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Anandamide

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https://www.readbyqxmd.com/read/28632393/the-antinociceptive-agent-sbfi-26-binds-to-anandamide-transporters-fabp5-and-fabp7-at-two-different-sites
#1
Hao-Chi Hsu, Simon Tong, Yuchen Zhou, Matthew W Elmes, Su Yan, Martin Kaczocha, Dale G Deutsch, Robert C Rizzo, Iwao Ojima, Huilin Li
Human FABP5 and FABP7 are intracellular endocannabinoid transporters. SBFI-26 is an -truxillic acid 1-naphthyl monoester that competitively inhibits the activities of FABP5 and FABP7 and produces antinociceptive and anti-inflammatory effects in mice. The synthesis of SBFI-26 yields several stereoisomers, and it is not known how the inhibitor binds the transporters. Here we report co-crystal structures of SBFI-26 in complex with human FABP5 and FABP7 at a resolution of 2.2 Å and 1.9 Å, respectively. We found that only (S)-SBFI-26 was present in the crystal structures...
June 20, 2017: Biochemistry
https://www.readbyqxmd.com/read/28625856/nitroglycerin-increases-serotonin-transporter-expression-in-rat-spinal-cord-but-anandamide-modulated-this-effect
#2
Gábor Nagy-Grócz, Zsuzsanna Bohár, Annamária Fejes-Szabó, Klaudia Flóra Laborc, Eleonóra Spekker, Lilla Tar, László Vécsei, Árpád Párdutz
Migraine is one of the most prevalent neurological diseases, which affects 16% of the total population. The exact pathomechanism of this disorder is still not well understood, but it seems that serotonin and its transporter have a crucial role in the pathogenesis. One of the animal models of migraine is the systemic administration of nitroglycerin (NTG), a nitric oxide (NO) donor. NO can initiate a central sensitization process in the trigeminal system, which is also present in migraineurs. Recent studies showed that the endocannabinoid system has a modulatory role on the trigeminal activation and sensitization...
June 15, 2017: Journal of Chemical Neuroanatomy
https://www.readbyqxmd.com/read/28611591/metabolism-of-the-endocannabinoid-anandamide-open-questions-after-25-years
#3
REVIEW
Mauro Maccarrone
Cannabis extracts have been used for centuries, but its main active principle ∆(9)-tetrahydrocannabinol (THC) was identified about 50 years ago. Yet, it is only 25 years ago that the first endogenous ligand of the same receptors engaged by the cannabis agents was discovered. This "endocannabinoid (eCB)" was identified as N-arachidonoylethanolamine (or anandamide (AEA)), and was shown to have several receptors, metabolic enzymes and transporters that altogether drive its biological activity. Here I report on the latest advances about AEA metabolism, with the aim of focusing open questions still awaiting an answer for a deeper understanding of AEA activity, and for translating AEA-based drugs into novel therapeutics for human diseases...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28611585/role-of-n-arachidonoyl-serotonin-aa-5-ht-in-sleep-wake-cycle-architecture-sleep-homeostasis-and-neurotransmitters-regulation
#4
Eric Murillo-Rodríguez, Vincenzo Di Marzo, Sergio Machado, Nuno B Rocha, André B Veras, Geraldo A M Neto, Henning Budde, Oscar Arias-Carrión, Gloria Arankowsky-Sandoval
The endocannabinoid system comprises several molecular entities such as endogenous ligands [anandamide (AEA) and 2-arachidonoylglycerol (2-AG)], receptors (CB1 and CB2), enzymes such as [fatty acid amide hydrolase (FAHH) and monoacylglycerol lipase (MAGL)], as well as the anandamide membrane transporter. Although the role of this complex neurobiological system in the sleep-wake cycle modulation has been studied, the contribution of the blocker of FAAH/transient receptor potential cation channel subfamily V member 1 (TRPV1), N-arachidonoyl-serotonin (AA-5-HT) in sleep has not been investigated...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28584105/chemical-probes-to-potently-and-selectively-inhibit-endocannabinoid-cellular-reuptake
#5
Andrea Chicca, Simon Nicolussi, Ruben Bartholomäus, Martina Blunder, Alejandro Aparisi Rey, Vanessa Petrucci, Ines Del Carmen Reynoso-Moreno, Juan Manuel Viveros-Paredes, Marianela Dalghi Gens, Beat Lutz, Helgi B Schiöth, Michael Soeberdt, Christoph Abels, Roch-Philippe Charles, Karl-Heinz Altmann, Jürg Gertsch
The extracellular effects of the endocannabinoids anandamide and 2-arachidonoyl glycerol are terminated by enzymatic hydrolysis after crossing cellular membranes by facilitated diffusion. The lack of potent and selective inhibitors for endocannabinoid transport has prevented the molecular characterization of this process, thus hindering its biochemical investigation and pharmacological exploitation. Here, we report the design, chemical synthesis, and biological profiling of natural product-derived N-substituted 2,4-dodecadienamides as a selective endocannabinoid uptake inhibitor...
