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Cannabinoid receptors

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https://www.readbyqxmd.com/read/29350472/the-chemistry-and-pharmacology-of-synthetic-cannabinoid-sdb-006-and-its-regioisomeric-fluorinated-and-methoxylated-analogues
#1
Samuel D Banister, Alexander Olson, Matthew Winchester, Jordyn Stuart, Amelia R Edington, Richard C Kevin, Mitchell Longworth, Marco Herrera, Mark Connor, Iain S McGregor, Roy R Gerona, Michael Kassiou
Synthetic cannabinoids are the largest and most structurally diverse class of new psychoactive substances, with manufacturers often using isomerism to evade detection and circumvent legal restriction. The regioisomeric methoxy- and fluorine-substituted analogues of SDB-006 (N-benzyl-1-pentyl-1H-indole-3-carboxamide) were synthesized and could not be differentiated by gas chromatography-mass spectrometry (GC-MS), but were distinguishable by liquid chromatography-quadrupole time-of-flight-MS (LC-QTOF-MS). In a fluorescence-based plate reader membrane potential assay, SDB-006 acted as a potent agonist at human cannabinoid receptors (CB1 EC50 = 19 nM)...
January 19, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29349551/medical-marijuana-current-concepts-pharmacological-actions-of-cannabinoid-receptor-mediated-activation-and-societal-implications
#2
REVIEW
Nalini Vadivelu, Alice M Kai, Gopal Kodumudi, Julie Sramcik, Alan D Kaye
PURPOSE OF REVIEW: The purpose of the following review is to summarize the history and current policies related to marijuana use and prevalence, basic and clinical science pharmacological literature regarding efficacy, subpopulations of concern, and varying policies regarding its use at present. RECENT FINDINGS: With the increasingly widespread utilization of marijuana, there is also a growing complexity of public health policy, regulation, and necessity to further assess the medical indications and adverse long-term effects of marijuana use...
January 18, 2018: Current Pain and Headache Reports
https://www.readbyqxmd.com/read/29340966/cannabinomimetric-lipids-from-natural-extract-to-artificial-synthesis
#3
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/29338785/benefits-of-vce-003-2-a-cannabigerol-quinone-derivative-against-inflammation-driven-neuronal-deterioration-in-experimental-parkinson-s-disease-possible-involvement-of-different-binding-sites-at-the-ppar%C3%AE-receptor
#4
Concepción García, María Gómez-Cañas, Sonia Burgaz, Belén Palomares, Yolanda Gómez-Gálvez, Cristina Palomo-Garo, Sara Campo, Joel Ferrer-Hernández, Carolina Pavicic, Carmen Navarrete, M Luz Bellido, Moisés García-Arencibia, M Ruth Pazos, Eduardo Muñoz, Javier Fernández-Ruiz
BACKGROUND: Neuroprotection with cannabinoids in Parkinson's disease (PD) has been afforded predominantly with antioxidant or anti-inflammatory cannabinoids. In the present study, we investigated the anti-inflammatory and neuroprotective properties of VCE-003.2, a quinone derivative of the non-psychotrophic phytocannabinoid cannabigerol (CBG), which may derive its activity at the peroxisome proliferator-activated receptor-γ (PPARγ). The compound is also an antioxidant. METHODS: We evaluated VCE-003...
January 16, 2018: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29338068/single-and-combined-effects-of-plant-derived-thc-cbd-and-synthetic-win-55-212-cannabinoids-on-cognition-and-cannabinoid-associated-withdrawal-signs-in-mice
#5
Alyssa M Myers, Patrick B Siegele, Jeffrey D Foss, Ronald F Tuma, Sara Jane Ward
BACKGROUND AND PURPOSE: It has been suggested that the non-euphorogenic phytocannabinoid cannabidiol (CBD) can ameliorate adverse effects of delta-9-tetrahydrocannabinol (THC). We determined whether CBD ameliorates cognitive deficits and withdrawal signs induced by cannabinoid CB1/CB2 receptor agonists or produces these pharmacological effects on its own. EXPERIMENTAL APPROACH: The effects of THC or the CB1/CB2 receptor full agonist WIN55212 (WIN) alone, CBD alone, or their combination were tested across a range of doses...
