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https://www.readbyqxmd.com/read/28805944/suppression-of-acute-and-anticipatory-nausea-by-peripherally-restricted-faah-inhibitor-in-animal-models-role-of-ppar%C3%AE-and-cb1-receptors
#1
Erin M Rock, Guillermo Moreno-Sanz, Cheryl L Limebeer, Gavin N Petrie, Roberto Angelini, Daniele Piomelli, Linda A Parker
To evaluate the ability of the peripherally restricted fatty acid amide hydrolase (FAAH) inhibitor, URB937 (cyclohexylcarbamic acid 3'-carbamoyl-6-hydroxybiphenyl-3-yl ester) to suppress acute and anticipatory nausea in rats, and to examine the pharmacological mechanism of such an effect. EXPERIMENTAL APPROACH: We investigated the potential of URB937 to reduce the establishment of lithium chloride (LiCl)-induced conditioned gaping (a model of acute nausea) and to reduce the expression of contextually elicited conditioned gaping (a model of anticipatory nausea) in rats...
August 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28799775/a-review-of-the-therapeutic-antitumor-potential-of-cannabinoids
#2
Višnja Bogdanović, Jasminka Mrdjanović, Ivana Borišev
OBJECTIVES: The aim of this review is to discuss cannabinoids from a preclinical and clinical oncological perspective and provide the audience with a concise, retrospective overview of the most significant findings concerning the potential use of cannabinoids in cancer treatment. METHODS: A literature survey of medical and scientific databases was conducted with a focus on the biological and medical potential of cannabinoids in cancer treatment. RESULTS: Cannabis sativa is a plant rich in more than 100 types of cannabinoids...
August 11, 2017: Journal of Alternative and Complementary Medicine: Research on Paradigm, Practice, and Policy
https://www.readbyqxmd.com/read/28792725/pharmacology-of-cumyl-carboxamide-synthetic-cannabinoid-new-psychoactive-substances-nps-cumyl-bica-cumyl-pica-cumyl-5f-pica-cumyl-5f-pinaca-and-their-analogues
#3
Mitchell Longworth, Samuel D Banister, Rochelle Boyd, Richard C Kevin, Mark Connor, Iain S McGregor, Michael Kassiou
Synthetic cannabinoids (SC) are the largest class of new psychoactive substances (NPS), and are increasingly associated with serious adverse effects. The majority of SC NPS are 1,3-disubstituted indoles and indazoles featuring a diversity of subunits at the 1- and 3-positions. Most recently, cumyl-derived indole- and indazole-3-carboxamides have been detected by law enforcement agencies and by emergency departments. Herein we describe the synthesis, characterization, and pharmacology of SCs CUMYL-BICA, CUMYL-PICA, CUMYL-5F-PICA, CUMYL-PINACA, CUMYL-5F-PINACA, and related analogues...
August 11, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28771321/activity-based-detection-of-consumption-of-synthetic-cannabinoids-in-authentic-urine-samples-using-a-stable-cannabinoid-reporter-system
#4
Annelies Cannaert, Florian Franz, Volker Auwärter, Christophe P Stove
Synthetic cannabinoids (SCs) continue to be the largest group of new psychoactive substances (NPS) monitored by the European Monitoring Center of Drugs and Drugs of Abuse (EMCDDA). The identification and subsequent prohibition of single SCs has driven clandestine chemists to produce analogues of increasing structural diversity, intended to evade legislation. That structural diversity, combined with the mostly unknown metabolic profiles of these new SCs, poses a big challenge for the conventional targeted analytical assays, as it is difficult to screen for 'unknown' compounds...
August 3, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28758232/administrations-of-thalidomide-into-the-rostral-ventromedial-medulla-produce-antinociceptive-effects-in-a-rat-model-of-postoperative-pain
#5
Tieying Song, Xiaojing Ma, Pengyu Ma, Kunfeng Gu, Jianhui Zhao, Yunliang Yang, Bo Jiang, Yuxia Li, Chunping Wang
The rostral ventromedial medulla (RVM) is highly involved in pain signal transmissions. Previous studies have shown that thalidomide is anti-nociceptive. Thus, we evaluated the neurobiological mechanisms of thalidomide in the RVM in the regulation of postoperative pain. We used a rat model of postoperative pain to investigate the effects of intra-RVM thalidomide treatments on postoperative pain, and evaluate the role of cannabinoid receptors in the effects of intra-RVM thalidomide treatments on GABAergic neurotransmission in the RVM neurons...
