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https://www.readbyqxmd.com/read/29457749/chemical-and-biological-studies-on-bridelia-ferruginea-grown-in-nigeria
#1
Michael Afolayan, Radhakrishnan Srivedavyasasri, Olayinka T Asekun, Oluwole B Familoni, Samir A Ross
Phytochemical investigation of the methanolic extract of dried leaves of Bridelia ferruginea led to the isolation and identification of fourteen compounds (1-14): compound 1 [mixture of palmitic, stearic and oleic acids], stearyl monoester of 2-O-β-ᴅ-glucosylglycerol (2), 6β-hydroxy-(20R)-24-ethylcholest-4-en-3-one (3a), 6β-hydroxy-(20R)-24-ethylcholest-4,22-dien-3-one (3b), lutein (4), vomifoliol (5), corilagin (6), kaempferide-3-O-β-ᴅ-glucoside (7), myricetin (8), isomericitrin (9), isoquercetin (10), myricitrin (11), quercitrin (12), rutin (13), and β-sitosterol glucoside (14)...
February 19, 2018: Natural Product Research
https://www.readbyqxmd.com/read/29441900/role-of-the-endocannabinoid-system-in-the-formation-and-development-of-depression
#2
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/29439093/dysregulated-genes-and-their-functional-pathways-in-luteinized-granulosa-cells-from-pcos-patients-after-cabergoline-treatment
#3
Hortensia Ferrero, Patricia Diaz-Gimeno, Patricia Sebastian-Leon, Amparo Faus, Raul Gómez, Antonio Pellicer
Polycystic ovarian syndrome (PCOS) is a common reproductive disorder frequently associated with a substantial risk factor for ovarian hyperstimulation syndrome (OHSS). Dopamine receptor 2 (D2) agonists, like Cabergoline (Cb2), have been used to reduce the OHSS risk. However, lutein granulosa cells (LGCs) from PCOS patients treated with Cb2 still show a deregulated dopaminergic tone (decreased D2 expression and low dopamine production) and increased vascularization compared to non-PCOS LGCs. Therefore, to understand the PCOS ovarian physiology, it is important to explore the mechanisms that underlie syndrome based on the therapeutic effects of Cb2...
February 9, 2018: Reproduction: the Official Journal of the Society for the Study of Fertility
https://www.readbyqxmd.com/read/29435814/alterations-in-gene-and-protein-expression-of-cannabinoid-cb-2-and-gpr55-receptors-in-the-dorsolateral-prefrontal-cortex-of-suicide-victims
#4
María S García-Gutiérrez, Francisco Navarrete, Gemma Navarro, Irene Reyes-Resina, Rafael Franco, Jose Luis Lanciego, Salvador Giner, Jorge Manzanares
Recent studies point to the cannabinoid CB 2 receptors (CB 2 r) and the non-cannabinoid receptor GPR55 as potential key targets involved in the response to stress, anxiety, and depression. Considering the close relationship between neuropsychiatric disorders and suicide, the purpose of this study was to evaluate the potential alterations of CB 2 r and GPR55 in suicide victims. We analyzed gene and protein expression of both receptors by real-time PCR and western blot, respectively, in the dorsolateral prefrontal cortex (DLPFC) of 18 suicide victims with no clinical psychiatric history or treatment with anxiolytics or antidepressants, and 15 corresponding controls...
February 12, 2018: Neurotherapeutics: the Journal of the American Society for Experimental NeuroTherapeutics
https://www.readbyqxmd.com/read/29425797/antinociceptive-effects-of-the-endogenous-cannabinoid-peptide-agonist-vd-hemopressin-%C3%AE-in-mice
#5
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
https://www.readbyqxmd.com/read/29424035/involvement-of-spinal-cannabinoid-receptors-in-the-antipruritic-effects-of-win-55-212-2-a-cannabinoid-receptor-agonist
#6
K A Bilir, G Anli, E Ozkan, O Gunduz, A Ulugol
BACKGROUND: Cannabinoids have been used for their analgesic and euphoric effects for millennia, but recently the antipruritic effects of cannabis have been discovered. Considering the similarities between pain and itch sensations, we hypothesized that cannabinoid receptors may play a role in the antipruritic effects of cannabinoids. AIM: To analyse the role of the spinal cannabinoid receptors, CB1 and CB2, in the antipruritic effects of the cannabinoid agonist WIN 55,212-2...