January 16, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29336868/the-therapeutic-potential-of-targeting-the-peripheral-endocannabinoid-cb1-receptor-system
#6
REVIEW
Joseph Tam, Liad Hinden, Adi Drori, Shiran Udi, Shahar Azar, Saja Baraghithy
Endocannabinoids (eCBs) are internal lipid mediators recognized by the cannabinoid-1 and -2 receptors (CB1R and CB2R, respectively), which also mediate the different physiological effects of marijuana. The endocannabinoid system, consisting of eCBs, their receptors, and the enzymes involved in their biosynthesis and degradation, is present in a vast number of peripheral organs. In this review we describe the role of the eCB/CB1R system in modulating the metabolism in several peripheral organs. We assess how eCBs, via activating the CB1R, contribute to obesity and regulate food intake...
January 11, 2018: European Journal of Internal Medicine
https://www.readbyqxmd.com/read/29335480/novel-analgesic-effects-of-melanin-concentrating-hormone-on-persistent-neuropathic-and-inflammatory-pain-in-mice
#7
Jae-Hwan Jang, Ji-Yeun Park, Ju-Young Oh, Sun-Jeong Bae, Hyunchul Jang, Songhee Jeon, Jongpil Kim, Hi-Joon Park
The melanin-concentrating hormone (MCH) is a peptidergic neuromodulator synthesized by neurons in the lateral hypothalamus and zona incerta. MCHergic neurons project throughout the central nervous system, indicating the involvements of many physiological functions, but the role in pain has yet to be determined. In this study, we found that pMCH-/- mice showed lower baseline pain thresholds to mechanical and thermal stimuli than did pMCH+/+ mice, and the time to reach the maximum hyperalgesic response was also significantly earlier in both inflammatory and neuropathic pain...
January 15, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29335158/arvanil-olvanil-am-1172-and-ly-2183240-various-cannabinoid-cb1-receptor-agonists-increase-the-threshold-for-maximal-electroshock-induced-seizures-in-mice
#8
Piotr Tutka, Aleksandra Wlaź, Magdalena Florek-Łuszczki, Patrycjusz Kołodziejczyk, Dorota Bartusik-Aebisher, Jarogniew J Łuszczki
BACKGROUND: Recent evidence reveals therapeutic potential for cannabinoids to reduce seizure frequency, severity and duration. Animal models are useful tools to determine the potential antiseizure or antiepileptic effects of cannabinoids. The objective of this study was evaluation of the effect of arvanil, olvanil, AM 1172 and LY 2183240, the compounds interacted with endocannabinoid and/or endovanilloid systems, on convulsions in the commonly used model of convulsions in mice. METHODS: Arvanil and olvanil were injected intraperitoneally (ip) 30 min and AM 1172 and LY 2183240 were administered ip 60 min before the maximal electroshock seizure threshold (MEST) test...
August 24, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29331500/peripheral-modulation-of-the-endocannabinoid-system-in-metabolic-disease
#9
REVIEW
Nirajan Shrestha, James S M Cuffe, Dana S Hutchinson, John P Headrick, Anthony V Perkins, Andrew J McAinch, Deanne H Hryciw
Dysfunction of the endocannabinoid system (ECS) has been identified in metabolic disease. Cannabinoid receptor 1 (CB1) is abundantly expressed in the brain but also expressed in the periphery. Cannabinoid receptor 2 (CB2) is more abundant in the periphery, including the immune cells. In obesity, global antagonism of overexpressed CB1 reduces bodyweight but leads to centrally mediated adverse psychological outcomes. Emerging research in isolated cultured cells or tissues has demonstrated that targeting the endocannabinoid system in the periphery alleviates the pathologies associated with metabolic disease...
January 10, 2018: Drug Discovery Today
https://www.readbyqxmd.com/read/29328379/mir%C3%A2-1273g%C3%A2-3p-promotes-proliferation-migration-and-invasion-of-lovo-cells-via-cannabinoid-receptor-1-through-activation-of-erbb4-pik3r3-mtor-s6k2-signaling-pathway
#10
Min Li, Xiaoping Qian, Mingzhen Zhu, Aiyi Li, Mingzhi Fang, Yong Zhu, Jingyu Zhang
MicroRNAs (miR) are important in various crucial cell processes including proliferation, migration and invasion. Dysregulation of miRNAs have been increasingly reported to contribute to colorectal cancer. However, the detailed biological function and potential mechanisms of miR‑1273g‑3p in colorectal cancer remain poorly understood. The expression levels of miR‑1273g‑3p in human colorectal cancer LoVo cell lines were detected via reverse transcription‑quantitative polymerase chain reaction (RT‑qPCR)...
