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https://www.readbyqxmd.com/read/29669714/cannabidiol-inhibits-endocannabinoid-signaling-in-autaptic-hippocampal-neurons
#1
Alex Straiker, Michaela Dvorakova, Anaelle Zimmowitch, Ken P Mackie
Δ9-THC and cannabidiol (CBD) are two main cannabinoid constituents of marijuana and hashish. The pharmacology of Δ9-THC has been extensively studied, while our understanding of the pharmacology of CBD has remained limited, despite excitement in CBD's potential role in treating certain pediatric epilepsies and its reputation for attenuating some Δ9-THC-induced effects. It was established early on that CBD binds poorly to the orthosteric site of CB1 or CB2 cannabinoid receptors and its actions were commonly attributed to other non-cannabinoid receptor mechanisms...
April 18, 2018: Molecular Pharmacology
https://www.readbyqxmd.com/read/29662438/cannabinoid-receptor-type-1-expression-in-the-developing-avian-retina-morphological-and-functional-correlation-with-the-dopaminergic-system
#2
Luzia da Silva Sampaio, Regina C C Kubrusly, Yolanda P Colli, Priscila P Trindade, Victor T Ribeiro-Resende, Marcelo Einicker-Lamas, Roberto Paes-de-Carvalho, Patricia F Gardino, Fernando G de Mello, Ricardo A De Melo Reis
The avian retina has been used as a model to study signaling by different neuro- and gliotransmitters. It is unclear how dopaminergic and cannabinoid systems are related in the retina. Here we studied the expression of type 1 and 2 cannabinoid receptors (CB1 and CB2 ), as well as monoacylglycerol lipase (MAGL), the enzyme that degrades 2-arachidonoylglycerol (2-AG), during retina development. Our data show that CB1 receptor is highly expressed from embryonic day 5 (E5) until post hatched day 7 (PE7), decreasing its levels throughout development...
2018: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29624642/cannabidiol-regulates-behavioural-alterations-and-gene-expression-changes-induced-by-spontaneous-cannabinoid-withdrawal
#3
Francisco Navarrete, Auxiliadora Aracil-Fernández, Jorge Manzanares
BACKGROUND AND PURPOSE: Cannabidiol (CBD) represents a promising therapeutic tool for treating cannabis use disorder (CUD). This study aimed to evaluate the effects of CBD on the behavioural and gene expression alterations induced by spontaneous cannabinoid withdrawal. EXPERIMENTAL APPROACH: Spontaneous cannabinoid withdrawal was evaluated 12 h after cessation of CP-55,940 treatment (0.5 mg·kg-1 /12 h; intraperitoneally (i.p.); 7 days) in C57BL/6J mice. The effects of CBD (5, 10 and 20 mg·kg-1 ; i...
April 6, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29618679/low-risk-of-pulmonary-vein-stenosis-after-contemporary-atrial-fibrillation-ablation-lessons-from-repeat-procedures-after-radiofrequency-current-cryoballoon-and-laser-balloon
#4
Takahiko Nagase, Stefano Bordignon, Laura Perrotta, Fabrizio Bologna, Felix K Weise, Athanasios Konstantinou, Ritsushi Kato, Boris Schmidt, Julian K R Chun
BACKGROUND: The incidence of pulmonary vein stenosis (PVS) after AF ablation following contemporary procedures remains unclear. We compared the incidence of PVS/narrowing (PVS/N) after PV isolation (PVI) for (1) 3-D mapping-guided wide-area encircling irrigated radiofrequency current (RFC) ablation; (2) first-third-generation big cryoballoon (CB1-3) ablation; and (3) laser balloon (LB) ablation.Methods and Results:All patients undergoing a second procedure between January 2012 and November 2016 were subgrouped according to index ablation (PVI): RFC; CB; or LB...
April 5, 2018: Circulation Journal: Official Journal of the Japanese Circulation Society
https://www.readbyqxmd.com/read/29601300/cannabinoids-in-health-and-disease-pharmacological-potential-in-metabolic-syndrome-and-neuroinflammation
#5
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/29574689/targeting-glial-cb-2-receptors-to-delay-the-progression-of-the-pathological-phenotype-in-tdp-43-a315t-transgenic-mice-a-model-of-amyotrophic-lateral-sclerosis
#6
Francisco Espejo-Porras, Laura García-Toscano, Carmen Rodríguez-Cueto, Irene Santos-García, Eva de Lago, Javier Fernández-Ruiz
BACKGROUND AND PURPOSE: CB2 receptors up-regulate in reactive microglia in the spinal cord of TDP-43(A315T) transgenic mice, an experimental model of ALS. To determine whether such up-regulation may be pharmacologically exploited, we investigated different treatments modulating the CB2 receptor function. EXPERIMENTAL APPROACH: We treated TDP-43(A315T) transgenic mice with the non-selective agonist WIN55,212-2, alone or combined with selective CB1 or CB2 antagonists, as well as with the selective CB2 agonist HU-308, and evaluated their effects on the pathological phenotype...
