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https://www.readbyqxmd.com/read/27905004/ocular-disposition-of-%C3%A2-8-tetrahydrocannabinol-from-various-topical-ophthalmic-formulations
#1
Nagendra S Punyamurthula, Goutham R Adelli, Waseem Gul, Michael A Repka, Mahmoud A ElSohly, Soumyajit Majumdar
The purposes of this project are to enhance the trans-membrane penetration of Δ(8)-Tetrahydrocannabinol (Δ(8)-THC) and to study the effect of various lipid based systems in delivering the compound, non-invasively, to anterior and posterior ocular chambers. Solid lipid nanoparticles (SLNs), fast gelling films were manufactured using high pressure homogenization and melt cast techniques, respectively. The formulations were characterized for drug content, entrapment efficiency, particle size and subsequently evaluated in vitro for trans-corneal permeation...
November 30, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27899300/role-of-the-endocannabinoid-system-in-the-control-of-mouse-myometrium-contractility-during-the-menstrual-cycle
#2
Ester Pagano, Pierangelo Orlando, Stefania Finizio, Antonietta Rossi, Lorena Buono, Fabio Arturo Iannotti, Fabiana Piscitelli, Angelo A Izzo, Vincenzo Di Marzo, Francesca Borrelli
Cannabis and cannabinoids are known to affect female reproduction. However, the role of the endocannabinoid system in mouse uterine contractility in the dioestrus and oestrus phases has not been previously investigated. The present study aimed at filling this gap. Endocannabinoid (anandamide and 2-arachidonoylglycerol) levels were measured in mouse uterus at dioestrus and oestrus phases by liquid chromatography-mass spectrometry; quantitative reverse transcription-PCR measured mRNA expression of cannabinoid receptors and enzymes involved in the metabolism of endocannabinoids...
November 26, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27891602/cannabimimetic-phytochemicals-in-the-diet-an-evolutionary-link-to-food-selection-and-metabolic-stress-adaptation
#3
REVIEW
Jürg Gertsch
The endocannabinoid system (ECS) is a major lipid signaling network that plays important pro-homeostatic (allostatic) roles not only in the nervous system but in peripheral organs. Increasing evidence points towards a dietary component in the modulation of the ECS. Cannabinoid receptors in hominids co-evolved with diet and the ECS constitutes a feedback loop for food selection and energy metabolism. Here it is postulated that the mismatch of ancient lipid genes of hunter-gatheres and pastoralists with the high carbohydrate diet introduced by agriculture could be compensated via dietary modulation of the ECS...
November 27, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27890711/the-endogenous-lipid-n-arachidonoyl-glycine-is-hypotensive-and-nitric-oxide-cgmp-dependent-vasorelaxant
#4
Yousuf M Al Suleimani, Ahmed S Al Mahruqi
N-arachidonoyl glycine (NAGLY), is the endogenous lipid that activates the G protein-couple receptor 18 (GPR18) with vasodilatory activity in resistance arteries. This study investigates its hemodynamic effects and mechanisms of vasorelaxation. Hemodynamic effects of NAGLY in rats were assessed using a Biopac system and its vascular responses were assessed using a wire myograph. NAGLY (1 mg/kg) decreased blood pressure by 69.4 ± 5.5% and reduced renal blood flow by 88 ± 12% and the effects were not sensitive to inhibition by O-1918 (3 mg/kg)...
November 24, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27884725/endocannabinoid-system-in-sexual-motivational-processes-is-it-a-novel-therapeutic-horizon
#5
REVIEW
Renata Androvicova, Jiri Horacek, Tibor Stark, Filippo Drago, Vincenzo Micale
The endocannabinoid system (ECS), which is composed of the cannabinoid receptors types 1 and 2 (CB1 and CB2) for marijuana's psychoactive ingredient Δ(9)-tetrahydrocannabinol (Δ(9)-THC), the endogenous ligands (AEA and 2-AG) and the enzymatic systems involved in their biosynthesis and degradation, recently emerged as important modulator of emotional and non-emotional behaviors. For centuries, in addition to its recreational actions, several contradictory claims regarding the effects of Cannabis use in sexual functioning and behavior (e...
November 21, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27875353/cannabinoid-receptor-2-functional-variant-contributes-to-the-risk-for-pediatric-inflammatory-bowel-disease
#6
Caterina Strisciuglio, Giulia Bellini, Erasmo Miele, Massimo Martinelli, Sabrina Cenni, Chiara Tortora, Carlo Tolone, Emanuele Miraglia Del Giudice, Francesca Rossi
GOALS: We conducted a case-control association analysis to establish the role of a common CB2 functional variant, Q63R, in the susceptibility to inflammatory bowel disease (IBD). BACKGROUND: Endocannabinoids may limit intestinal inflammation through cannabinoid receptor 1 and/or 2 (CB1, CB2). STUDY: We genotyped 217 pediatric IBD patients [112 Crohn's disease (CD), 105 ulcerative colitis (UC)] and 600 controls for the CB2-Q63R variant by Taqman assay...
