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https://www.readbyqxmd.com/read/28814985/activation-of-endocannabinoid-receptor-2-as-a-mechanism-of-propofol-pretreatment-induced-cardioprotection-against-ischemia-reperfusion-injury-in-rats
#1
Hai-Jing Sun, Yan Lu, Hao-Wei Wang, Hao Zhang, Shuang-Ran Wang, Wen-Yun Xu, Hai-Long Fu, Xue-Ya Yao, Feng Yang, Hong-Bin Yuan
Propofol pretreatment before reperfusion, or propofol conditioning, has been shown to be cardioprotective, while its mechanism is unclear. The current study investigated the roles of endocannabinoid signaling in propofol cardioprotection in an in vivo model of myocardial ischemia/reperfusion (I/R) injury and in in vitro primary cardiomyocyte hypoxia/reoxygenation (H/R) injury. The results showed that propofol conditioning increased both serum and cell culture media concentrations of endocannabinoids including anandamide (AEA) and 2-arachidonoylglycerol (2-AG) detected by LC-MS/MS...
2017: Oxidative Medicine and Cellular Longevity
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
#2
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/28803965/the-great-divide-separation-between-in-vitro-and-in-vivo-effects-of-psncbam-based-cb1-receptor-allosteric-modulators
#3
Thomas F Gamage, Charlotte E Farquhar, Timothy W Lefever, Brian F Thomas, Thuy Nguyen, Yanan Zhang, Jenny L Wiley
While allosteric modulators of the cannabinoid type-1 receptor (CB1) continue to be developed and characterized, the gap between the in vitro and in vivo data is widening, raising questions regarding translatability of their effects and biological relevance. Among the CB1 allosteric modulators, PSNCBAM-1 has received little attention regarding its effects in vivo. Recently, pregnenolone was reported to act as an allosteric modulator of CB1, blocking THC's effects in vitro and in vivo, highlighting the potential of CB1 allosteric modulators for treatment of cannabis intoxication...
August 10, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28800377/antidote-to-cannabinoid-intoxication-inverse-cannabinoid-receptor-one-cb1-agonism-by-n-piperidin-1-yl-5-4-iodophenyl-1-2-4-dichlorophenyl-4-methyl-1h-pyrazole-3-carboxamidse-am251-reverses-the-hypothermic-effects-of-cannabinoid-receptor-one-agonism-by-1-naphthalenyl
#4
Gareth Pryce, David Baker
BACKGROUND & PURPOSE: Cannabis is a recreational drug leading to intoxication, due to cannabinoid receptor one (CB1 ) stimulation. However, more recently herbs mixed with synthetic cannabinoids sometimes known as "Spice" and "Black Mamba" have been increasing used and their high CB1 receptor affinity means not only marked intoxication, but life-threatening complications and an increasing number of deaths. Whilst many studies have indicated that prophylactic CB1 receptor antagonism can block cannabimimetic effects in animals and humans...
August 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28799775/a-review-of-the-therapeutic-antitumor-potential-of-cannabinoids
#5
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/28794966/synthetic-cannabinoid-induced-acute-respiratory-depression-case-series-and-literature-review
#6
Mark Henry Alon, Margaret Olibrice Saint-Fleur
Synthetic Cannabinoids are a street drug that is widely attainable and cheap compared to natural cannabis, and has variable potency and unpredictable effects with no commercially available diagnostic test to confirm its presence. Similar to natural cannabis, Synthetic Cannabinoid intoxication can present in several ways with the most common emergency room presentations to be of neurologic and psychiatric manifestation. The respiratory depressive effect of Synthetic Cannabinoids has not been well documented in medical literature...
