target the endocannabinoid (EC) system, which appears dysregulated in AN patients...
May 31, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28554529/maternal-alcohol-exposure-during-mid-pregnancy-dilates-fetal-cerebral-arteries-via-endocannabinoid-receptors
#11
Olga Seleverstov, Ana Tobiasz, J Scott Jackson, Ryan Sullivan, Dejian Ma, J Pierce Sullivan, Steven Davison, Yada Akkhawattanangkul, Danielle L Tate, Terry Costello, Stacey Barnett, Wei Li, Giancarlo Mari, Alex M Dopico, Anna N Bukiya
Prenatal alcohol exposure often results in fetal alcohol syndrome and fetal alcohol spectrum disorders. Mechanisms of fetal brain damage by alcohol remain unclear. We used baboons (Papio spp.) to study alcohol-driven changes in the fetal cerebral artery endocannabinoid system. Pregnant baboons were subjected to binge alcohol exposure via gastric infusion three times during a period equivalent to the second trimester of human pregnancy. A control group was infused with orange-flavored drink that was isocaloric to the alcohol-containing solution...
June 2017: Alcohol
https://www.readbyqxmd.com/read/28549792/endocannabinoids-modulate-apoptosis-in-endometriosis-and-adenomyosis
#12
Elif Bilgic, Elif Guzel Meydanli, Sevil Kose, Makbule Cisel Aydin, Eda Karaismailoglu, Irem Akar, Alp Usubutun, Petek Korkusuz
Adenomyosis that is a form of endometriosis is the growth of ectopic endometrial tissue within the muscular wall of the uterus (myometrium), which may cause dysmenorrhea and infertility. Endocannabinoid mediated apoptotic mechanisms of endometriosis and adenomyosis are not known. We hypothesized that the down regulation of endocannabinoid receptors and/or alteration in their regulatory enzymes may have a direct role in the pathogenesis of endometriosis and adenomyosis through apoptosis. Endocannabinoid receptors CB1 and CB2, their synthesizing and catabolizing enzymes (FAAH, NAPE-PLD, DAGL, MAGL) and the apoptotic indexes were immunohistochemically assessed in endometriotic and adenomyotic tissues...
May 23, 2017: Acta Histochemica
https://www.readbyqxmd.com/read/28540200/targeting-cannabinoid-signaling-for-peritoneal-dialysis-induced-oxidative-stress-and-fibrosis
#13
REVIEW
Chih-Yu Yang, Yat-Pang Chau, Ann Chen, Oscar Kuang-Sheng Lee, Der-Cherng Tarng, An-Hang Yang
Long-term exposure to bioincompatible peritoneal dialysis (PD) solutions frequently results in peritoneal fibrosis and ultrafiltration failure, which limits the life-long use of and leads to the cessation of PD therapy. Therefore, it is important to elucidate the pathogenesis of peritoneal fibrosis in order to design therapeutic strategies to prevent its occurrence. Peritoneal fibrosis is associated with a chronic inflammatory status as well as an elevated oxidative stress (OS) status. Beyond uremia per se, OS also results from chronic exposure to high glucose load, glucose degradation products, advanced glycation end products, and hypertonic stress...
May 6, 2017: World Journal of Nephrology
https://www.readbyqxmd.com/read/28526263/n-stearoyl-l-tyrosine-inhibits-the-cell-senescence-and-apoptosis-induced-by-h2o2-in-hek293-tau-cells-via-the-cb2-receptor
#14
Yue Hu, Kai-Yi Zhou, Ze-Jian Wang, Yang Lu, Ming Yin
Although considerable energy and money have been spent trying to inhibit Aβ production and its related metabolic enzyme activities, there are still no drug treatments available to cure even slow for Alzheimer's disease. Therefore, tau protein has been focused recently as the new target for the treatment of Alzheimer's disease. The transfected human embryonic kidney 293 (HEK 293) cells with or without Tau 411 plasmid were used to evaluate the effect of tau protein on cell viability. H2O2 was added to simulate microenvironment of oxidative stress (OS) during aging...
June 25, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28523112/development-of-highly-affine-and-selective-fluorinated-cannabinoid-type-2-receptor-ligands
#15
Rareş-Petru Moldovan, Kristin Hausmann, Winnie Deuther-Conrad, Peter Brust
Cannabinoid type 2 receptors (CB2 receptors) are involved in various pathological processes, and the visualization of their in vivo availability with positron emission tomography (PET) is of high interest. The study focuses on the introduction of fluorine into the structure of the highly affine and selective CB2 receptor ligand N-(adamantan-1-yl)-5-ethyl-2-methyl-1-phenyl-1H-imidazole-4-carboxamide (5). A novel series of compounds was developed by modifying (i) the adamantane-3-position, (ii) the imidazole-N-phenyl ring, and (iii) the imidazole-2-position, and the impact on the CB2 binding affinity and selectivity toward cannabinoid type 1 receptors (CB1) was evaluated...
