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https://www.readbyqxmd.com/read/28240187/the-endocannabinoid-system-modulating-levels-of-consciousness-emotions-and-likely-dream-contents
#1
Eric Murillo-Rodriguez, José Carlos Pastrana-Trejo, Mireille Salas-Crisóstomo, Miriel de-la-Cruz
Cannabinoids are derivatives that are either compounds occurring naturally in the plant, Cannabis sativa or synthetic analogs of these molecules. The first and most widely investigated of the cannabinoids is ∆9-tetrahydrocannabinol (Δ9-THC), which is the main psychotropic constituent of cannabis and undergoes significant binding to cannabinoid receptors. These cannabinoid receptors are seven-transmembrane receptors that received their name from the fact that they respond to cannabinoid compounds, including Δ9-THC...
February 23, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28131783/antihyperalgesic-effect-of-cb1-receptor-activation-involves-the-modulation-of-p2x3-receptor-in-the-primary-afferent-neuron
#2
Maria Cláudia Gonçalves Oliveira-Fusaro, Cristiane Isabel Silva Zanoni, Gilson Gonçalves Dos Santos, Luis Paulo Manzo, Dionéia Araldi, Ivan José Magayewski Bonet, Cláudia Herrera Tambeli, Elayne Vieira Dias, Carlos Amilcar Parada
Cannabinoid system is a potential target for pain control. Cannabinoid receptor 1 (CB1) activation play a role in the analgesic effect of cannabinoids once it is expressed in primary afferent neurons. This study investigates whether the anti-hyperalgesic effect of CB1 receptor activation involves P2X3 receptor in primary afferent neurons. Mechanical hyperalgesia was evaluated by electronic von Frey test. Cannabinoid effect was evaluated using anandamide or ACEA, a non-selective or a selective CB1 receptor agonists, respectively; AM251, a CB1 receptor antagonist, and antisense ODN for CB1 receptor...
January 25, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28107590/endocannabinoid-activation-of-cb1-receptors-contributes-to-long-lasting-reversal-of-neuropathic-pain-by-repetitive-spinal-cord-stimulation
#3
L Sun, L Tai, Q Qiu, R Mitchell, S Fleetwood-Walker, E A Joosten, C W Cheung
BACKGROUND: Spinal cord stimulation (SCS) has been shown to be effective in the management of certain neuropathic pain conditions, however, the underlying mechanisms are incompletely understood. In this study, we investigated repetitive SCS in a rodent neuropathic pain model, revealing long-lasting and incremental attenuation of hyperalgesia and a mechanism of action involving endocannabinoids. METHOD: Animals were implanted with monopolar electrodes at the time of partial sciatic nerve injury...
January 20, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28100744/compensatory-activation-of-cannabinoid-cb2-receptor-inhibition-of-gaba-release-in-the-rostral-ventromedial-medulla-in-inflammatory-pain
#4
Ming-Hua Li, Katherine L Suchland, Susan L Ingram
The rostral ventromedial medulla (RVM) is a relay in the descending pain modulatory system and an important site of endocannabinoid modulation of pain. Endocannabinoids inhibit GABA release in the RVM, but it is not known whether this effect persists in chronic pain states. In the present studies, persistent inflammation induced by complete Freund's adjuvant (CFA) increased GABAergic miniature IPSCs (mIPSCs). Endocannabinoid activation of cannabinoid (CB1) receptors known to inhibit presynaptic GABA release was significantly reduced in the RVM of CFA-treated rats compared with naive rats...
January 18, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28010996/pharmacological-characterization-of-rat-vd-hemopressin-%C3%AE-an-%C3%AE-hemoglobin-derived-peptide-exhibiting-cannabinoid-agonist-like-effects-in-mice
#5
Ting Zheng, Ting Zhang, Run Zhang, Zi-Long Wang, Zheng-Lan Han, Ning Li, Xu-Hui Li, Meng-Na Zhang, Biao Xu, Xiong-Li Yang, Quan Fang, Rui Wang
Hemopressin and related peptides have shown to function as the endogenous ligands or the regulator of cannabinoid receptors. Moreover, hemopressin and its truncated peptides were also reported to produce a slight modulatory effect on opioid system. In the present work, based on the amino acid sequence analyses of hemoglobin subunit α, rat VD-hemopressin(α) [(r)VD-Hpα] was predicted as a cannabinoid peptide derived from rat α-hemoglobin. Furthermore, (r)VD-Hpα was synthesized and characterized in a series of in vitro and in vivo assays...