March 25, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29556136/secondary-metabolites-isolated-from-pinus-roxburghii-and-interpretation-of-their-cannabinoid-and-opioid-binding-properties-by-virtual-screening-and-in-vitro-studies
#7
Rola M Labib, Radhakrishnan Srivedavyasasri, Fadia S Youssef, Samir A Ross
Pinus roxburghii is highly popular as a potent analgesic and anti-inflammatory agent; however its exact mechanism of action was not fully elucidated. We aimed to interpret the analgesic and anti-inflammatory activity of the total ethanol extract of Pinus roxburghii bark (PRE) and its isolated compounds by both in silico molecular modelling and in-vitro cannabinoid and opioid binding activities evaluation for the first time. Comprehensive phytochemical investigation of PRE resulted in the isolation of sixteen compounds that were fully elucidated using1 H NMR and13 C NMR...
March 2018: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/29552078/isolation-and-biological-evaluation-of-prenylated-flavonoids-from-maclura-pomifera
#8
Yerkebulan Orazbekov, Mohamed A Ibrahim, Serjan Mombekov, Radhakrishnan Srivedavyasasri, Ubaidilla Datkhayev, Bauyrzhan Makhatov, Narayan D Chaurasiya, Babu L Tekwani, Samir A Ross
Phytochemical analysis of the ethanolic extract of Maclura pomifera fruits yielded four new compounds ( I - IV ) along with eleven known compounds ( V - XV ). The crude extract exhibited significant activity towards cannabinoid receptors (CB1: 103.4% displacement; CB2: 68.8% displacement) and possibly allosteric interaction with δ and μ opioid receptors (-49.7 and -53.8% displacement, resp.). Compound I was found to be possibly allosteric for κ and μ opioid receptors (-88.4 and -27.2% displacement, resp...
2018: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/29551733/impacts-of-cannabinoid-receptor-ligands-on-nicotine-and-chronic-mild-stress-induced-cognitive-and-depression-like-effects-in-mice
#9
Karolina Pekala, Agnieszka Michalak, Marta Kruk-Slomka, Barbara Budzynska, Grazyna Biala
Taking into account the rather frequent concomitance of nicotine abuse and stress, we aimed to research memory- and depression-related effects of nicotine administration in combination with chronic mild unpredictable stress (CMUS) in mice and an involvement of the endocannabinoid system through CB1 and CB2 receptors. Mice were submitted to the CMUS for 4 weeks. Effects on depression-like behaviors and cognition, exerted by a combined administration of CB1, i.e., Oleamide (2.5, 5.0 mg/kg), AM 251 (0.1, 0.25 mg/kg) and CB2, i...
March 15, 2018: Behavioural Brain Research
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
#10
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/29547827/pharmacological-characterization-of-the-cannabinoid-receptor-2-agonist-%C3%AE-caryophyllene-on-seizure-models-in-mice
#11
Jana Tchekalarova, Keylla da Conceição Machado, Antonio Luiz Gomes Júnior, Ana Amélia de Carvalho Melo Cavalcante, Albena Momchilova, Rumyana Tzoneva
PURPOSE: Activation of CB1 receptors, produces anticonvulsant effect accompanied by memory disturbance both in animal seizure tests and in patients with epilepsy. Few reports considered the role of CB2 receptor on seizure susceptibility and cognitive functions. The aim of the present study was to explore the effect of a selective CB2 receptor agonist β-caryophyllene (BCP) in models of seizures and cognition in mice. METHODS: Dose-dependent effects of BCP was studied in maximal electroshock seizure (MES) test, subcutaneous pentylenetetrazole (scPTZ) test and Morris water maze test...