May 11, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28497982/neuroprotection-in-oxidative-stress-related-neurodegenerative-diseases-role-of-endocannabinoid-system-modulation
#16
Janos Paloczi, Zoltan V Varga, George Hasko, Pal Pacher
SIGNIFICANCE: Redox imbalance may lead to overproduction of reactive oxygen and nitrogen species (ROS/RNS) and subsequent oxidative tissue damage which is a critical event in the course of neurodegenerative diseases. It is still not fully elucidated, however, whether oxidative stress is the primary trigger or a consequence in process of neurodegeneration. Recent Advances: Increasing evidence suggests that oxidative stress is involved in the propagation of neuronal injury and consequent inflammatory response, which in concert promote development of pathological alterations characteristic of most common neurodegenerative diseases...
May 12, 2017: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/28467971/anti-proliferative-pro-apoptotic-and-anti-invasive-effect-of-ec-ev-system-in-human-osteosarcoma
#17
Francesca Punzo, Chiara Tortora, Daniela Di Pinto, Iolanda Manzo, Giulia Bellini, Fiorina Casale, Francesca Rossi
Osteosarcoma is the most common and aggressive bone tumor in children. The Endocannabinoid/Endovanilloid system has been proposed as anticancer target in tumor of different origins. This system is composed of two receptors (CB1 and CB2), the Transient Potential Vanilloid 1 (TRPV1) channel and their ligands and enzymes. CB1 is expressed mainly in central nervous system while CB2 predominantly on immune and peripheral cells. We investigated the effects of JWH-133 (CB2 agonist) and RTX (TRPV1 agonist) in six human Osteosarcoma cell lines: MG-63, U-2OS, MNNG/HOS, Saos-2, KHOS/NP, Hs888Lu, by Apoptosis and Migration-Assay...
April 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/28460003/evidence-for-cb2-receptor-involvement-in-lps-induced-reduction-of-camp-intracellular-levels-in-uterine-explants-from-pregnant-mice-pathophysiological-implications
#18
Ana Inés Salazar, Alejandro Carozzo, Fernando Correa, Carlos Davio, Ana María Franchi
STUDY QUESTION: What is the role of the endocannabinoid system (eCS) on the lipopolysaccharide (LPS) effects on uterine explants from 7-day pregnant mice in a murine model of endotoxin-induced miscarriage? SUMMARY ANSWER: We found evidence for cannabinoid receptor type2 (CB2) involvement in LPS-induced increased prostaglandin-F2α (PGF2α) synthesis and diminished cyclic adenosine monophosphate (cAMP) intracellular content in uterine explants from early pregnant mice...
April 28, 2017: Molecular Human Reproduction
https://www.readbyqxmd.com/read/28448548/altered-striatal-endocannabinoid-signaling-in-a-transgenic-mouse-model-of-spinocerebellar-ataxia-type-3
#19
Carmen Rodríguez-Cueto, Mariluz Hernández-Gálvez, Cecilia J Hillard, Patricia Maciel, Sara Valdeolivas, José A Ramos, María Gómez-Ruiz, Javier Fernández-Ruiz
Spinocerebellar ataxia type-3 (SCA-3) is the most prevalent autosomal dominant inherited ataxia. We recently found that the endocannabinoid system is altered in the post-mortem cerebellum of SCA-3 patients, and similar results were also found in the cerebellar and brainstem nuclei of a SCA-3 transgenic mouse model. Given that the neuropathology of SCA-3 is not restricted to these two brain regions but rather, it is also evident in other structures (e.g., the basal ganglia), we studied the possible changes to endocannabinoid signaling in the striatum of these transgenic mice...
2017: PloS One
https://www.readbyqxmd.com/read/28446875/cannabinoid-modulation-of-memory-consolidation-in-rats-beyond-the-role-of-cannabinoid-receptor-subtype-1
#20
Patrizia Ratano, Maura Palmery, Viviana Trezza, Patrizia Campolongo
The effects induced by exogenous manipulation of endocannabinoid neurotransmission on emotion and memory are often contradictory. Among the different factors involved, of particular interest is the binding affinity of endocannabinoids, and their analogs, for other receptor families beyond cannabinoid receptors, such as the peroxisome proliferator-activated receptors (PPARs), and the transient receptor potential cation channel subfamily V member 1 (TRPV1). The aim of this study was to investigate which receptor subtype mediates cannabinoid effects on memory consolidation for emotionally arousing experiences...
2017: Frontiers in Pharmacology
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