February 9, 2018: Clinical and Experimental Dermatology
https://www.readbyqxmd.com/read/29420021/a-selective-photoaffinity-probe-enables-assessment-of-cannabinoid-cb2-receptor-expression-and-ligand-engagement-in-human-cells
#7
Marjolein Soethoudt, Sara C Stolze, Matthias V Westphal, Luuk van Stralen, Andrea Martella, Eva J van Rooden, Wolfgang Guba, Zoltan V Varga, Hui Deng, Sander I van Kasteren, Uwe Grether, Adriaan P IJzerman, Pal Pacher, Erick M Carreira, Herman S Overkleeft, Andreea Ioan-Facsinay, Laura H Heitman, Mario van der Stelt
Chemical tools and methods that report on G protein-coupled receptor (GPCR) expression levels and receptor occupancy by small molecules are highly desirable. We report the development of LEI121 as a photoreactive probe to study the type 2 cannabinoid receptor (CB2R), a promising GPCR to treat tissue injury and inflammatory diseases. LEI121 is the first CB2R-selective bifunctional probe that covalently captures CB2R upon photoactivation. An incorporated alkyne serves as ligation handle for the introduction of reporter groups...
February 8, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29419319/synthesis-and-biological-evaluation-of-ferrocene-based-cannabinoid-receptor-2-ligands
#8
Supojjanee Sansook, Wei Tuo, Mélanie Bollier, Amélie Barczyk, Xavier Dezitter, Fredérique Klupsch, Natascha Leleu-Chavain, Amaury Farce, Graham J Tizzard, Simon J Coles, John Spencer, Régis Millet
Ferrocene analogs of known fatty acid amide hydrolase inhibitors and CB2 ligands have been synthesized and characterized spectroscopically and crystallographically. The resulting bio-organometallic isoxazoles were assayed for their effects on CB1 and CB2 receptors as well as on fatty acid amide hydrolase. None had any fatty acid amide hydrolase activity but compound 3, 5-(2-(pentyloxy)phenyl)-N-ferrocenylisoxazole-3-carboxamide, was found to be a potent CB2 ligand (Ki = 32.5 nM).
February 8, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29412125/the-endocannabinoid-system-and-heart-disease-the-role-of-cannabinoid-receptor-type-2
#9
Morad Hebi, Douglas P Thewke
Decades of research has provided evidence for the role of the endocannabinoid system in human health and disease. This versatile system, consisting of two receptors (CB1 and CB2), their endogenous ligands (endocannabinoids), and metabolic enzymes has been implicated in a wide variety of disease states, ranging from neurological disorders to cancer. CB2 has gained much interest for its beneficial immunomodulatory role that can be obtained without eliciting psychotropic effects through CB1. Recent studies have shed light on a protective role of CB2 in cardiovascular disease, an ailment which currently takes more lives each year in Western countries than any other disease or injury...
February 6, 2018: Cardiovascular & Hematological Disorders Drug Targets
https://www.readbyqxmd.com/read/29410032/the-synthetic-cannabinoid-xlr-11-induces-in-vitro-nephrotoxicity-by-impairment-of-endocannabinoid-mediated-regulation-of-mitochondrial-function-homeostasis-and-triggering-of-apoptosis
#10
João P Silva, Helena Carmo, Félix Carvalho
Synthetic cannabinoids (SCBs)-related intoxications and deaths have been increasingly reported, turning its widespread recreational use into a major public health concern. Specifically, a direct link between SCBs and acute kidney injury (AKI) has been established. XLR-11 is an SCB commonly found in the toxicological analysis of patients with SCB-associated AKI. However, the pathophysiology of AKI among SCB consumers remains unknown. This work thus represents the first in vitro assessment of SCB nephrotoxicity, as a first approach to identify its cellular targets...
February 3, 2018: Toxicology Letters
https://www.readbyqxmd.com/read/29408878/the-endocannabinoid-system-in-canine-steroid-responsive-meningitis-arteritis-and-intraspinal-spirocercosis
#11
Jessica Freundt-Revilla, Franciska Heinrich, Alexander Zoerner, Felix Gesell, Martin Beyerbach, Merav Shamir, Anna Oevermann, Wolfgang Baumgärtner, Andrea Tipold
Endocannabinoids (ECs) are involved in immunomodulation, neuroprotection and control of inflammation in the central nervous system (CNS). Activation of cannabinoid type 2 receptors (CB2) is known to diminish the release of pro-inflammatory factors and enhance the secretion of anti-inflammatory cytokines. Furthermore, the endocannabinoid 2-arachidonoyl glycerol (2-AG) has been proved to induce the migration of eosinophils in a CB2 receptor-dependent manner in peripheral blood and activate neutrophils independent of CB activation in humans...