July 31, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28754373/cannabidiol-disrupts-the-consolidation-of-specific-and-generalized-fear-memories-via-dorsal-hippocampus-cb1-and-cb2-receptors
#6
Cristina A J Stern, Thiago R da Silva, Ana M Raymundi, Camila P de Souza, Vinicius A Hiroaki-Sato, Luiza Kato, Francisco S Guimarães, Roberto Andreatini, Reinaldo N Takahashi, Leandro J Bertoglio
Pharmacological interventions able to modulate a fear memory while it is consolidated could have therapeutic value in tempering those maladaptively overconsolidated. Animal and human studies have shown the intensity of unconditioned stimulus delivered during fear conditioning influences qualitative and quantitative aspects of the memory to be established. By varying the shock intensity used for contextual pairing in rats, here we induced specific and more generalized long-term fear memories to investigate whether, how and where in the brain the cannabidiol (CBD; 3...
July 25, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28750813/methods-for-the-development-of-in-silico-gpcr-models
#7
Paula Morales, Dow P Hurst, Patricia H Reggio
The Reggio group has constructed computer models of the inactive and G-protein-activated states of the cannabinoid CB1 and CB2 receptors, as well as, several orphan receptors that recognize a subset of cannabinoid compounds, including GPR55 and GPR18. These models have been used to design ligands, mutations, and covalent labeling studies. The resultant second-generation models have been used to design ligands with improved affinity, efficacy, and subtype selectivity. Herein, we provide a guide for the development of GPCR models using the most recent orphan receptor studied in our lab, GPR3...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28747360/cannabinoids-and-the-kidney-effects-in-health-and-disease
#8
Frank Park, Praveen K Potukuchi, Hamid Moradi, Csaba P Kovesdy
Consumption of cannabis and various related products (cannabinoids) for both medicinal and recreational use is gaining popularity. Furthermore, regulatory changes are fostering a cultural shift towards increasing liberalization of cannabis use, thereby increasing the likelihood of even larger numbers of individuals being exposed in the future. The two different types of receptors (CB1 and CB2) that are activated by the pharmacologically active ingredients of cannabis are found in numerous tissues, including the kidneys...
July 26, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28743542/the-endocannabinoid-system-expression-in-the-female-reproductive-tract-is-modulated-by-estrogen
#9
J Maia, M Almada, A Silva, G Correia-da-Silva, N Teixeira, S I Sá, B M Fonseca
The endocannabinoid system (ECS) is involved in several physiological events that resulted in a growing interest in its modulation. Moreover, the uterine levels of anandamide (AEA), the major endocannabinoid, must be tightly regulated to create proper embryo implantation conditions. However, there are no evidences about the regulation of AEA in uterus by estrogen. Thus, the aim of this study is to elucidate whether estradiol benzoate (EB) and tamoxifen (TAM) administration to ovariectomized (OVX) rats can induce changes in the expression of cannabinoid receptors and AEA-metabolic enzymes in uterus by evaluating gene transcription and protein levels by qPCR, Western blot and immunohistochemistry...
July 22, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28738764/neuroprotection-by-endo-cannabinoids-in-glaucoma-and-retinal-neurodegenerative-diseases
#10
Cinzia Rapino, Daniel Tortolani, Lucia Scipioni, Mauro Maccarrone
Emerging neuroprotective strategies are being explored to preserve the retina from degeneration, that occurs in eye pathologies like glaucoma, diabetic retinopathy, age-related macular degeneration, and retinitis pigmentosa. Incidentally, neuroprotection of retina is a defending mechanism designed to prevent or delay neuronal cell death, and to maintain neural function following an initial insult, thus avoiding loss of vision. Numerous studies have investigated potential neuroprotective properties of plant-derived phytocannabinoids, as well as of their endogenous counterparts collectively termed endocannabinoids (eCBs), in several degenerative diseases of the retina...
July 24, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28729064/effects-of-cannabinoid-drugs-on-aversive-and-rewarding-drug-associated-memory-extinction-and-reconsolidation
#11
REVIEW
Cristina A J Stern, Cristiane R de Carvalho, Leandro J Bertoglio, Reinaldo N Takahashi
Posttraumatic stress and drug use disorders may stem from aberrant memory formation. As the endocannabinoid (eCB) system has a pivotal role in emotional memory processing and related synaptic plasticity, here we seek to review and discuss accumulating evidence on how and where in the brain interventions targeting the eCB system would attenuate outcomes associated with traumatic events and/or drug addiction through memory extinction facilitation or memory reconsolidation disruption. Currently available data from mouse, rat, monkey and healthy human studies investigating the effects of cannabinoid drugs on the extinction and reconsolidation of aversive memories are more consistent than those related to rewarding drug-associated memories...