June 20, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28583049/n-arachidonoyl-serotonin-a-dual-faah-and-trpv1-blocker-inhibits-the-retrieval-of-contextual-fear-memory-role-of-the-cannabinoid-cb1-receptor-in-the-dorsal-hippocampus
#6
Pedro H Gobira, Isabel V Lima, Luara A Batista, Antônio C de Oliveira, Leonardo B Resstel, Carsten T Wotjak, Daniele C Aguiar, Fabricio A Moreira
Anandamide, an endocannabinoid, inhibits aversive responses by activating the CB1 cannabinoid receptor. At high concentrations, however, anandamide may exert pro-aversive activities mediated by the transient receptor potential vanilloid type-1 channel (TRPV1). Accordingly, N-arachidonoyl-serotonin (AA-5-HT), a dual blocker of the anandamide-hydrolysing enzyme fatty acid amide hydrolase (FAAH) and the TRPV1 channel, induces anxiolytic-like effects. Here we tested the hypothesis that AA-5-HT inhibits the expression of contextual fear conditioning by facilitating CB1 receptor signalling in the dorsal hippocampus of mice...
June 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28579186/endocannabinoid-modulation-of-homeostatic-and-non-homeostatic-feeding-circuits
#7
REVIEW
Benjamin K Lau, Daniela Cota, Luigia Cristino, Stephanie L Borgland
The endocannabinoid system has emerged as a key player in the control of eating. Endocannabinoids, including 2-arachidonoylglycerol (2-AG) and anandamide (AEA), modulate neuronal activity via cannabinoid 1 receptors (CB1Rs) in multiple nuclei of the hypothalamus to induce or inhibit food intake depending on nutritional and hormonal status, suggesting that endocannabinoids may act in the hypothalamus to integrate different types of signals informing about the animal's energy needs. In the mesocorticolimbic system, (endo)cannabinoids modulate synaptic transmission to promote dopamine release in response to palatable food...
June 1, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28577869/polyunsaturated-fatty-acids-differentially-modulate-cell-proliferation-and-endocannabinoid-system-in-two-human-cancer-lines
#8
Repossi Gastón, Pasqualini María Eugenia, Undurti N Das, Aldo R Eynard
BACKGROUND AND AIMS: Evidence suggests that quantity and quality of dietary polyunsaturated fatty acids (PUFAs) play a role in the development of cancer. However, the mechanisms involved in this interaction(s) are not clear. Endocannabinoids are lipid metabolites known to have growth modulatory actions. We studied the effect of supplementation with PUFAs ω-6 and ω-3 (essential fatty acids, EFAs), saturated and monounsaturated fatty acids (non-EFAs) on the growth of tumor cells and modifications in their endocannabinoid content...