November 21, 2016: Journal of Clinical Gastroenterology
https://www.readbyqxmd.com/read/27867358/biased-agonism-of-three-different-cannabinoid-receptor-agonists-in-mouse-brain-cortex
#7
Rebeca Diez-Alarcia, Inés Ibarra-Lecue, Ángela P Lopez-Cardona, Javier Meana, Alfonso Gutierrez-Adán, Luis F Callado, Ekaitz Agirregoitia, Leyre Urigüen
Cannabinoid receptors are able to couple to different families of G proteins when activated by an agonist drug. It has been suggested that different intracellular responses may be activated depending on the ligand. The goal of the present study was to characterize the pattern of G protein subunit stimulation triggered by three different cannabinoid ligands, Δ(9)-THC, WIN55212-2, and ACEA in mouse brain cortex. Stimulation of the [(35)S]GTPγS binding coupled to specific immunoprecipitation with antibodies against different subtypes of G proteins (Gαi1, Gαi2, Gαi3, Gαo, Gαz, Gαs, Gαq/11, and Gα12/13), in the presence of Δ(9)-THC, WIN55212-2 and ACEA (submaximal concentration 10 μM) was determined by scintillation proximity assay (SPA) technique in mouse cortex of wild type, CB1 knock-out, CB2 knock-out and CB1/CB2 double knock-out mice...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27861558/modulation-of-type-1-and-type-2-cannabinoid-receptors-by-saffron-in-a-rat-model-of-retinal-neurodegeneration
#8
Rita Maccarone, Cinzia Rapino, Darin Zerti, Monia di Tommaso, Natalia Battista, Stefano Di Marco, Silvia Bisti, Mauro Maccarrone
Experimental studies demonstrated that saffron (Crocus sativus) given as a dietary supplement counteracts the effects of bright continuous light (BCL) exposure in the albino rat retina, preserving both morphology and function and probably acting as a regulator of programmed cell death [1]. The purpose of this study was to ascertain whether the neuroprotective effect of saffron on rat retina exposed to BCL is associated with a modulation of the endocannabinoid system (ECS). To this aim, we used eight experimental groups of Sprague-Dawley rats, of which six were exposed to BCL for 24 hours...
2016: PloS One
https://www.readbyqxmd.com/read/27851727/high-resolution-crystal-structure-of-the-human-cb1-cannabinoid-receptor
#9
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
#10
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/27832960/novel-indole-based-compounds-that-differentiate-alkylindole-sensitive-receptors-from-cannabinoid-receptors-and-microtubules-characterization-of-their-activity-on-glioma-cell-migration
#11
Susan Fung, Cong Xu, Ernest Hamel, James B Wager-Miller, Grace Woodruff, Aaron Miller, Christina Sanford, Ken Mackie, Nephi Stella
Indole-based compounds, such as the alkyl-indole (AI) compound WIN55212-2, activate the cannabinoid receptors, CB1 and CB2, two well-characterized G protein-coupled receptors (GPCR). Reports indicate that several indole-based cannabinoid agonists, including WIN55212-2, lack selectivity and interact with at least two additional targets: AI-sensitive GPCRs and microtubules. Studying how indole-based compounds modulate the activity of these 4 targets has been difficult as selective chemical tools were not available...
November 7, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27806128/exposure-to-a-highly-caloric-palatable-diet-during-the-perinatal-period-affects-the-expression-of-the-endogenous-cannabinoid-system-in-the-brain-liver-and-adipose-tissue-of-adult-rat-offspring
#12
María Teresa Ramírez-López, Raquel Arco, Juan Decara, Mariam Vázquez, Rosario Noemí Blanco, Francisco Alén, Juan Suárez, Raquel Gómez de Heras, Fernando Rodríguez de Fonseca
Recent studies have linked gestational exposure to highly caloric diets with a disrupted endogenous cannabinoid system (ECS). In the present study, we have extended these studies by analyzing the impact of the exposure to a palatable diet during gestation and lactation on a) the adult expression of endocannabinoid-related behaviors, b) the metabolic profile of adult offspring and c) the mRNA expression of the signaling machinery of the ECS in the hypothalamus, the liver and the adipose tissue of adult offspring of both sexes...
2016: PloS One
https://www.readbyqxmd.com/read/27798285/endocannabinoid-system-and-pregnancy
#13
REVIEW
Fernando Correa, Manuel L Wolfson, Paula Valchi, Julieta Aisemberg, Ana María Franchi
The endocannabinoid system (eCS), is a complex system, comprising the main endogenous ligands anandamide and 2-arachidonoyl glycerol, the cannabinoid receptors CB1 and CB2 and the biosynthetic and degrading enzymes. Cumulative evidence shows that the eCS plays an important role in reproduction, from egg fertilization to parturition. Therefore, alterations in this system, either by recreation/therapeutic use of cannabis or deregulation of the endogenous cannabinoids, might lead to adverse pregnancy outcomes, including retardation in embryo development, poor blastocyst implantation, inhibition of decidualization, miscarriage and compromised placentation...