January 9, 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29325907/corrigendum-to-cannabinoid-cb1-receptor-inverse-agonist-mj08-stimulates-glucose-production-via-hepatic-sympathetic-innervation-in-rats-european-journal-of-pharmacology-814-2017-232-239
#11
Wei Chen, Hongying Liu, Hua Guan, Nina Xue, Lili Wang
No abstract text is available yet for this article.
January 15, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29325757/the-role-of-fatty-acids-and-their-endocannabinoid-like-derivatives-in-the-molecular-regulation-of-appetite
#12
REVIEW
Renger F Witkamp
Intake, absorption and synthesis of fatty acids, including those produced by the intestinal microbiota are tightly monitored via specific receptors and, indirectly through their conversion into a variety of signalling molecules. The resulting information is integrated and translated to different physiological processes, including the regulation of appetite and satiation. Direct chemosensing of fatty acids takes place via interaction with free fatty acid (FFA) and other receptors. These are present in the oronasal cavity and along the entire gastrointestinal tract, in various other tissues, and, for some receptors also in brain...
January 8, 2018: Molecular Aspects of Medicine
https://www.readbyqxmd.com/read/29325278/-effect-of-cannabinoid-receptor-2-agonist-am1241-on-platelet-derived-growth-factor-expression-in-the-liver-tissue-of-mice-with-hepatic-fibrosis
#13
P He, Y F Wu, H Y Yang, M L Cheng, Y D Liang, Y P Wang
Objective: To investigate the effect of cannabinoid receptor-2 (CB2) agonist AM1241 on the mRNA and protein expression of platelet-derived growth factor (PDGF) and collagen-III (Col-III) in the liver tissue of mice with experimental liver fibrosis induced by carbon tetrachloride (CCl(4)). Methods: Totally 38 8-week-old male C57BL/6J mice were randomly divided into control group, model group, 3 mg/kg CB2 receptor agonist (AM1241) group, and 9 mg/kg AM1241 group. All mice, except for the control group, were treated with 30% CCl(4) (three times a week, 5 ml/kg body weight, 16 weeks) to establish a liver fibrosis model...
November 20, 2017: Zhonghua Gan Zang Bing za Zhi, Zhonghua Ganzangbing Zazhi, Chinese Journal of Hepatology
https://www.readbyqxmd.com/read/29317072/betacaryophyllene-a-phytocannabinoid-as-potential-therapeutic-modality-for-human-sepsis
#14
Angel Meza, Christian Lehmann
Sepsis is a clinical condition resulting from a dysregulated immune response to an infection that leads to organ dysfunction. Despite numerous efforts to optimize treatment, sepsis remains to be the main cause of death in most intensive care units. The endogenous cannabinoid system (ECS) plays an important role in inflammation. Cannabinoid receptor 2 (CB2R) activation is immunosuppressive, which might be beneficial during the hyper-inflammatory phase of sepsis. Beta-caryophyllene (BCP) is a non-psychoactive natural cannabinoid (phytocannabinoid) found in Cannabis sativa and in essential oils of spices and food plants, that acts as a selective agonist of CB2R...
January 2018: Medical Hypotheses
https://www.readbyqxmd.com/read/29314831/a-fluorescent-probe-to-unravel-functional-features-of-cannabinoid-receptor-cb1-in-human-blood-and-tonsil-immune-system-cells
#15
Mar Martín-Fontecha, Alba Angelina, Beate Rückert, Ainoa Rueda-Zubiaurre, Leticia Martin-Cruz, Willem van de Veen, Mübeccel Akdis, Silvia Ortega-Gutierrez, María L López-Rodrí Guez, Cezmi Akdis, Oscar Palomares
The human endogenous cannabinoid system (ECS) regulates key physiological processes and alterations in its signalling pathways and endocannabinoid levels are associated to diseases such as neurological and neuropsychiatric conditions, cancer, pain and inflammation, obesity, 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...