January 2017: Archives of Medical Research
https://www.readbyqxmd.com/read/28570479/sensitization-of-c-fiber-nociceptors-in-mice-with-sickle-cell-disease-is-decreased-by-local-inhibition-of-anandamide-hydrolysis
#9
Megan L Uhelski, Kalpna Gupta, Donald A Simone
Chronic pain and hyperalgesia, as well as pain resulting from episodes of vasoocclusion, are characteristic features of sickle cell disease (SCD) and are difficult to treat. Since there is growing evidence that increasing local levels of endocannabinoids can decrease hyperalgesia, we examined the effects of URB597, a fatty acid amide hydrolase (FAAH) inhibitor which blocks the hydrolysis of the endogenous cannabinoid anandamide (AEA), on hyperalgesia and sensitization of cutaneous nociceptors in a humanized mouse model of SCD...
May 31, 2017: Pain
https://www.readbyqxmd.com/read/28554848/sex-and-hormone-dependent-alterations-in-alcohol-withdrawal-induced-anxiety-and-corticolimbic-endocannabinoid-signaling
#10
Angela M Henricks, Anthony L Berger, Janelle M Lugo, Lydia N Baxter-Potter, Kennedy V Bieniasz, Gavin Petrie, Martin A Sticht, Matthew N Hill, Ryan J McLaughlin
Alcohol dependence is associated with anxiety during withdrawal. The endocannabinoid (ECB) system participates in the neuroendocrine and behavioral response to stress and changes in corticolimbic ECB signaling may contribute to alcohol withdrawal-induced anxiety. Moreover, symptoms of alcohol withdrawal differ between sexes and sexual dimorphism in withdrawal-induced ECB recruitment may be a contributing factor. Herein, we exposed intact male and female rats and ovariectomized (OVX) female rats with or without estradiol (E2) replacement to 6 weeks of chronic intermittent alcohol vapor and measured anxiety-like behavior, ECB content, and ECB-related mRNA in the basolateral amygdala (BLA) and ventromedial prefrontal cortex (vmPFC)...
May 26, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28554529/maternal-alcohol-exposure-during-mid-pregnancy-dilates-fetal-cerebral-arteries-via-endocannabinoid-receptors
#11
Olga Seleverstov, Ana Tobiasz, J Scott Jackson, Ryan Sullivan, Dejian Ma, J Pierce Sullivan, Steven Davison, Yada Akkhawattanangkul, Danielle L Tate, Terry Costello, Stacey Barnett, Wei Li, Giancarlo Mari, Alex M Dopico, Anna N Bukiya
Prenatal alcohol exposure often results in fetal alcohol syndrome and fetal alcohol spectrum disorders. Mechanisms of fetal brain damage by alcohol remain unclear. We used baboons (Papio spp.) to study alcohol-driven changes in the fetal cerebral artery endocannabinoid system. Pregnant baboons were subjected to binge alcohol exposure via gastric infusion three times during a period equivalent to the second trimester of human pregnancy. A control group was infused with orange-flavored drink that was isocaloric to the alcohol-containing solution...
June 2017: Alcohol
https://www.readbyqxmd.com/read/28554131/protective-role-of-the-novel-hybrid-3-5-dipalmitoyl-nifedipine-in-a-cardiomyoblast-culture-subjected-to-simulated-ischemia-reperfusion
#12
Eduarda Santa-Helena, Stefanie Teixeira, Micheli Rosa de Castro, Diego da Costa Cabrera, Caroline Da Ros Montes D'Oca, Marcelo G Montes D'Oca, Ana Paula S Votto, Luiz Eduardo Maia Nery, Carla Amorim Neves Gonçalves
This work investigated the acute effects of the calcium channel blocker nifedipine and its new fatty hybrid derived from palmitic acid, 3,5-dipalmitoyl-nifedipine, compared to endocannabinoid anandamide during the process of inducing ischemia and reperfusion in cardiomyoblast H9c2 heart cells. The cardiomyoblasts were treated in 24 or 96-well plates (according to the test being performed) and maintaining the treatment until the end of hypoxia induction. The molecules were tested at concentrations of 10 and 100μM, cells were treated 24h after assembling the experimental plates and immediately before the I/R...