July 17, 2017: Neuroscience
https://www.readbyqxmd.com/read/28728428/consequence-of-dopamine-d2-receptor-blockade-on-the-hyperphagic-effect-induced-by-cannabinoid-cb1-and-cb2-receptors-in-layers
#12
M Khodadadi, M Zendehdel, A Baghbanzadeh, V Babapour
1. Endocannabinoids (ECBs) and their receptors play a regulatory function on several physiological processes such as feed-intake behaviour, mainly in the brain. This study was carried out in order to investigate the effects of the dopaminergic D1 and D2 receptors on CB1/CB2 ECB receptor-induced hyperphagia in 3-h feed-deprived neonatal layer chickens. 2. A total of 8 experiments were designed to explore the interplay of these two modulatory systems on feed intake in neonatal chickens. In Experiment 1, chickens were intracerebroventricular (ICV) injected with control solution, l-DOPA (levo-dihydroxyphenylalanine as precursor of dopamine; 125 nmol), 2-AG (2-arachidonoylglycerol as CB1 receptor agonist; 2 µg) and co-administration of l-DOPA (125 nmol) plus 2-AG (2 µg)...
August 16, 2017: British Poultry Science
https://www.readbyqxmd.com/read/28726401/amidoalkylindoles-as-potent-and-selective-cannabinoid-type-2-receptor-agonists-with-in-vivo-efficacy-in-a-mouse-model-of-multiple-sclerosis
#13
Ying Shi, Yan-Hui Duan, Yue-Yang Ji, Zhi-Long Wang, Yan-Ran Wu, Hendra Gunosewoyo, Xiao-Yu Xie, Jian-Zhong Chen, Fan Yang, Jing Li, Jie Tang, Xin Xie, Li-Fang Yu
Selective CB2 agonists represent an attractive therapeutic strategy for the treatment of a variety of diseases without psychiatric side effects mediated by the CB1 receptor. We carried out a rational optimization of a black market designer drug SDB-001 that led to the identification of potent and selective CB2 agonists. A 7-methoxy or 7-methylthio substitution at the 3-amidoalkylindoles resulted in potent CB2 antagonists (27 or 28, IC50 = 16-28 nM). Replacement of the amidoalkyls from 3-position to the 2-position of the indole ring dramatically increased the agonist selectivity on the CB2 over CB1 receptor...
August 3, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28726104/n-acyl-dopamines-induce-apoptosis-in-pc12-cell-line-via-the-gpr55-receptor-activation
#14
M G Akimov, A M Ashba, N M Gretskaya, V V Bezuglov
Dopamine amides of arachidonic, docosahexaenoic, and oleic acids were found to induce apoptosis in PC12 cells, which was blocked exclusively by antagonists and preincubation agonists of the receptor GPR55, belonging to the group of non-CB1/CB2 receptors.
May 2017: Doklady. Biochemistry and Biophysics
https://www.readbyqxmd.com/read/28722246/delta-9-tetrahydrocannabinol-decreases-masticatory-muscle-sensitization-in-female-rats-through-peripheral-cannabinoid-receptor-activation
#15
H Wong, S Hossain, B E Cairns
BACKGROUND: This study investigated whether intramuscular injection of delta-9-tetrahydrocannabinol (THC), by acting on peripheral cannabinoid (CB) receptors, could decrease nerve growth factor (NGF)-induced sensitization in female rat masseter muscle; a model which mimics the symptoms of myofascial temporomandibular disorders. METHODS: Immunohistochemistry was used to explore the peripheral expression of cannabinoid receptors in the masseter muscle while behavioural and electrophysiology experiments were employed to assess the functional effects of intramuscular injection of THC...
July 18, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28720466/antinociceptive-effects-of-huf-101-a-fluorinated-cannabidiol-derivative
#16
Nicole R Silva, Felipe V Gomes, Miriam D Fonseca, Raphael Mechoulam, Aviva Breuer, Thiago M Cunha, Francisco S Guimarães
Cannabidiol (CBD) is a phytocannabinoid with multiple pharmacological effects and several potential therapeutic properties. Its low oral bioavailability, however, can limit its clinical use. Preliminary results indicate that fluorination of the CBD molecule increases its pharmacological potency. Here, we investigated whether HUF-101 (3, 10, and 30mg/kg), a fluorinated CBD analogue, would induce antinociceptive effects. HUF-101 effects were compared to those induced by CBD (10, 30, and 90mg/kg) and the cannabinoid CB1/2 receptor agonist WIN55,212-2 (1, 3, and 5mg/kg)...