January 9, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29314474/multiple-binding-sites-contribute-to-the-mechanism-of-the-2-phenylindole-mixed-orthosteric-agonistic-and-pam-action-on-the-cannabinoid-cb1-receptor
#16
Noureldin Saleh, Oliver Hucke, Florian Montel, Gert Kramer, Boris Ferger, Esther Schmidt, Timothy Clark, Peter Hildebrand, Christofer Tautermann, Radoslaw Lipinski
The cannabinoid CB1 receptor (CB1R) is an abundant metabotropic G-protein coupled receptor that has been difficult to address therapeutically because of CNS side effects exerted by orthosteric ligands. Recent efforts have focused on developing allosteric modulators that target CB1R. Compounds from a recently discovered of 2-phenylindoles mixed agonist and positive allosteric modulators (Ago-PAMs), have shown promising properties for CB1R. Here, we identify binding modes of both the CP 55,940 agonist and GAT228 a 2-phenylindole allosteric modulator using a metadynamics simulation, and quantify their affinity and cooperativity...
January 3, 2018: Angewandte Chemie
https://www.readbyqxmd.com/read/29313218/thallium-induced-toxicity-in-rat-brain-crude-synaptosomal-mitochondrial-fractions-is-sensitive-to-anti-excitatory-and-antioxidant-agents
#17
Marisol Maya-López, María Verónica Mireles-García, Monserrat Ramírez-Toledo, Ana Laura Colín-González, Sonia Galván-Arzate, Isaac Túnez, Abel Santamaría
The mechanisms by which the heavy metal thallium (Tl+) produces toxicity in the brain remain unclear. Herein, isolated synaptosomal/mitochondrial P2 crude fractions from adult rat brains were exposed to Tl+ (5-250 μM) for 30 min. Three toxic endpoints were evaluated: mitochondrial dysfunction, lipid peroxidation, and Na+/K+-ATPase activity inhibition. Concentration-response curves for two of these endpoints revealed the optimum concentration of Tl+ to induce damage in this preparation, 5 μM. Toxic markers were also estimated in preconditioned synaptosomes incubated in the presence of the N-methyl-D-aspartate receptor antagonist kynurenic acid (KYNA, 50 μM), the cannabinoid receptor agonist WIN 55,212-2 (1 μM), or the antioxidant S-allyl-L-cysteine (SAC, 100 μM)...
January 8, 2018: Neurotoxicity Research
https://www.readbyqxmd.com/read/29311110/long-lasting-in-vivo-effects-of-the-cannabinoid-cb1-antagonist-am6538
#18
Carol A Paronis, Girish R Chopda, Kiran Vemuri, Ani S Zakarian, Alexandros Makriyannis, Jack Bergman
AM6538 is a cannabinoid antagonist that binds CB1 receptors expressed in HEK-293 cells in a wash-resistant manner. The effects of AM6538 in live animals has not previously been established. We characterized the antagonist effects of AM6538 in male mice, using a warm-water tail-withdrawal assay, and in male squirrel monkeys trained to discriminate the CB1 agonist AM4054 from vehicle. The cannabinoid agonists WIN 55,212, Δ9-tetrahydrocannabinol (THC), and AM4054 all produced 100% maximum possible antinociceptive effects in mice following vehicle pretreatment...
January 8, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29310667/wwl70-protects-against-chronic-constriction-injury-induced-neuropathic-pain-in-mice-by-cannabinoid-receptor-independent-mechanisms
#19
Jie Wen, Melissa Jones, Mikiei Tanaka, Prabhuanand Selvaraj, Aviva J Symes, Brian Cox, Yumin Zhang
BACKGROUND: Targeting the endocannabinoid system has emerged as an effective strategy for the treatment of inflammatory and neurological diseases. Unlike the inhibition of the principal 2-arachidonyl glycerol (2-AG) hydrolytic enzyme monoacylglycerol lipase (MAGL), which leads to 2-AG overload and cannabinoid receptor desensitization, selective inhibition of the minor 2-AG hydrolytic enzyme alpha, beta-hydrolase domain 6 (ABHD6) can provide therapeutic benefits without producing cannabimimetic side effects...
January 8, 2018: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29306933/mechanisms-and-treatment-of-painful-neuromas
#20
Changfeng Lu, Xun Sun, Chong Wang, Yu Wang, Jiang Peng
A painful neuroma is a common complication of a peripheral nerve injury or amputation, and it can cause tremendous pain that is resistant to most analgesics. Furthermore, painful neuromas have a high postoperative recurrence rate. Painful neuromas are often accompanied by functional disorders, drastically reducing the patient's quality of life. Several pathophysiological mechanisms have been proposed to explain this type of neuropathic pain, including peripheral and central sensitisation and the involvement of nerve growth factor, α-smooth muscle actin, the cannabinoid CB2 receptor and structural changes in neuroma fibres...
January 8, 2018: Reviews in the Neurosciences
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