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https://www.readbyqxmd.com/read/29232588/bioactive-products-from-singlet-oxygen-photooxygenation-of-cannabinoids
#1
Ahmed Galal Osman, Khaled M Elokely, Vivek K Yadav, Paulo Carvalho, Mohamed Radwan, Desmond Slade, Waseem Gul, Shabana Khan, Olivia R Dale, Afeef S Husni, Michael L Klein, Stephen J Cutler, Samir A Ross, Mahmoud A ElSohly
Photooxygenation of Δ8 tetrahydrocannabinol (Δ8-THC), Δ9 tetrahydrocannabinol (Δ9-THC), Δ9 tetrahydrocannabinolic acid (Δ9-THCA) and some derivatives (acetate, tosylate and methyl ether) yielded 24 oxygenated derivatives, 18 of which were new and 6 were previously reported, including allyl alcohols, ethers, quinones, hydroperoxides, and epoxides. Testing these compounds for their modulatory effect on cannabinoid receptors CB1 and CB2 led to the identification of 7 and 21 as CB1 partial agonists with Ki values of 0...
November 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29229226/novel-sulfenamides-and-sulfonamides-based-on-pyridazinone-and-pyridazine-scaffolds-as-cb1-receptor-ligand-antagonists
#2
Gabriele Murineddu, Francesco Deligia, Giulio Ragusa, Laura García-Toscano, María Gómez-Cañas, Battistina Asproni, Valentina Satta, Elena Cichero, Ruth Pazos, Paola Fossa, Giovanni Loriga, Javier Fernández-Ruiz, Gerard A Pinna
A series of sulfenamide and sulfonamide derivatives was synthesized and evaluated for the affinity at CB1 and CB2 receptors. The N-bornyl-S-(5,6-di-p-tolylpyridazin-3-yl)-sulfenamide, compound 11, displayed good affinity and high selectivity for CB1 receptors (Ki values of 44.6 nM for CB1 receptors and >40 μM for CB2 receptors, respectively). The N-isopinocampheyl-sulfenamide 12 and its sulfonamide analogue 22 showed similar selectivity for CB1 receptors with Ki values of 75.5 and 73.2 nM, respectively...
December 2, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29225001/dorsal-hippocampal-cannabinergic-and-gabaergic-systems-modulate-memory-consolidation-in-passive-avoidance-task
#3
Mohammad Nasehi, Parisa Gerami, Fatemeh Khakpai, Mohammad-Reza Zarrindast
In the present research, we examined the possible interaction between the hippocampal CB2 and GABAA receptors on modulation of memory consolidation. In this research, step-down passive avoidance task was used to evaluate memory consolidation in adult male NMRI mice. The results showed that post-training intra-CA1 administration of muscimol (0.05 and 0.1μg/mouse) impaired memory consolidation as evidenced by a decrease in step-down latency on the test day, which was suggestive of drug-produced amnesia. However co-administration of different doses of muscimol (0...
December 7, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/29218862/the-presence-and-distribution-of-cannabinoid-type-1-and-2-receptors-in-the-mandibular-gland-the-influence-of-different-physical-forms-of-diets-on-their-expression-in-piglets
#4
C Pirino, M G Cappai, M Maranesi, D Tomassoni, A Giontella, W Pinna, C Boiti, J Kamphues, C Dall'Aglio
We explored the expression and cell type distribution of cannabinoid receptors type 1 (CB1) and cannabinoid receptors type 2 (CB2) in the mandibular glands of pigs in relation to different physical forms of the diet. Thirty-two crossbred growing pigs (ages 5-6 weeks) were randomly allotted to four experimental groups (eight pigs/group) and fed four different physical types of the same diet for 4 weeks: finely ground pellet (FP), coarsely ground meal (CM), coarsely ground pellet (CP) and coarsely ground extruded (CE) with dMEAN of 0...
December 7, 2017: Journal of Animal Physiology and Animal Nutrition
https://www.readbyqxmd.com/read/29192123/the-slowly-signaling-g-protein-biased-cb2-cannabinoid-receptor-agonist-ly2828360-suppresses-neuropathic-pain-with-sustained-efficacy-and-attenuates-morphine-tolerance-and-dependence
#5
Xiaoyan Lin, Amey S Dhopeshwarkar, Megan Huibregtse, Ken Mackie, Andrea G Hohmann
The CB2 cannabinoid agonist LY2828360 lacked both toxicity and efficacy in a clinical trial for osteoarthritis. Whether LY2828360 suppresses neuropathic pain has not been reported and its signaling profile is unknown. In vitro, LY2828360 was a slowly acting but efficacious G protein-biased CB2 agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling while failing to recruit arrestin, activate inositol phosphate signaling or internalize CB2 receptors. In wildtype (WT) mice, LY2828360 (3 mg/kg/day i...