2017: Respiratory Medicine Case Reports
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
#7
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/28792219/novel-diarylurea-based-allosteric-modulators-of-the-cannabinoid-cb1-receptor-evaluation-of-importance-of-6-pyrrolidinylpyridinyl-substitution
#8
Thuy Nguyen, Nadezhda German, Ann M Decker, Tiffany L Langston, Thomas F Gamage, Charlotte E Farquhar, Jun-Xu Li, Jenny L Wiley, Brian F Thomas, Yanan Zhang
Allosteric modulators of the cannabinoid CB1 receptor have recently been reported as an alternative approach to modulate the CB1 receptor for therapeutic benefits. In this study, we report the design and synthesis of a series of diarylureas derived from PSNCBAM-1 (2). Similar to 2, these diarylureas dose-dependently inhibited CP55,940-induced intracellular calcium mobilization and [(35)S]GTP-γ-S binding while enhancing [(3)H]CP55,940 binding to the CB1 receptor. Structure-activity relationship studies revealed that the pyridinyl ring of 2 could be replaced by other aromatic rings and the pyrrolidinyl ring is not required for CB1 allosteric modulation...
August 18, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28780734/intra-accumbal-cannabinoid-agonist-attenuated-reinstatement-but-not-extinction-period-of-morphine-induced-conditioned-place-preference-evidence-for-different-characteristics-of-extinction-period-and-reinstatement
#9
Hossein Khaleghzadeh-Ahangar, Abbas Haghparast
The brain reward system consists of the ventral tegmental area that sends its dopaminergic projections to the forebrain, cortical areas, amygdala and largely to the nucleus accumbens (NAc). The present study aims were to investigate the effects of bilateral intra-accumbal microinjection of WIN55,212-2, a CB1 receptor agonist, on the duration of extinction period and reinstatement to morphine by the conditioned place preference (CPP) paradigm in the rat. Forty-six adult male albino Wistar rats received intra-accumbal WIN55,212-2 [p0...
August 5, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28771697/effects-of-centrally-administered-endocannabinoids-and-opioids-on-orofacial-pain-perception-in-rats
#10
Marek Zubrzycki, Anna Janecka, Andreas Liebold, Mechthild Ziegler, Maria Zubrzycka
BACKGROUND AND PURPOSE: Endocannabinoids and opioids play a vital role in mediating pain-induced analgesia. The specific effects of these compounds within orofacial region are largely unknown. In this study we tried to determine whether the increase of cannabinoid and opioid concentration in cerebrospinal fluid affects impulse transmission between the motor centers localized in the vicinity of the third and fourth cerebral ventricles. EXPERIMENTAL APPROACH: The study objectives were realized on rats using the method allowing to record the amplitude of evoked tongue jerks (ETJ) in response to noxious tooth pulp stimulation...
August 3, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28771321/activity-based-detection-of-consumption-of-synthetic-cannabinoids-in-authentic-urine-samples-using-a-stable-cannabinoid-reporter-system
#11
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/28759733/protective-effect-of-rimonabant-a-canabinoid-receptor-1-antagonist-on-nonalcoholic-fatty-liver-disease-in-a-rat-model-by-modulating-the-hepatic-expression-of-activin-a-and-follistatin
#12
Noha Ibrahim Hussien, Hanan I El-Kerdasy, Mohamed El-Tantawy Ibrahim
Non-alcoholic fatty liver disease (NAFLD) is a major cause of liver morbidity and mortality with no proven effective therapy yet. Endocannabinoid system plays an important role in various liver diseases. Activin A is a member of the transforming growth factor beta (TGF-β) superfamily and inhibits hepatocyte growth. Follistatin antagonizes the biological actions of activin A. The present study was designed to investigate the effect of rimonabant (a potent cannabinoid receptor1 (CB1) antagonist) on NAFLD induced by choline deficient (CD) diet in rats, as well as to detect whether it can modulate the hepatic expression of activin A and follistatin or not...