2018: PloS One
https://www.readbyqxmd.com/read/29407967/optimization-of-the-metabolic-stability-of-a-fluorinated-cannabinoid-receptor-subtype-2-cb2-ligand-designed-for-pet-studies
#12
Dominik Heimann, Frederik Börgel, Henk de Vries, Marius Patberg, Eliot Jan-Smith, Bastian Frehland, Dirk Schepmann, Laura H Heitman, Bernhard Wünsch
The central CB2 receptor represents a promising target for the treatment of neuroinflammatory diseases as CB2 activation mediates anti-inflammatory effects. Recently, the F-18 labeled PET radiotracer [18F]7a was reported, which shows high CB2 affinity and high selectivity over the CB1 subtype but low metabolic stability due to hydrolysis of the amide group. Based on these findings twelve bioisosteres of 7a were synthesized containing a non-hydrolysable functional group instead of the amide group. The secondary amine 23a (Ki = 7...
January 30, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29407590/alkyl-indole-based-cannabinoid-type-2-receptor-tools-exploration-of-linker-and-fluorophore-attachment
#13
Anna G Cooper, Christa MacDonald, Michelle Glass, Sarah Hook, Joel D A Tyndall, Andrea J Vernall
Cannabinoid type 2 (CB2) receptor continues to emerge as a promising drug target for many diseases and conditions. New tools for studying CB2 receptor are required to further inform how this receptor functions in healthy and diseased states. The alkyl indole scaffold is a well-recognised ligand for cannabinoid receptors, and in this study the indole C5-7 positions were explored for linker and fluorophore attachment. A new high affinity, CB2 receptor selective inverse agonist was identified (16b) along with a general trend of C5-substituted indoles acting as agonists versus C7-substituted indoles acting as inverse agonists...
February 10, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29406831/contribution-of-spinal-5-ht5a-receptors-to-the-antinociceptive-effects-of-systemically-administered-cannabinoid-agonist-win-55-212-2-and-morphine
#14
Ahmet Goktan Aksu, Ozgur Gunduz, Ahmet Ulugol
The antinociceptive effects of cannabinoids and opioids have been known for centuries. Serotonin and its receptors are also known to play important roles in nociception. However, the contribution of spinal 5-HT5A receptors in antinociceptive effects of cannabinoids and opioids has not been studied. We conducted this study to clarify spinal mechanisms of the actions of the antinociceptive effects of cannabinoids and opioids. Hot-plate and tail-flick tests were used to assess the antinociceptive activity in Balb/c mice...
February 6, 2018: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/29404698/novel-derivatives-of-1-2-3-triazole-cannabinoid-1-receptor-ligands-modulate-gastrointestinal-motility-in-mice
#15
Agata Szymaszkiewicz, Marta Zielinska, Kun Li, Mani Ramanathan, Safiul Alam, Duen-Ren Hou, Jakub Fichna, Martin Storr
Cannabinoid-1 (CB1) receptors are broadly distributed in the central and peripheral nervous systems; among others, they are located in the enteric nervous system. In the gastrointestinal (GI) system, they participate in regulation of intestinal motility or ion transport. The aim of our study was to assess the effect of 1,2,3-triazole derivatives (compound 1: 2-[4,5-bis(2,4-dichlorophenyl)-2H-1,2,3-triazol-2-yl]-N-(2-fluorobenzyl)acetamide, compound 2: 2-[4,5-bis(2,4-dichlorophenyl)-2H-1,2,3-triazol-2-yl]-N-(4-fluorobenzyl)acetamide, compound 3: N-benzyl-2-[4-(4-chlorophenyl)-5-(2,4-dichlorophenyl)-2H-1,2,3-triazol-2-yl]acetamide]), characterized in vitro as CB1 antagonists with high CB1 over CB2 selectivity, in the mouse GI tract...
February 5, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/29402275/acute-administration-of-beta-caryophyllene-prevents-endocannabinoid-system-activation-during-transient-common-carotid-artery-occlusion-and-reperfusion
#16
Laura Poddighe, Gianfranca Carta, Maria Pina Serra, Tiziana Melis, Marianna Boi, Sara Lisai, Elisabetta Murru, Laura Muredda, Maria Collu, Sebastiano Banni, Marina Quartu
BACKGROUND: The transient global cerebral hypoperfusion/reperfusion achieved by induction of Bilateral Common Carotid Artery Occlusion followed by Reperfusion (BCCAO/R) has been shown to stimulate early molecular changes that can be easily traced in brain tissue and plasma, and that are indicative of the tissue physiological response to the reperfusion-induced oxidative stress and inflammation. The aim of the present study is to probe the possibility to prevent the molecular changes induced by the BCCAO/R with dietary natural compounds known to possess anti-inflammatory activity, such as the phytocannabinoid beta-caryophyllene (BCP)...