November 30, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29187590/selective-cannabinoid-2-receptor-stimulation-reduces-tubular-epithelial-cell-damage-following-renal-ischemia-reperfusion-injury
#6
Jeffrey D Pressly, Suni M Mustafa, Ammaar Abidi, Sahar Alghamdi, Pankaj Pandey, Kuldeep K Roy, Robert Doerksen, Bob M Moore, Frank Park
Ischemia-reperfusion injury (IRI) is a common cause of acute kidney injury (AKI), which is an increasing problem in the clinic and has been associated with increased rates of mortality. Currently, therapies to treat AKI are not available, so identification of new targets which, upon diagnosis of AKI, can be modulated to ameliorate renal damage is essential. In this study, a novel cannabinoid receptor 2 (CB2) agonist, SMM-295, was designed, synthesized, and tested in vitro and in silico. In vivo testing of the CB2 agonist was performed using a mouse model of bilateral IRI, which is a common model to mimic human AKI...
November 29, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29176975/targeting-cannabinoid-signaling-in-the-immune-system-high-ly-exciting-questions-possibilities-and-challenges
#7
REVIEW
Attila Oláh, Zoltán Szekanecz, Tamás Bíró
It is well known that certain active ingredients of the plants of Cannabis genus, i.e., the "phytocannabinoids" [pCBs; e.g., (-)-trans-Δ9-tetrahydrocannabinol (THC), (-)-cannabidiol, etc.] can influence a wide array of biological processes, and the human body is able to produce endogenous analogs of these substances ["endocannabinoids" (eCB), e.g., arachidonoylethanolamine (anandamide, AEA), 2-arachidonoylglycerol (2-AG), etc.]. These ligands, together with multiple receptors (e.g., CB1 and CB2 cannabinoid receptors, etc...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/29170454/cb2-receptor-activation-causes-an-erk1-2-dependent-inflammatory-response-in-human-rpe-cells
#8
M Hytti, S Andjelic, N Josifovska, N Piippo, E Korhonen, M Hawlina, K Kaarniranta, T J Nevalainen, G Petrovski, T Parkkari, A Kauppinen
A chronic low-level inflammation contributes to the pathogenesis of age-related macular degeneration (AMD), the most common cause of blindness in the elderly in Western countries. The loss of central vision results from attenuated maintenance of photoreceptors due to the degeneration of retinal pigment epithelium (RPE) cells beneath the photoreceptor layer. It has been proposed that pathologic inflammation initiated in RPE cells could be regulated by the activation of type 2 cannabinoid receptors (CB2). Here, we have analysed the effect of CB2 activation on cellular survival and inflammation in human RPE cells...
November 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29169951/regulation-of-noradrenergic-and-serotonergic-systems-by-cannabinoids-relevance-to-cannabinoid-induced-effects
#9
REVIEW
Aitziber Mendiguren, Erik Aostri, Joseba Pineda
The cannabinoid system is composed of Gi/o protein-coupled cannabinoid type 1 receptor (CB1) and cannabinoid type 2 (CB2) receptor and endogenous compounds. The CB1 receptor is widely distributed in the central nervous system (CNS) and it is involved in the regulation of common physiological functions. At the neuronal level, the CB1 receptor is mainly placed at GABAergic and glutamatergic axon terminals, where it modulates excitatory and inhibitory synapses. To date, the involvement of CB2 receptor in the regulation of neurotransmission in the CNS has not been clearly shown...
November 20, 2017: Life Sciences
https://www.readbyqxmd.com/read/29167227/pericardial-adipose-tissue-regulates-granulopoiesis-fibrosis-and-cardiac-function-after-myocardial-infarction
#10
Michael Horckmans, Mariaelvy Bianchini, Donato Santovito, Remco T A Megens, Jean-Yves Springael, Irene Negri, Michele Vacca, Marco Di Eusanio, Antonio Moschetta, Christian Weber, Johan Duchene, Sabine Steffens
Background -The pericardial adipose tissue (AT) contains a high density of lymphoid clusters. Is unknown whether these clusters play a role in post-myocardial infarction (MI) inflammatory responses and cardiac outcome. Methods -Lymphoid clusters were examined in epicardial AT of humans with or without coronary artery disease (CAD). Murine pericardial lymphoid clusters were visualized in mice subjected to coronary artery ligation. To study the relevance of pericardial clusters during inflammatory responses after MI, we surgically removed the pericardial AT, performed B cell depletion and GM-CSF blockade...