July 31, 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28758232/administrations-of-thalidomide-into-the-rostral-ventromedial-medulla-produce-antinociceptive-effects-in-a-rat-model-of-postoperative-pain
#13
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/28757328/interferon-%C3%AE-causes-mood-abnormalities-by-altering-cannabinoid-cb1-receptor-function-in-the-mouse-striatum
#14
Georgia Mandolesi, Silvia Bullitta, Diego Fresegna, Antonietta Gentile, Francesca De Vito, Ettore Dolcetti, Francesca R Rizzo, Georgios Strimpakos, Diego Centonze, Alessandra Musella
Interferon-γ (IFN-γ) has been implicated in the pathogenesis of multiple sclerosis (MS) and in its animal model, experimental autoimmune encephalomyelitis (EAE). The type-1 cannabinoid receptors (CB1Rs) are heavily involved in MS pathophysiology, and a growing body of evidence suggests that mood disturbances reflect specific effects of proinflammatory cytokines on neuronal activity. Here, we investigated whether IFN-γ could exert a role in the anxiety- and depressive-like behavior observed in mice with EAE, and in the modulation of CB1Rs...
July 27, 2017: Neurobiology of Disease
https://www.readbyqxmd.com/read/28757061/radiosynthesis-and-evaluation-of-new-pet-ligands-for-peripheral-cannabinoid-receptor-type-1-imaging
#15
Tomoteru Yamasaki, Masayuki Fujinaga, Yoko Shimoda, Wakana Mori, Yiding Zhang, Hidekatsu Wakizaka, Masanao Ogawa, Ming-Rong Zhang
Cannabinoid receptor type 1 (CB1) is mainly expressed in the brain, as well as being expressed in functional relevant concentrations in various peripheral tissues. 1-(4-Chlorophenyl)-3-(3-(6-(pyrrolidin-1-yl)pyridin-2-yl)phenyl)urea (PSNCBAM-1, 1) was developed as a potent allosteric antagonist for CB1 and its oral administration led to reductions in the appetite and body weight of rats. Several analogs of 1 (compounds 2 and 3) were recently identified through a series of structure-activity relationship studies...
July 18, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28754373/cannabidiol-disrupts-the-consolidation-of-specific-and-generalized-fear-memories-via-dorsal-hippocampus-cb1-and-cb2-receptors
#16
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/28750814/real-time-measurement-of-cannabinoid-receptor-mediated-camp-signaling
#17
Morag R Hunter, David B Finlay, Christa E Macdonald, Erin E Cawston, Natasha L Grimsey, Michelle Glass
Cannabinoid receptors, like other GPCRs, signal via a spectrum of related signaling pathways. Recently, monitoring GPCR-mediated cAMP signaling has become significantly easier with the development of genetically encoded, transfectable cAMP biosensors. Cell lines transfected with these biosensors can be monitored continuously, allowing the analysis of receptor-mediated signaling in unprecedented detail. Here, we describe a protocol for transfectable biosensors which report cellular cAMP concentrations by bioluminescence resonance energy transfer (BRET)...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28750813/methods-for-the-development-of-in-silico-gpcr-models
#18
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/28750810/purification-of-functional-cb1-and-analysis-by-site-directed-fluorescence-labeling-methods
#19
Jonathan F Fay, David L Farrens
The human cannabinoid receptor, CB1, has been difficult to purify in a functional form, hampering structural and biophysical studies. Here, we present our approaches for obtaining pure, detergent solubilized, functional CB1. We also discuss our site-directed fluorescence labeling (SDFL) methods for identifying different structural changes that CB1 can undergo upon binding different cannabinoid ligands. To identify optimal CB1 constructs for these studies (those with the best expression levels, solubility in detergent and function), we first screened various CB1-green fluorescent protein chimeras in a mammalian expression system...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28750809/assessing-allosteric-modulation-of-cb1-at-the-receptor-and-cellular-levels
#20
Caitlin E Scott, Debra A Kendall
The cannabinoid CB1 receptor is abundant in the central nervous system and regulates neuronal transmission and other key physiological processes including those leading to pain, inflammation, memory, and feeding behavior. CB1 is activated by the endogenous ligands, arachidonoyl ethanolamine and 2-arachidonoyl glycerol, by various synthetic ligands (e.g., CP55940), and by Δ(9)-tetrahydrocannabinol, the psychoactive component of Cannabis sativa. These CB1 ligands are orthosteric and transduce downstream signals by binding CB1 and primarily inducing Gi coupling, but Gs and β-arrestin coupling are also possible...
2017: Methods in Enzymology
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