May 26, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28535469/novel-propanamides-as-fatty-acid-amide-hydrolase-inhibitors
#13
Alessandro Deplano, Carmine Marco Morgillo, Monica Demurtas, Emmelie Björklund, Mariateresa Cipriano, Mona Svensson, Sanaz Hashemian, Giovanni Smaldone, Emilia Pedone, F Javier Luque, Maria G Cabiddu, Ettore Novellino, Christopher J Fowler, Bruno Catalanotti, Valentina Onnis
Fatty acid amide hydrolase (FAAH) has a key role in the control of the cannabinoid signaling, through the hydrolysis of the endocannabinoids anandamide and in some tissues 2-arachidonoylglycerol. FAAH inhibition represents a promising strategy to activate the cannabinoid system, since it does not result in the psychotropic and peripheral side effects characterizing the agonists of the cannabinoid receptors. Here we present the discovery of a novel class of profen derivatives, the N-(heteroaryl)-2-(4-((2-(trifluoromethyl)pyridin-4-yl)amino)phenyl)propanamides, as FAAH inhibitors...
May 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28529018/effects-of-anandamide-administration-on-components-of-reward-processing-during-free-choice
#14
Luke C Zona, Benjamin R Fry, Jacob A LaLonde, Howard C Cromwell
Previous research has implicated the positive modulation of anandamide, an endocannabinoid neurotransmitter, on feeding behavior. Anandamide is particularly noteworthy as it acts as an endogenous ligand of the CB1 receptor, the same receptor that is activated by tetrahydrocannabinol, the primary psychoactive component in Cannabis sativa. Cannabis legalization in North America has presented with a need to study endocannabinoid agonists and their effects on behavior. Much has yet to be determined in terms of the role of the endocannabinoid system in decision-making scenarios...
July 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28522407/high-throughput-screening-and-bioinformatic-analysis-to-ascertain-compounds-that-prevent-saturated-fatty-acid-induced-%C3%AE-cell-apoptosis
#15
Seung-Hee Lee, Daniel Cunha, Carlo Piermarocchi, Giovanni Paternostro, Anthony Pinkerton, Laurence Ladriere, Piero Marchetti, Decio L Eizirik, Miriam Cnop, Fred Levine
Pancreatic β-cell lipotoxicity is a central feature of the pathogenesis of type 2 diabetes. To study the mechanism by which fatty acids cause β-cell death and develop novel approaches to prevent it, a high-throughput screen on the β-cell line INS1 was carried out. The cells were exposed to palmitate to induce cell death and compounds that reversed palmitate-induced cytotoxicity were ascertained. Hits from the screen were analyzed by an increasingly more stringent testing funnel, ending with studies on primary human islets treated with palmitate...
May 15, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28515018/plasma-levels-of-the-endocannabinoid-anandamide-related-n-acylethanolamines-and-linoleic-acid-derived-oxylipins-in-patients-with-migraine
#16
Sandra Gouveia-Figueira, Kristina Goldin, Sanaz A Hashemian, Agneta Lindberg, Monica Persson, Malin L Nording, Katarina Laurell, Christopher J Fowler
There is evidence that patients with migraine have deficient levels of the endogenous cannabinoid receptor ligand anandamide (AEA). It is not known, however, if this is a localised or generalised phenomenon. In the present study, levels of AEA, related N-acylethanolamines (NAEs) and linoleic acid-derived oxylipins have been measured in the blood of 26 healthy women and 38 women with migraine (26 with aura, 12 without aura) who were matched for age and body-mass index. Blood samples were taken on two occasions: the first sample near the start of the menstrual cycle (when present) and the second approximately fourteen days later...