March 12, 2018: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/29546501/cannabinoid-receptors-mental-pain-and-suicidal-behavior-a-systematic-review
#12
REVIEW
Laura Colino, Javier Herranz-Herrer, Elena Gil-Benito, Teresa Ponte-Lopez, Pablo Del Sol-Calderon, Maria Rodrigo-Yanguas, María Gil-Ligero, Antonio J Sánchez-López, Jose de Leon, Hilario Blasco-Fontecilla
PURPOSE OF REVIEW: The current serotonin-based biological model of suicidal behavior (SB) may be too simplistic. There is emerging evidence that other biomarkers and biological systems may be involved in SB pathophysiology. The literature on the endocannabinoid (EC) systems and SB is limited. The objective of the present article is to review all available information on the relationship between cannabinoid receptors (CB1 and CB2 receptors), and SB and/or psychological pain. RECENT FINDINGS: Our review is limited by the small number and heterogeneity of studies identified: (1) an autopsy study describing elevated levels of CB1 receptor activity in the prefrontal cortex and suicide in both depression and alcoholism and (2) studies supporting the involvement of both CB1 and CB2 receptors in the regulation of neuropathic pain and stress-induced analgesia...
March 15, 2018: Current Psychiatry Reports
https://www.readbyqxmd.com/read/29540562/monoacylglycerol-lipase-inhibitors-reverse-paclitaxel-induced-nociceptive-behavior-and-proinflammatory-markers-in-a-mouse-model-of-chemotherapy-induced-neuropathy
#13
Zachary Curry, Jenny Wilkerson, Deniz Bagdas, Sarah Kyte, Nipa Patel, Giulia Donvito, Mohammed A Mustafa, Justin Poklis, Micah Niphakis, Ku-Lung Hsu, Benjamin F Cravatt, David A Gewirtz, M Imad Damaj, Aron H Lichtman
Although paclitaxel effectively treats various cancers, its debilitating peripheral neuropathic pain side effects often persist long after treatment has ended. Therefore, a compelling need exists for the identification of novel pharmacologic strategies to mitigate this condition. As inhibitors of monoacylglycerol lipase (MAGL), the primary hydrolytic enzyme of the endogenous cannabinoid 2-arachidonyolglycerol, produce antinociceptive effects in numerous rodent models of pain, we investigated whether inhibitors of this enzyme (i...
March 14, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29528965/evaluation-of-different-drug-classes-on-transient-sciatic-nerve-injury-depressed-marble-burying-in-mice
#14
Jenny L Wilkerson, Zachary A Curry, Pamela D Kinlow, Brittany L Mason, Ku-Lung Hsu, Mario van der Stelt, Benjamin F Cravatt, Aron H Lichtman
A great need exists for the identification of new effective analgesics to treat sustained pain. However, most preclinical nociceptive assays measure behavioral responses evoked by noxious stimuli (i.e., pain-stimulated behavior), which presents a challenge to distinguish between motor impairing and antinociceptive effects of drugs. Here, we demonstrate that chronic constriction injury of the sciatic nerve (CCI) elicits common pain-stimulated responses (i.e., mechanical allodynia and thermal hyperalgesia) as well as reduces marble burying/digging behaviors that occur during the early stages of the neuropathy and resolve within one week...
March 8, 2018: Pain
https://www.readbyqxmd.com/read/29510186/the-anxiolytic-effects-of-cannabidiol-in-chronically-stressed-mice-are-mediated-by-the-endocannabinoid-system-role-of-neurogenesis-and-dendritic-remodeling
#15
Manoela V Fogaça, Alline C de Campos, Ludmila D Coelho, Ronald S Duman, Francisco S Guimarães
Repeated injections of cannabidiol (CBD), the major non-psychotomimetic compound present in the Cannabis sativa plant, attenuate the anxiogenic effects induced by Chronic Unpredictable Stress (CUS). The specific mechanisms remain to be fully understood but seem to involve adult hippocampal neurogenesis and recruitment of endocannabinoids. Here we investigated for the first time if the behavioral and pro-neurogenic effects of CBD administered concomitant the CUS procedure (14 days) are mediated by CB1 , CB2 or 5HT1A receptors, as well as CBD effects on dendritic remodeling and on intracellular/synaptic signaling (fatty acid amide hydrolase - FAAH, Akt, GSK3β and the synaptic proteins Synapsin Ia/b, mGluR1 and PSD95)...