February 5, 2018: Lipids in Health and Disease
https://www.readbyqxmd.com/read/29400965/structure-activity-relationships-and-computational-investigations-into-the-development-of-potent-and-balanced-dual-acting-butyrylcholinesterase-inhibitors-and-human-cannabinoid-receptor-2-ligands-with-pro-cognitive-in-vivo-profiles
#17
Dominik Dolles, Matthias Hoffmann, Sandra Gunesch, Oliviero Marinelli, Jan Möller, Giorgio Santoni, Arnaud Chatonnet, Martin J Lohse, Hans-Joachim Wittmann, Andrea Strasser, Massimo Nabissi, Tangui Maurice, Michael Decker
The enzyme butyrylcholinesterase (BChE) and the human cannabinoid receptor 2 (hCB2R) represent promising targets for pharmacotherapy in the later stages of Alzheimer's disease. We merged pharmacophores for both targets into small benzimidazole-based molecules, investigated SARs, and identified several dual-acting ligands with a balanced affinity/inhibitory activity and an excellent selectivity over both hCB1R and hAChE. A homology model for the hCB2R was developed based on the hCB1R crystal structure and used for molecular dynamics studies to investigate binding modes...
February 5, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29390896/targeting-the-endocannabinoid-system-as-a-potential-anticancer-approach
#18
Rico Schwarz, Robert Ramer, Burkhard Hinz
The endocannabinoid system is currently under intense investigation due to the therapeutic potential of cannabinoid-based drugs as treatment options for a broad variety of diseases including cancer. Besides the canonical endocannabinoid system that includes the cannabinoid receptors CB1 and CB2 and the endocannabinoids N-arachidonoylethanolamine (anandamide) and 2-arachidonoylglycerol, recent investigations suggest that other fatty acid derivatives, receptors, enzymes, and lipid transporters likewise orchestrate this system as components of the endocannabinoid system when defined as an extended signaling network...
February 1, 2018: Drug Metabolism Reviews
https://www.readbyqxmd.com/read/29385102/preventive-effects-of-resveratrol-on-endocannabinoid-system-and-synaptic-protein-modifications-in-rat-cerebral-cortex-challenged-by-bilateral-common-carotid-artery-occlusion-and-reperfusion
#19
Gianfranca Carta, Laura Poddighe, Maria Pina Serra, Marianna Boi, Tiziana Melis, Sara Lisai, Elisabetta Murru, Laura Muredda, Maria Collu, Sebastiano Banni, Marina Quartu
This study aims to evaluate the putative roles of a single acute dose of resveratrol (RVT) in preventing cerebral oxidative stress induced by bilateral common carotid artery occlusion, followed by reperfusion (BCCAO/R) and to investigate RVT's ability to preserve the neuronal structural integrity. Frontal and temporal-occipital cortices were examined in two groups of adult Wistar rats, sham-operated and submitted to BCCAO/R. In both groups, 6 h before surgery, half the rats were gavage-fed with a single dose of RVT (40 mg/per rat in 300 µL of sunflower oil as the vehicle), while the second half received the vehicle alone...
January 31, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29367862/evaluation-of-carboxamide-type-synthetic-cannabinoids-as-cb1-cb2-receptor-agonists-difference-between-the-enantiomers
#20
Takahiro Doi, Takaomi Tagami, Akihiro Takeda, Akiko Asada, Yoshiyuki Sawabe
Recently, carboxamide-type synthetic cannabinoids have been distributed globally as new psychoactive substances (NPS). Some of these compounds possess asymmetric carbon, which is derived from an amide moiety composed of amino acid derivatives (i.e., amides or esters of amino acids). In this study, we synthesized both enantiomers of synthetic cannabinoids, N-(1-amino-3-methyl-1-oxobutan-2-yl)-1-(2-fluorobenzyl)-1H-indazole-3-carboxamide (AB-FUBINACA 2-fluorobenzyl isomer), N-(1-amino-1-oxo-3-phenylpropan-2-yl)-1-(cyclohexylmethyl)-1H-indazole-3-carboxamide (APP-CHMINACA), ethyl [1-(5-fluoropentyl)-1H-indazole-3-carbonyl]valinate (5F-EMB-PINACA), ethyl [1-(4-fluorobenzyl)-1H-indazole-3-carbonyl]valinate (EMB-FUBINACA), and methyl 2-[1-(4-fluorobenzyl)-1H-indole-3-carboxamido]-3,3-dimethylbutanoate (MDMB-FUBICA), which were reported as NPS found in Europe from 2014 to 2015, to evaluate their activities as CB1/CB2 receptor agonists...
2018: Forensic Toxicology
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