November 22, 2017: Circulation
https://www.readbyqxmd.com/read/29151076/modulation-of-the-endocannabinoid-system-by-the-fatty-acid-amide-hydrolase-monoacylglycerol-and-diacylglycerol-lipase-inhibitors-as-an-attractive-target-for-secretory-diarrhoea-therapy
#11
A Wasilewski, A Misicka, M Sacharczuk, J Fichna
Secretory diarrhoea is a leading cause of mortality and morbidity worldwide. Our aim was to characterize the effect of inhibition of selected enzymes involved in the synthesis or degradation of endocannabinoids on electrolyte equilibrium in the mouse colonic tissue. The aim of this study was to evaluate the effects of PF-3845, JZL-184 and RHC-80267, as inhibitors of fatty acid amide hydrolase (FAAH), monoacylglycerol (MAGL) and diacylglycerol lipase (DAGL), respectively on epithelial ion transport in isolated mouse colon stimulated by forskolin (FSK), veratridine (VER) and bethanechol (BET)...
August 2017: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/29130941/remote-ischemia-preconditioning-attenuates-blood-spinal-cord-barrier-breakdown-in-rats-undergoing-spinal-cord-ischemia-reperfusion-injury-associated-with-activation-and-upregulation-of-cb1-and-cb2-receptors
#12
Na Jing, Bo Fang, Zhi-Lin Wang, Hong Ma
BACKGROUND/AIMS: Remote ischemic preconditioning (RIPC) has protective effects on spinal cord ischemia reperfusion (I/R) injury, but the potential mechanisms remain unclear. In our study, the effects and underlying mechanisms of RIPC on blood-spinal cord barrier (BSCB) breakdown following I/R injury were investigated. METHODS: animals underwent intraperitoneal administration with cannabinoid-1 (CB1) receptor antagonist AM251, cannabinoid-2 (CB2) receptor antagonist AM630 or vehicle 15 minutes before three 3-minute occlusion-reperfusion cycles on the right femoral artery or a sham operation...
October 31, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29128791/acpa-and-jwh-133-modulate-the-vascular-tone-of-superior-mesenteric-arteries-through-cannabinoid-receptors-bkca-channels-and-nitric-oxide-dependent-mechanisms
#13
Evelyn López-Dyck, Felipa Andrade-Urzúa, Alejandro Elizalde, Tania Ferrer-Villada, Adan Dagnino-Acosta, Miguel Huerta, Zyanya Osuna-Calleros, Cinthia Rangel-Sandoval, Enrique Sánchez-Pastor
BACKGROUND: Some cannabinoids, a family of compounds derived from Cannabis sativa (marijuana), have previously shown vasodilator effects in several studies, a feature that makes them suitable for the generation of a potential treatment for hypertension. The mechanism underlying this vasodilator effect in arteries is still controversial. In this report, we explored how the synthetic cannabinoids ACPA (CB1-selective agonist) and JWH-133 (CB2-selective agonist) regulate the vascular tone of rat superior mesenteric arteries...
July 1, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29127599/cb1-receptors-mediated-inhibition-of-atp-induced-ca-2-i-increase-in-cultured-rat-spinal-dorsal-horn-neurons
#14
Jingdong Long, Xiaolu Lei, Meiyun Chen, Shulei Yang, Tao Sun, Junwei Zeng, Deqian Yu, Hong Tian, Xiaohong Liu
Spinal cannabinoid receptor 1 (CB1R) and purinergic P2X receptors (P2XR) play a critical role in the process of pathological pain. Both CB1R and P2XR are expressed in spinal dorsal horn (DH) neurons. It is not clear whether CB1 receptor activation modulates the function of P2X receptor channels within dorsal horn. For this reason, we observed the effect of CP55940 (cannabinoid receptor agonist) on ATP-induced Ca(2+) mobilization in cultured rat DH neurons. The changes of intracellular calcium concentration ([Ca(2+)]i) were detected with confocal laser scanning microscopy using fluo-4/AM as a calcium fluorescent indicator...
November 10, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/29126730/optimization-of-pharmacokinetic-properties-by-modification-of-a-carbazole-based-cannabinoid-receptor-subtype-2-cb2-ligand
#15
Dominik Heimann, Frederik Börgel, Henk de Vries, Kim Bachmann, Victoria E Rose, Bastian Frehland, Dirk Schepmann, Laura H Heitman, Bernhard Wünsch
Recently, the development of the fluorinated PET tracer [(18)F]1a for imaging of CB2 receptors in the central nervous system was reported. [(18)F]1a showed high CB2 affinity and selectivity over the CB1 subtype, but rapid biotransformation in mice. In addition to the amide hydrolysis, oxidative N-dealkylation and carbazole oxidation were postulated as main metabolic pathways. Based on these results, novel carbazole derivatives with additional 6-substituents (23a, 24a), modified hydrogenation state (26a) and enlarged fluoroalkyl substituent (13a, 13b) were synthesized and pharmacologically evaluated...