December 16, 2016: Neuropeptides
https://www.readbyqxmd.com/read/27997038/inflammation-of-peripheral-tissues-and-injury-to-peripheral-nerves-induce-diferring-effects-in-the-expression-of-the-calcium-sensitive-anandamide-synthesising-enzyme-and-related-molecules-in-rat-primary-sensory-neurons
#6
João Sousa-Valente, Angelika Varga, Jose Vicente Torres Perez, Agnes Jenes, John Wahba, Ken Mackie, Benjamin Cravatt, Natsuo Ueda, Kazuhito Tsuboi, Peter Santha, Gabor Jancso, Hiren Tailor, António Avelino, Istvan Nagy
Elevation of intracellular Ca(2+) concentration induces the synthesis of N-arachydonoylethanolamine (anandamide) in a sub-population of primary sensory neurons. N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) is the only known enzyme, which synthesises anandamide in a Ca(2+) -dependent manner. NAPE-PLD mRNA, as well as anandamide's main targets, the excitatory transient receptor potential vanilloid type 1 ion channel (TRPV1) and the inhibitory cannabinoid type 1 (CB1) receptor and the main anandamide-hydrolysing enzyme fatty acid amide hydrolase (FAAH) are all expressed by sub-populations of nociceptive primary sensory neurons...
December 20, 2016: Journal of Comparative Neurology
https://www.readbyqxmd.com/read/27941994/deletion-of-gpr55-results-in-subtle-effects-on-energy-metabolism-motor-activity-and-thermal-pain-sensation
#7
Mikael Bjursell, Erik Ryberg, Tingting Wu, Peter J Greasley, Mohammad Bohlooly-Y, Stephan Hjorth
The G-protein coupled receptor 55 (GPR55) is activated by cannabinoids and non-cannabinoid molecules and has been speculated to play a modulatory role in a large variety of physiological and pathological processes, including in metabolically perturbed states. We therefore generated male mice deficient in the gene coding for the cannabinoid/lysophosphatidylinositol (LPI) receptor Gpr55 and characterized them under normal dietary conditions as well as during high energy dense diet feeding followed by challenge with the CB1 receptor antagonist/GPR55 agonist rimonabant...
2016: PloS One
https://www.readbyqxmd.com/read/27940994/compensatory-activation-of-cannabinoid-cb2-receptor-inhibition-of-gaba-release-in-the-rostral-ventromedial-medulla-rvm-in-inflammatory-pain
#8
Ming-Hua Li, Katherine L Suchland, Susan L Ingram
The rostral ventromedial medulla (RVM) is a relay in the descending pain modulatory system and an important site of endocannabinoid modulation of pain. Endocannabinoids inhibit GABA release in the RVM but it is not known if this effect persists in chronic pain states. In the present studies, persistent inflammation induced by complete Freund's adjuvant (CFA) increased GABAergic miniature inhibitory postsynaptic currents (mIPSCs). Endocannabinoid activation of cannabinoid (CB1) receptors known to inhibit presynaptic GABA release was significantly reduced in the RVM of CFA-treated rats compared to naïve rats...
December 9, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27906750/role-of-orexin-2-and-cb1-receptors-within-the-periaqueductal-gray-matter-in-lateral-hypothalamic-induced-antinociception-in-rats
#9
Mohammad-Hossein Esmaeili, Zahra Reisi, Somayeh Ezzatpanah, Abbas Haghparast
Orexin plays an important role in pain modulation. Orexin-1 and orexin-2 receptors (Ox1r and Ox2r) are found at high density in the ventrolateral periaqueductal gray matter (vlPAG). Our previous study showed that chemical stimulation of the lateral hypothalamus with carbachol induces antinociception in the tail-flick test, a model of acute pain, and Ox1r-mediated antinociception in the vlPAG is modulated by the activity of vlPAG CB1 receptors. In the current study, TCS OX2 29, an Ox2r antagonist (5, 15, 50, 150, and 500 nmol/l), was microinjected into the vlPAG 5 min before the administration of carbachol (125 nmol/l)...
November 30, 2016: Behavioural Pharmacology
https://www.readbyqxmd.com/read/27851727/high-resolution-crystal-structure-of-the-human-cb1-cannabinoid-receptor
#10
Zhenhua Shao, Jie Yin, Karen Chapman, Magdalena Grzemska, Lindsay Clark, Junmei Wang, Daniel M Rosenbaum
The human cannabinoid G-protein-coupled receptors (GPCRs) CB1 and CB2 mediate the functional responses to the endocannabinoids anandamide and 2-arachidonyl glycerol (2-AG), as well as the widely consumed plant (phyto)cannabinoid Δ(9)-tetrahydrocannabinol (THC)(1). The cannabinoid receptors have been the targets of intensive drug discovery efforts owing to the therapeutic potential of modulators for controlling pain(2), epilepsy(3), obesity(4), and other maladies. Although much progress has recently been made in understanding the biophysical properties of GPCRs, investigations of the molecular mechanisms of the cannabinoids and their receptors have lacked high-resolution structural data...