March 3, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29484980/innovative-therapeutic-potential-of-cannabinoid-receptors-as-targets-in-alzheimer-s-disease-and-less-well-known-diseases
#16
Juan A Paez, Nuria E Campillo
The discovery of cannabinoid receptors at the beginning of the 1990s, CB1 being cloned in 1990 and CB2 cloned in 1993, and the availability of selective and potent cannabimimetics could only be justified by the existence of endogenous ligands that are capable of binding to them. Thus, the characterisation and cloning of the first cannabinoid receptor (CB1) led to the isolation and characterisation of the first endocannabinoid, arachidonoylethanolamide (AEA), two years later and the subsequent identification of a family of lipid transmitters known as the fatty acid ester 2-arachidonoylglycerol (2-AG)...
February 25, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29482740/cannabinoids-and-cancer-pain-a-new-hope-or-a-false-dawn
#17
REVIEW
Matthew R D Brown, W Paul Farquhar-Smith
The endocannabinoid system is involved in many areas of physiological function and homeostasis. Cannabinoid receptors are expressed in the peripheral and central nervous system and on immune cells, all areas ideally suited to modulation of pain processing. There are a wealth of preclinical data in a number of acute, chronic, neuropathic and cancer pain models that have demonstrated a potent analgesic potential for cannabinoids, especially in patients with cancer. However, although there are some positive results in pain of cancer patients, the clinical evidence for cannabinoids as analgesics has not been convincing and their use can only be weakly recommended...
March 2018: European Journal of Internal Medicine
https://www.readbyqxmd.com/read/29461930/the-role-of-cannabinoid-receptor-1-in-the-immunopathology-of-respiratory-syncytial-virus
#18
Alireza Tahamtan, Masoumeh Tavakoli-Yaraki, Azadeh Shadab, Farhad Rezaei, Sayed Mahdi Marashi, Fazel Shokri, Talat Mokhatri-Azad, Vahid Salimi
Endocannabinoid system plays an important role in pathophysiologic processes such as immune functions and impacts on disease severity. Our previous study showed that cannabinoid receptor 2 (CB2) affects clinical course of respiratory syncytial virus (RSV) infection. In this study, we investigated the role of cannabinoid receptor 1 (CB1) in RSV immunopathology and its therapeutic potential in mice model. To study the role of CB1 receptors in the immunopathology of RSV, CB1 was blocked daily with AM281 as a selective antagonist in Balb/c mice and were infected by intranasal inoculation of RSV-A2 24 h following the first dose of antagonist administration...
February 20, 2018: Viral Immunology
https://www.readbyqxmd.com/read/29441900/role-of-the-endocannabinoid-system-in-the-formation-and-development-of-depression
#19
Dan Zhou, Yue Li, Tian Tian, Wei Quan, Lei Wang, Qing Shao, Lian-Qiang Fu, Xiao-Hong Zhang, Xiao-Ye Wang, Hui Zhang, Yan-Min Ma
Two types of cannabinoid (CB) receptors have been described in the human body: CB1 and CB2 receptors. CB1 receptor distribution may be related to the cannabinoid functions of memory and cognition regulation as well as motor control. In addition, the endocannabinoid system (ECS) related to CB1 receptors may be involved in human emotion regulation, especially depression occurrence. Indeed, CB1 receptors are all distributed in depression associated neuroanatomical structures and neural circuits. Both animal experiments and clinical studies have demonstrated that impairment of the ECS pathway is present in depression models and patients, and application of both CB1 receptor agonists and anandamide (cannabinoid-like substance) degradation inhibitors produce similar biochemical and behavioral effects as antidepressants...
August 1, 2017: Die Pharmazie
https://www.readbyqxmd.com/read/29425797/antinociceptive-effects-of-the-endogenous-cannabinoid-peptide-agonist-vd-hemopressin-%C3%AE-in-mice
#20
Pei Wang, Ting Zheng, Mengna Zhang, Biao Xu, Run Zhang, Ting Zhang, Weidong Zhao, Xuerui Shi, Qinqin Zhang, Quan Fang
Cannabinoids (CBs) play important roles in pain modulation. Recently, VD-hemopressin(β) [VD-Hpβ], a 12-residue β-hemoglobin-derived peptide, was reported to activate both CB1 and CB2 receptors in vitro. To further characterize in vivo actions of VD-Hpβ, its antinociceptive activity and site(s) were evaluated in the mouse tail-flick test, and supraspinal antinociception of VD-Hpβ was further assessed in the writhing test. Our results demonstrated that supraspinal, intrathecal, subcutaneous and intraperitoneal administrations of VD-Hpβ produced analgesia in the tail-flick test...
February 6, 2018: Brain Research Bulletin
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