October 16, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29120578/role-of-cannabinoid-cb2-receptor-gene-cnr2-polymorphism-in-children-with-immune-thrombocytopenic-purpura-in-beni-suef-governorate-in-egypt
#16
Dina A Ezzat, Amira A Hammam, Waleed M El-Malah, Rasha A Khattab, Eman M Mangoud
The cannabinoid system is involved in the immune regulation by modulation of Th cells type 1 and 2. It is composed of the CB2 receptor which is expressed at 10 to 100 folds greater levels on immune cells than the CB1 receptors. The CB2 is encoded by the cannabinoid CB receptor gene (CNR2) gene. This study aims to investigate the polymorphism in CNR2 gene variation rs 35761398 (Q63R) in Egyptian children with immune thrombocytopenic purpura and to investigate the relation between this gene polymorphism and either the susceptibility to or the chronicity of the disease...
January 2017: Egyptian Journal of Immunology
https://www.readbyqxmd.com/read/29113898/finding-order-in-chemical-chaos-continuing-characterization-of-synthetic-cannabinoid-receptor-agonists
#17
REVIEW
Julie A Marusich, Jenny L Wiley, Timothy W Lefever, Purvi R Patel, Brian F Thomas
Diversion of synthetic cannabinoids from the lab to drugs of abuse has become increasingly prevalent in recent years. Moreover, as earlier synthetic cannabinoids were banned, manufacturers introduced a new supply of novel compounds to serve as replacements. Hence, the chemical diversity of synthetic cannabinoid analogs has also rapidly increased. The present study examined 8 new synthetic cannabinoids: AM-1220, AM-2232, AM-2233, AM-679, EAM-2201, JWH-210, JHW-251, and MAM-2201. Each compound was assessed for binding affinity and functional activation of CB1 and CB2 receptors, and pharmacological equivalence with Δ(9)-tetrahydrocannabinol (THC) in THC drug discrimination...
November 4, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29111112/anti-migraine-effect-of-%C3%A2-9-tetrahydrocannabinol-in-the-female-rat
#18
Ram Kandasamy, Cole T Dawson, Rebecca M Craft, Michael M Morgan
Current anti-migraine treatments have limited efficacy and many side effects. Although anecdotal evidence suggests that marijuana is useful for migraine, this hypothesis has not been tested in a controlled experiment. Thus, the present study tested whether administration of ∆(9)-tetrahydrocannabinol (THC) produces anti-migraine effects in the female rat. Microinjection of the TRPA1 agonist allyl isothiocyanate (AITC) onto the dura mater produced migraine-like pain for 3h as measured by depression of home cage wheel running...
October 28, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29110748/perinatal-maternal-high-fat-diet-induces-early-obesity-and-sex-specific-alterations-of-the-endocannabinoid-system-in-white-and-brown-adipose-tissue-of-weanling-rat-offspring
#19
Mariana M Almeida, Camilla P Dias-Rocha, André S Souza, Mariana F Muros, Leonardo S Mendonca, Carmen C Pazos-Moura, Isis H Trevenzoli
Perinatal maternal high-fat (HF) diet programmes offspring obesity. Obesity is associated with overactivation of the endocannabinoid system (ECS) in adult subjects, but the role of the ECS in the developmental origins of obesity is mostly unknown. The ECS consists of endocannabinoids, cannabinoid receptors (cannabinoid type-1 receptor (CB1) and cannabinoid type-2 receptor (CB2)) and metabolising enzymes. We hypothesised that perinatal maternal HF diet would alter the ECS in a sex-dependent manner in white and brown adipose tissue of rat offspring at weaning in parallel to obesity development...
November 7, 2017: British Journal of Nutrition
https://www.readbyqxmd.com/read/29110331/radioligands-for-positron-emission-tomography-imaging-of-cannabinoid-type-2-receptor
#20
Francesco Spinelli, Linjing Mu, Simon M Ametamey
The cannabinoid type 2 (CB2) receptor is an immunomodulatory receptor mainly expressed in peripheral cells and organs of the immune system. The expression level of CB2 in the central nervous system under physiological conditions is negligible, however under neuroinflammatory conditions an upregulation of CB2 protein or mRNA mainly co-localized with activated microglial cells has been reported. Consequently, CB2 agonists have been confirmed to play a role in neuroprotective and anti-inflammatory processes. A suitable PET radioligand for imaging CB2 would provide an invaluable research tool to explore the role of CB2 receptor expression in inflammatory disorders...
November 6, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
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