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https://www.readbyqxmd.com/read/29910713/the-endocannabinoid-reuptake-inhibitor-wobe437-is-orally-bioavailable-and-exerts-indirect-polypharmacological-effects-via-different-endocannabinoid-receptors
#1
Inés Reynoso-Moreno, Andrea Chicca, Mario E Flores-Soto, Juan M Viveros-Paredes, Jürg Gertsch
Different anandamide (AEA) transport inhibitors show antinociceptive and antiinflammatory effects in vivo , but due to their concomitant inhibition of fatty acid amide hydrolase (FAAH) and overall poor bioavailability, they cannot be used unequivocally to study the particular role of endocannabinoid (EC) transport in pathophysiological conditions in vivo . Here, the potent and selective endocannabinoid reuptake inhibitor WOBE437, which inhibits AEA and 2-arachidonoylglycerol (2-AG) transport, was tested for its oral bioavailability to the brain...
2018: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29885522/cannabinoid-receptor-type-1-in-the-brain-regulates-the-affective-component-of-visceral-pain-in-mice
#2
Danica Bajic, Krisztina Monory, Andrea Conrad, Christina Maul, Roland M Schmid, Carsten T Wotjak, Christoph K Stein-Thoeringer
Endocannabinoids acting through cannabinoid receptor type 1 (CB1) are major modulators of peripheral somatic and visceral nociception. Although only partially studied, some evidence suggests a particular role of CB1 within the brain in nociceptive processes. As the endocannabinoid system regulates affect and emotional behaviors, we hypothesized that cerebral CB1 influences affective processing of visceral pain-related behaviors in laboratory animals. To study nocifensive responses modulated by supraspinal CB1, we used conditional knock-out mice lacking CB1 either in cortical glutamatergic neurons (Glu-CB1-KO), or in forebrain GABAergic neurons (GABA-CB1-KO), or in principle neurons of the forebrain (CaMK-CB1-KO)...
June 6, 2018: Neuroscience
https://www.readbyqxmd.com/read/29882158/localization-of-cannabinoid-receptors-cb1-cb2-gpr55-and-ppar%C3%AE-in-the-canine-gastrointestinal-tract
#3
Giorgia Galiazzo, Fiorella Giancola, Agnese Stanzani, Federico Fracassi, Chiara Bernardini, Monica Forni, Marco Pietra, Roberto Chiocchetti
The endocannabinoid system (ECS) is composed of cannabinoid receptors, their endogenous ligands, and the enzymes involved in endocannabinoid turnover. Modulating the activity of the ECS may influence a variety of physiological and pathophysiological processes. A growing body of evidence indicates that activation of cannabinoid receptors by endogenous, plant-derived, or synthetic cannabinoids may exert beneficial effects on gastrointestinal inflammation and visceral pain. The present ex vivo study aimed to investigate immunohistochemically the distribution of cannabinoid receptors CB1, CB2, G protein-coupled receptor 55 (GPR55), and peroxisome proliferation activation receptor alpha (PPARα) in the canine gastrointestinal tract...
June 7, 2018: Histochemistry and Cell Biology
https://www.readbyqxmd.com/read/29847859/the-prefrontal-cortical-endocannabinoid-system-modulates-fear-pain-interactions-in-a-subregion-specific-manner
#4
Kieran Rea, Fiona McGowan, Louise Corcoran, Michelle Roche, David P Finn
BACKGROUND AND PURPOSE: The emotional processing and coordination of top-down responses to noxious and conditioned aversive stimuli involves the medial prefrontal cortex (mPFC). Evidence suggests that subregions of the mPFC, (infralimbic (IL), prelimbic (PrL), anterior cingulate (ACC) cortices), differentially alter the expression of contextually-induced fear and nociceptive behaviour. We investigated the role of the endocannabinoid system in the IL, PrL and ACC in formalin-evoked nociceptive behaviour, fear-conditioned analgesia (FCA) and conditioned fear in the presence of nociceptive tone...
May 30, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29781960/a-peripherally-restricted-cannabinoid-1-receptor-agonist-as-a-novel-analgesic-in-cancer-induced-bone-pain
#5
Hong Zhang, Dominique M Lund, Haley A Ciccone, William D Staatz, Mohab M Ibrahim, Tally M Largent-Milnes, Herbert H Seltzman, Igor Spigelman, Todd W Vanderah
Many malignant cancers, including breast cancer, have a propensity to invade bones, leading to excruciating bone pain. Opioids are the primary analgesics used to alleviate this cancer-induced bone pain (CIBP) but are associated with numerous severe side effects, including enhanced bone degradation, which significantly impairs patients' quality of life. In contrast, agonists activating only peripheral CB1 receptors (CB1Rs) have been shown to effectively alleviate multiple chronic pain conditions with limited side effects, yet no studies have evaluated their role(s) in CIBP...