May 2017: Prostaglandins, Leukotrienes, and Essential Fatty Acids
https://www.readbyqxmd.com/read/28499834/n-stearoyltyrosine-protects-primary-cortical-neurons-against-oxygen-glucose-deprivation-induced-apoptosis-through-inhibiting-anandamide-inactivation-system
#17
Heng-Jing Cui, Sha Liu, Rui Yang, Guo-Hui Fu, Yang Lu
N-stearoylthrosine (NST), a synthesized anandamide (AEA) analogue, plays a neuroprotective role in neurodegenerative diseases and cerebrovascular diseases. Several studies have demonstrated that the endocannabinoids systems (ECS) are involved in the neuroprotective effects against cerebral ischemic injury. Oxygen-glucose deprivation (OGD)-induced neuronal injury elevated the levels of endocannabinoids and activated ECS. This research was conducted to investigate the neuroprotective effect of NST against OGD-induced neuronal injury in cultured primary cortical neurons and the potential mechanism involved...
May 9, 2017: Neuroscience Research
https://www.readbyqxmd.com/read/28479394/ampk-contributes-to-aerobic-exercise-induced-antinociception-downstream-of-endocannabinoids
#18
Tanya S King-Himmelreich, Christine V Möser, Miriam C Wolters, Julia Schmetzer, Yannik Schreiber, Nerea Ferreirós, Otto Q Russe, Gerd Geisslinger, Ellen Niederberger
Physical exercise has been repeatedly associated with decreased nociceptive responses but the underlying mechanisms have still not been fully clarified. In this study, we investigated exercise-induced effects after a single bout of treadmill running on the mouse model of formalin-induced inflammatory nociception. As potential molecular mediators, we focused on endogenous endocannabinoids as well as AMP-activated protein kinase (AMPK). Our results showed that wild type mice display a reduced nociceptive response in the formalin test after treadmill running, while exercise had no effect on inflammatory nociception in AMPKα2 knockout mice...
May 4, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28478955/spatial-distribution-of-cannabinoid-receptor-1-and-fatty-acid-amide-hydrolase-in-the-cat-ovary-and-oviduct
#19
Andrea Pirone, Carla Lenzi, Angela Briganti, Francesco Abbate, Maria Levanti, Francesca Abramo, Vincenzo Miragliotta
Involvement of the endocannabinoid system in female reproduction has been extensively described in humans with the cognate receptors and ligands being found in the ovaries and genital tract. In human, an imbalance of the endocannabinoid system is linked with both ectopic pregnancy and infertility. In bovine species anandamide levels regulate aspects of sperm-oviduct interaction. Here we report the immunohistochemical distribution of cannabinoid receptor 1 (CB1R) and fatty acid amide hydrolase (FAAH) in cat ovary and oviduct, using paraffin-embedded tissue samples and commercially available antibodies...
May 4, 2017: Acta Histochemica
https://www.readbyqxmd.com/read/28476070/peripheral-inflammation-affects-modulation-of-nociceptive-synaptic-transmission-in-the-spinal-cord-induced-by-n-arachidonoylphosphatidylethanolamine
#20
Vladimir Nerandzic, Petra Mrozkova, Pavel Adamek, Diana Spicarova, Istvan Nagy, Jiri Palecek
BACKGROUND AND PURPOSE: Endocannabinoids play an important role in modulating spinal nociceptive signalling, crucial for the development of pain. The cannabinoid CB1 receptor and the TRPV1 cation channel are both activated by the endocannabinoid anandamide, a product of biosynthesis from the endogenous lipid precursor N-arachidonoylphosphatidylethanolamine (20:4-NAPE). Here, we report CB1 receptor- and TRPV1-mediated effects of 20:4-NAPE on spinal synaptic transmission in control and inflammatory conditions...
May 5, 2017: British Journal of Pharmacology
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