November 16, 2016: Nature
https://www.readbyqxmd.com/read/27835801/cannabinoid-receptor-ligand-bias-implications-in-the-central-nervous-system
#11
REVIEW
Robert B Laprairie, Amina M Bagher, Eileen M Denovan-Wright
The G protein-coupled cannabinoid receptors CB1, CB2, GPR18, and GPR55 regulate neurotransmission, pain, and inflammation and have been intensively investigated as potential drug targets. Each of these GPCRs is coupled to multiple effector proteins mediating divergent cellular signals. The ligand bias of cannabinoid-targeted compounds is only beginning to be quantified. Research into cannabinoid bias is now revealing correlations between bias in cell culture and functional outcomes in vivo. We present an example study of cannabinoid bias in the context of Huntington disease...
November 8, 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27812328/adverse-social-experiences-in-adolescent-rats-result-in-enduring-effects-on-social-competence-pain-sensitivity-and-endocannabinoid-signaling
#12
Peggy Schneider, Laura Bindila, Christian Schmahl, Martin Bohus, Andreas Meyer-Lindenberg, Beat Lutz, Rainer Spanagel, Miriam Schneider
Social affiliation is essential for many species and gains significant importance during adolescence. Disturbances in social affiliation, in particular social rejection experiences during adolescence, affect an individual's well-being and are involved in the emergence of psychiatric disorders. The underlying mechanisms are still unknown, partly because of a lack of valid animal models. By using a novel animal model for social peer-rejection, which compromises adolescent rats in their ability to appropriately engage in playful activities, here we report on persistent impairments in social behavior and dysregulations in the endocannabinoid (eCB) system...
2016: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/27773824/prophylactic-treatment-with-the-tricyclic-antidepressant-desipramine-prevents-development-of-paclitaxel-induced-neuropathic-pain-through-activation-of-endogenous-analgesic-systems
#13
Liting Deng, Wan-Hung Lee, Zhili Xu, Alexandros Makriyannis, Andrea G Hohmann
Neuropathic pain impacts approximately 3-4.5% of the global population and remains an unresolved health problem. The management of neuropathic pain has two distinct goals-prevention of development and control of established neuropathic pain. We examined the impact of both prophylactic and therapeutic treatments with the tricyclic antidepressant desipramine on the development and maintenance of toxic neuropathic pain induced by the chemotherapeutic agent paclitaxel. We also investigated the involvement of endogenous analgesic (i...
December 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27768894/crystal-structure-of-the-human-cannabinoid-receptor-cb1
#14
Tian Hua, Kiran Vemuri, Mengchen Pu, Lu Qu, Gye Won Han, Yiran Wu, Suwen Zhao, Wenqing Shui, Shanshan Li, Anisha Korde, Robert B Laprairie, Edward L Stahl, Jo-Hao Ho, Nikolai Zvonok, Han Zhou, Irina Kufareva, Beili Wu, Qiang Zhao, Michael A Hanson, Laura M Bohn, Alexandros Makriyannis, Raymond C Stevens, Zhi-Jie Liu
Cannabinoid receptor 1 (CB1) is the principal target of Δ(9)-tetrahydrocannabinol (THC), a psychoactive chemical from Cannabis sativa with a wide range of therapeutic applications and a long history of recreational use. CB1 is activated by endocannabinoids and is a promising therapeutic target for pain management, inflammation, obesity, and substance abuse disorders. Here, we present the 2.8 Å crystal structure of human CB1 in complex with AM6538, a stabilizing antagonist, synthesized and characterized for this structural study...
October 20, 2016: Cell
https://www.readbyqxmd.com/read/27766867/therapeutic-potential-of-fatty-acid-amide-hydrolase-monoacylglycerol-lipase-and-n-acylethanolamine-acid-amidase-inhibitors
#15
Wei Tuo, Natascha Leleu-Chavain, John Spencer, Supojjanee Sansook, Regis Millet, Philippe Chavatte
Fatty acid ethanolamides (FAEs) and endocannabinoids (ECs) have been shown to alleviate pain and inflammation, regulate motility and appetite, and produce anti-cancer, anxiolytic, and neuroprotective efficacies via cannabinoid receptor type 1 (CB1) or type 2 (CB2), or via peroxisome proliferator-activated receptor α (PPAR-α) stimulation. FAEs and ECs are synthesized by a series of endogenous enzymes, including N-acylphosphatidylethanolamine-phospholipase D (NAPE-PLD), diacylglycerol lipase (DAGL), or phospholipase C (PLC), and their metabolism is mediated by several metabolic enzymes, including fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL), N-acylethanolamine acid amidase (NAAA), or cyclooxygenase-2 (COX-2)...