May 16, 2018: Pain
https://www.readbyqxmd.com/read/29751000/2-arachidonoylglycerol-a-signaling-lipid-with-manifold-actions-in-the-brain
#6
REVIEW
Marc P Baggelaar, Mauro Maccarrone, Mario van der Stelt
2-Arachidonoylglycerol (2-AG) is a signaling lipid in the central nervous system that is a key regulator of neurotransmitter release. 2-AG is an endocannabinoid that activates the cannabinoid CB1 receptor. It is involved in a wide array of (patho)physiological functions, such as emotion, cognition, energy balance, pain sensation and neuroinflammation. In this review, we describe the biosynthetic and metabolic pathways of 2-AG and how chemical and genetic perturbation of these pathways has led to insight in the biological role of this signaling lipid...
May 8, 2018: Progress in Lipid Research
https://www.readbyqxmd.com/read/29740328/emerging-role-of-endo-cannabinoids-in-migraine
#7
REVIEW
Pinja Leimuranta, Leonard Khiroug, Rashid Giniatullin
In this mini-review, we summarize recent discoveries and present new hypotheses on the role of cannabinoids in controlling trigeminal nociceptive system underlying migraine pain. Individual sections of this review cover key aspects of this topic, such as: (i) the current knowledge on the endocannabinoid system (ECS) with emphasis on expression of its components in migraine related structures; (ii) distinguishing peripheral from central site of action of cannabinoids, (iii) proposed mechanisms of migraine pain and control of nociceptive traffic by cannabinoids at the level of meninges and in brainstem, (iv) therapeutic targeting in migraine of monoacylglycerol lipase and fatty acid amide hydrolase, enzymes which control the level of endocannabinoids; (v) dual (possibly opposing) actions of cannabinoids via anti-nociceptive CB1 and CB2 and pro-nociceptive TRPV1 receptors...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29681797/electroacupuncture-potentiates-cannabinoid-receptor-mediated-descending-inhibitory-control-in-a-mouse-model-of-knee-osteoarthritis
#8
Xiao-Cui Yuan, Bing Zhu, Xiang-Hong Jing, Li-Ze Xiong, Cai-Hua Wu, Fang Gao, Hong-Ping Li, Hong-Chun Xiang, He Zhu, Bin Zhou, Wei He, Chuan-You Lin, Hui-Lin Pan, Qiang Wang, Man Li
Knee osteoarthritis (KOA) is a highly prevalent, chronic joint disorder, which can lead to chronic pain. Although electroacupuncture (EA) is effective in relieving chronic pain in the clinic, the involved mechanisms remain unclear. Reduced diffuse noxius inhibitory controls (DNIC) function is associated with chronic pain and may be related to the action of endocannabinoids. In the present study, we determined whether EA may potentiate cannabinoid receptor-mediated descending inhibitory control and inhibit chronic pain in a mouse model of KOA...
2018: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29626639/assessing-the-real-time-activation-of-the-cannabinoid-cb1-receptor-and-the-associated-structural-changes-using-a-fret-biosensor
#9
Ying Liu, Lu-Yao Chen, Hong Zeng, Richard Ward, Nan Wu, Li Ma, Xi Mu, Qiu-Lan Li, Yang Yang, Su An, Xiao-Xi Guo, Qian Hao, Tian-Rui Xu
The cannabinoid receptor 1 (CB1) is mainly expressed in the nervous system and regulates learning, memory processes, pain and energy metabolism. However, there is no way to directly measure its activation. In this study, we constructed a CB1 intramolecular fluorescence resonance energy transfer (FRET) sensor, which could measure CB1 activation by monitoring structural changes between the third intracellular loop and the C-terminal tail. CB1 agonists induced a time- and concentration-dependent increase in the FRET signal, corresponding to a reduction in the distance between the third intracellular loop and the C-terminal tail...
June 2018: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/29546501/cannabinoid-receptors-mental-pain-and-suicidal-behavior-a-systematic-review
#10
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
#11
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
#12
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 (ie, pain-stimulated behavior), which presents a challenge to distinguish between motor impairing and antinociceptive effects of drugs. Here, we demonstrate that chronic constriction injury (CCI) of the sciatic nerve elicits common pain-stimulated responses (ie, 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 1 week...