July 15, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28716633/the-synthetic-cannabinoid-win55212-2-ameliorates-traumatic-spinal-cord-injury-via-inhibition-of-gapdh-siah1-in-a-cb2-receptor-dependent-manner
#17
Bin-Xiao Su, Xin Chen, Jia Huo, Shu-Yun Guo, Rui Ma, Yan-Wu Liu
The essential role of GAPDH/Siah1 signaling pathway in the pathogenesis of various injurious conditions such as traumatic spinal cord injury (SCI) has been gradually recognized. However, the drugs targeting this signaling pathway are still lacking. The endocannabinoid system, including its receptors (CB1 and CB2), act as neuroprotective and immunomodulatory modulators in SCI. WIN55212-2, an agonist for CB1 and CB2 receptors, has been demonstrated with anti-inflammatory and anti-apoptotic effects in multiple neurological diseases...
July 14, 2017: Brain Research
https://www.readbyqxmd.com/read/28700706/spatial-distribution-of-cannabinoid-receptor-type-1-cb1-in-normal-canine-central-and-peripheral-nervous-system
#18
Jessica Freundt-Revilla, Kristel Kegler, Wolfgang Baumgärtner, Andrea Tipold
The endocannabinoid system is a regulatory pathway consisting of two main types of cannabinoid receptors (CB1 and CB2) and their endogenous ligands, the endocannabinoids. The CB1 receptor is highly expressed in the central and peripheral nervous systems (PNS) in mammalians and is involved in neuromodulatory functions. Since endocannabinoids were shown to be elevated in cerebrospinal fluid of epileptic dogs, knowledge about the species specific CB receptor expression in the nervous system is required. Therefore, we assessed the spatial distribution of CB1 receptors in the normal canine CNS and PNS...
2017: PloS One
https://www.readbyqxmd.com/read/28691158/anticonvulsant-effect-of-cannabinoid-receptor-agonists-in-models-of-seizures-in-developing-rats
#19
Megan N Huizenga, Evan Wicker, Veronica C Beck, Patrick A Forcelli
OBJECTIVE: Although drugs targeting the cannabinoid system (e.g., CB1 receptor agonists) display anticonvulsant efficacy in adult animal models of seizures/epilepsy, they remain unexplored in developing animal models. However, cannabinoid system functions emerge early in development, providing a rationale for targeting this system in neonates. We examined the therapeutic potential of drugs targeting the cannabinoid system in three seizure models in developing rats. METHODS: Postnatal day (P) 10, Sprague-Dawley rat pups were challenged with the chemoconvulsant methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM) or pentylenetetrazole (PTZ), after treatment with either CB1/2 mixed agonist (WIN 55,212-2), CB1 agonist (arachidonyl-2'-chloroethylamide [ACEA]), CB2 agonist (HU-308), CB1 antagonist (AM-251), CB2 antagonist (AM-630), fatty acid amide hydrolase inhibitor (URB-597), or G protein-coupled receptor 55 agonist (O-1602)...
July 10, 2017: Epilepsia
https://www.readbyqxmd.com/read/28689299/4-o-methylhonokiol-protects-from-alcohol-carbon-tetrachloride-induced-liver-injury-in-mice
#20
Eleonora Patsenker, Andrea Chicca, Vanessa Petrucci, Sheida Moghadamrad, Andrea de Gottardi, Jochen Hampe, Jürg Gertsch, Nasser Semmo, Felix Stickel
Alcoholic liver disease (ALD) is a leading cause of liver cirrhosis, liver cancer, and related mortality. The endocannabinoid system contributes to the development of chronic liver diseases, where cannabinoid receptor 2 (CB2) has been shown to have a protecting role. Thus, here, we investigated how CB2 agonism by 4'-O-methylhonokiol (MHK), a biphenyl from Magnolia grandiflora, affects chronic alcohol-induced liver fibrosis and damage in mice. A combination of alcohol (10% vol/vol) and CCl4 (1 ml/kg) was applied to C57BL/6 mice for 5 weeks...
July 8, 2017: Journal of Molecular Medicine: Official Organ of the "Gesellschaft Deutscher Naturforscher und Ärzte"
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