December 2016: Reproduction: the Official Journal of the Society for the Study of Fertility
https://www.readbyqxmd.com/read/27798282/exocannabinoids-effect-on-in-vitro-bovine-oocyte-maturation-via-activation-of-akt-and-erk1-2
#14
A P López-Cardona, M J Sánchez-Calabuig, P Beltran-Breña, N Agirregoitia, D Rizos, E Agirregoitia, A Gutierrez-Adán
Endocannabinoids are known to mediate practically all reproductive events in mammals; however, little is known about their role in oocyte maturation. Through RT-PCR and immunocytochemistry, this study confirms the presence of CB1 and CB2 cannabinoid receptors in bovine oocytes and shows how exposure to the exogenous cannabinoids HU-210 and THC during their in vitro maturation (IVM) activates the phosphorylation of AKT and ERK1/2 proteins associated with the resumption of meiosis. Although supplementation with HU-210 or THC during IVM did not increase blastocyst yields, the expression of interferon tau (IFNτ) and gap junction alpha-1 protein (GJA1) was enhanced at the blastocyst stage...
December 2016: Reproduction: the Official Journal of the Society for the Study of Fertility
https://www.readbyqxmd.com/read/27779402/detection-and-activity-profiling-of-synthetic-cannabinoids-and-metabolites-with-a-newly-developed-bio-assay
#15
Annelies Cannaert, Jolien Storme, Florian Franz, Volker Auwärter, Christophe P Stove
Synthetic cannabinoids (SCs) are the largest group of compounds currently monitored in Europe by the EU Early Warning System on new psychoactive substances. Emerging recreational use of these products has led to multiple cases of adverse health effects and even death. In contrast to marijuana, where Δ9-tetrahydrocannabinol (Δ9THC) is metabolized to only one major active metabolite, it has been reported that several major phase I metabolites of SCs remain biologically active, exerting cannabinoid (CB) receptor affinity, potency and efficacy greater than Δ9THC...
October 25, 2016: Analytical Chemistry
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
#16
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...
October 20, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27766867/therapeutic-potential-of-fatty-acid-amide-hydrolase-monoacylglycerol-lipase-and-n-acylethanolamine-acid-amidase-inhibitors
#17
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/27748182/hemopressin-peptides-as-modulators-of-the-endocannabinoid-system-and-their-potential-applications-as-therapeutic-tools
#18
Giorgia Macedonio, Azzurra Stefanucci, Cristina Maccallini, Sako Mirzaie, Ettore Novellino, Adriano Mollica
The endocannabinoid system is activated by the binding of natural arachidonic acid derivatives (endogenous cannabinoids or endocannabinoids) as lipophilic messengers to cannabinoid receptors CB1 and CB2. The endocannabinoid system comprises also many hydrolytic enzymes responsible for the endocannabinoids cleavage, such as FAAH and MAGL. These two enzymes are possible therapeutic targets for the development of new drugs as indirect cannabinoid agonists. Recently a new family of endocannabinoid modulators was discovered; the lead of this family is the nonapeptide hemopressin produced from enzymatic cleavage of the α-chain of hemoglobin and acting as negative allosteric modulator of CB1...
October 7, 2016: Protein and Peptide Letters
https://www.readbyqxmd.com/read/27746343/revealing-the-role-of-the-endocannabinoid-system-modulators-sr141716a-urb597-and-vdm-11-in-sleep-homeostasis
#19
Eric Murillo-Rodríguez, Sergio Machado, Nuno Barbosa Rocha, Henning Budde, Ti-Fei Yuan, Oscar Arias-Carrión
The endocannabinoid system comprises receptors (CB1 and CB2 cannabinoid receptors), enzymes (Fatty Acid Amide Hydrolase [FAAH], which synthesizes the endocannabinoid anandamide), as well as the anandamide membrane transporter (AMT). Importantly, previous experiments have demonstrated that the endocannabinoid system modulates multiple neurobiological functions, including sleep. For instance, SR141716A (the CB1 cannabinoid receptor antagonist) as well as URB597 (the FAAH inhibitor) increase waking in rats whereas VDM-11 (the blocker of the AMT) enhances sleep in rodents...
December 17, 2016: Neuroscience
https://www.readbyqxmd.com/read/27734700/-the-endocannabinoid-system-and-bone
#20
Mikuláš Pura, Peter Vaňuga
Recent studies suggest an important role for the skeletal endocannabinoid system in the regulation of bone mass in both physiological and pathological conditions. Both major endocannabinoids (anandamid and 2-arachidonoylglycerol), endocannabinoid receptors - CB1-receptor (CB1R) a CB2-receptor (CB2R) and the endocannabinoid metabolizing enzymes are present or expressed in osteoblasts and osteoclasts. Previous studies identified multiple risk and protective variants of CNR2 gene dealing with the relationship to bone density and/or osteoporosis...
2016: Vnitr̆ní Lékar̆ství
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