October 21, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27696789/%C3%AE-caryophyllene-and-%C3%AE-caryophyllene-oxide-natural-compounds-of-anticancer-and-analgesic-properties
#16
Klaudyna Fidyt, Anna Fiedorowicz, Leon Strządała, Antoni Szumny
Natural bicyclic sesquiterpenes, β-caryophyllene (BCP) and β-caryophyllene oxide (BCPO), are present in a large number of plants worldwide. Both BCP and BCPO (BCP(O)) possess significant anticancer activities, affecting growth and proliferation of numerous cancer cells. Nevertheless, their antineoplastic effects have hardly been investigated in vivo. In addition, both compounds potentiate the classical drug efficacy by augmenting their concentrations inside the cells. The mechanisms underlying the anticancer activities of these sesquiterpenes are poorly described...
September 30, 2016: Cancer Medicine
https://www.readbyqxmd.com/read/27649266/n-palmitoylethanolamide-in-the-anterior-cingulate-cortex-attenuates-inflammatory-pain-behaviour-indirectly-via-a-cb1-receptor-mediated-mechanism
#17
Bright N Okine, Manish K Madasu, Fiona McGowan, Charles Prendergast, Jessica C Gaspar, Brendan Harhen, Michelle Roche, David P Finn
The neural substrates and mechanisms mediating the antinociceptive effects of the endogenous bioactive lipid, N-palmitoylethanolamide (PEA), require further investigation. We investigated the effects of exogenous PEA administration into the anterior cingulate cortex (ACC), an important brain region linked with cognitive and affective modulation of pain, on formalin-evoked nociceptive behaviour in rats. Potential involvement of peroxisome proliferator-activated receptor isoforms (PPAR) α and γ or endocannabinoid-mediated entourage effects at cannabinoid1 (CB1) receptors or transient receptor potential subfamily V member 1 (TRPV1) in mediating the effects of PEA was also investigated...
December 2016: Pain
https://www.readbyqxmd.com/read/27624384/high-intensity-swimming-exercise-decreases-glutamate-induced-nociception-by-activation-of-g-protein-coupled-receptors-inhibiting-phosphorylated-protein-kinase-a
#18
Daniel F Martins, Aline Siteneski, Daniela D Ludtke, Daniela Dal-Secco, Adair R S Santos
Several studies in humans have reported that improved pain control is associated with exercise in a variety of painful conditions, including osteoarthritis, fibromyalgia, and neuropathic pain. Despite the growing amount of experimental data on physical exercise and nociception, the precise mechanisms through which high-intensity exercise reduces pain remain elusive. Since the glutamatergic system plays a major role in pain transmission, we firstly analyzed if physical exercise could be able to decrease glutamate-induced nociception through G-protein-coupled receptor (G-PCR) activation...
September 13, 2016: Molecular Neurobiology
https://www.readbyqxmd.com/read/27600019/-progress-in-study-on-endocannabinoids-and-cannabinoid-receptors-in-the-treatment-for-neuropathic-pain
#19
Peng Liu, Wei Zhang, Shaobo Zhang, Yibao Zhang, Jing Wang
Endocannabinoids and cannabinoid receptors are expressed in various central pain modulation regions. They maintain in dynamic changes in the expression level and distribution under different pathological and physiological conditions. These changes possess advantage as well as disadvantage. Exogenous administration of endocannabinoids exerts analgesic effect in different pain models, which is mainly mediated by the cannabinoid CB1 and CB2 receptors. Inhibition of enzymes for degrading endocannabinoids in different pain models also shows analgesic effect due to the increased local levels of endocannabinoids...
August 2016: Zhong Nan da Xue Xue Bao. Yi Xue Ban, Journal of Central South University. Medical Sciences
https://www.readbyqxmd.com/read/27589093/activation-of-cannabinoid-cb1-receptor-contributes-to-suppression-of-spinal-nociceptive-transmission-and-inhibition-of-mechanical-hypersensitivity-by-a%C3%AE-fiber-stimulation
#20
Fei Yang, Qian Xu, Bin Shu, Vinod Tiwari, Shao-Qiu He, Louis P Vera-Portocarrero, Xinzhong Dong, Bengt Linderoth, Srinivasa N Raja, Yun Wang, Yun Guan
Activation of Aβ-fibers is an intrinsic feature of spinal cord stimulation (SCS) pain therapy. Cannabinoid receptor type 1 (CB1) is important to neuronal plasticity and pain modulation, but its role in SCS-induced pain inhibition remains unclear. In this study, we showed that CB1 receptors are expressed in both excitatory and inhibitory interneurons in substantia gelatinosa (SG). Patch-clamp recording of the evoked excitatory postsynaptic currents (eEPSCs) in mice after spinal nerve ligation (SNL) showed that electrical stimulation of Aβ-fibers (Aβ-ES) using clinical SCS-like parameters (50 Hz, 0...
November 2016: Pain
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