June 2018: Pain
https://www.readbyqxmd.com/read/29482740/cannabinoids-and-cancer-pain-a-new-hope-or-a-false-dawn
#13
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/29425797/antinociceptive-effects-of-the-endogenous-cannabinoid-peptide-agonist-vd-hemopressin-%C3%AE-in-mice
#14
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
#15
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/29364174/molecular-understanding-of-the-activation-of-cb1-and-blockade-of-trpv1-receptors-implications-for-novel-treatment-strategies-in-osteoarthritis
#16
Jakub Mlost, Magdalena Kostrzewa, Natalia Malek, Katarzyna Starowicz
Osteoarthritis (OA) is a joint disease in which cartilage degenerates as a result of mechanical and biochemical changes. The main OA symptom is chronic pain involving both peripheral and central mechanisms of nociceptive processing. Our previous studies have implicated the benefits of dual- over single-acting compounds interacting with the endocannabinoid system (ECS) in OA treatment. In the present study, we focused on the specific molecular alterations associated with pharmacological treatment. OA was induced in Wistar rats by intra-articular injection of 3 mg of monoiodoacetate (MIA)...
January 24, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29355030/allosteric-modulators-of-cannabinoid-receptor-1-developing-compounds-for-improved-specificity
#17
Rachel Dopart, Dai Lu, Aron H Lichtman, Debra A Kendall
The cannabinoid receptor 1 (CB1 ) is a G protein-coupled receptor (GPCR) that is located primarily in the central nervous system. CB1 is a therapeutic target which may impact pathways to mediate pain, neurodegenerative disorders, hunger, and drug-seeking behavior. Despite these benefits, development of orthosteric therapeutic compounds, which target the endogenous ligand-binding site of CB1 , has been challenging due to detrimental side effects including psychoactivity, depression, and suicidal thoughts. However, CB1 also has an allosteric binding site(s), which is topographically distinct from the orthosteric site...
February 2018: Drug Metabolism Reviews
https://www.readbyqxmd.com/read/29340966/cannabinomimetric-lipids-from-natural-extract-to-artificial-synthesis
#18
REVIEW
Ya-Ru Gao, Yong-Qiang Wang
Endocannabinoid system is related with various physiological and cognitive processes including fertility, pregnancy, during pre- and postnatal development, pain-sensation, mood, appetite, and memory. In the latest decades, an important milestone concerning the endocannabinoid system was the discovery of the existence of the cannabinoid receptors CB1 and CB2. Anandamide was the first reported endogenous metabolite, which adjusted the release of some neurotransmitters through binding to the CB1 or CB2 receptors...
January 16, 2018: Natural Products and Bioprospecting
https://www.readbyqxmd.com/read/29314831/a-fluorescent-probe-to-unravel-functional-features-of-cannabinoid-receptor-cb-1-in-human-blood-and-tonsil-immune-system-cells
#19
Mar Martín-Fontecha, Alba Angelina, Beate Rückert, Ainoa Rueda-Zubiaurre, Leticia Martín-Cruz, Willem van de Veen, Mübeccel Akdis, Silvia Ortega-Gutiérrez, María Luz López-Rodríguez, Cezmi A Akdis, Oscar Palomares
The human endogenous cannabinoid system (ECS) regulates key physiological processes and alterations in its signaling pathways, and endocannabinoid levels are associated with diseases such as neurological and neuropsychiatric conditions, cancer, pain and inflammation, obesity, and metabolic and different immune related disorders. Immune system cells express the G-protein coupled cannabinoid receptor 1 (CB1 ), but its functional role has not been fully understood, likely due to the lack of appropriate tools. The availability of novel tools to investigate the role of CB1 in immune regulation might contribute to identify CB1 as a potential novel therapeutic target or biomarker for many diseases...
February 21, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29274880/cb-1-cannabinoid-receptor-agonist-mouse-vd-hemopressin-%C3%AE-produced-supraspinal-analgesic-activity-in-the-preclinical-models-of-pain
#20
Ting Zheng, Run Zhang, Ting Zhang, Meng-Na Zhang, Biao Xu, Jing-Jing Song, Ning Li, Hong-Hai Tang, Pei Wang, Rui Wang, Quan Fang
Mouse VD-hemopressin(α) (VD-Hpα) is an undecapeptide that selectively activates CB1 cannabinoid receptor in in vitro functional tests, and exerts CB1 -mediated central antinociception in the mouse tail-flick assay. The aim of the present study was to further investigate the analgesic properties of supraspinal mouse VD-Hpα in a range of preclinical pain models. Our results indicated that the classical cannabinoid agonist WIN 55,212-2 produced supraspinal analgesia in preclinical pain models, which was selectively antagonized by the CB1 antagonist/inverse agonist AM251, but not by the CB2 antagonist AM630...
February 1, 2018: Brain Research
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