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https://www.readbyqxmd.com/read/28805944/suppression-of-acute-and-anticipatory-nausea-by-peripherally-restricted-faah-inhibitor-in-animal-models-role-of-ppar%C3%AE-and-cb1-receptors
#1
Erin M Rock, Guillermo Moreno-Sanz, Cheryl L Limebeer, Gavin N Petrie, Roberto Angelini, Daniele Piomelli, Linda A Parker
To evaluate the ability of the peripherally restricted fatty acid amide hydrolase (FAAH) inhibitor, URB937 (cyclohexylcarbamic acid 3'-carbamoyl-6-hydroxybiphenyl-3-yl ester) to suppress acute and anticipatory nausea in rats, and to examine the pharmacological mechanism of such an effect. EXPERIMENTAL APPROACH: We investigated the potential of URB937 to reduce the establishment of lithium chloride (LiCl)-induced conditioned gaping (a model of acute nausea) and to reduce the expression of contextually elicited conditioned gaping (a model of anticipatory nausea) in rats...
August 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28803438/inhibitor-of-endocannabinoid-deactivation-protects-against-in-vitro-and-in-vivo-neurotoxic-effects-of-paraoxon
#2
Karen L G Farizatto, Sara A McEwan, Vinogran Naidoo, Spyros P Nikas, Vidyanand G Shukla, Michael F Almeida, Aaron Byrd, Heather Romine, David A Karanian, Alexandros Makriyannis, Ben A Bahr
The anticholinesterase paraoxon (Pxn) is related to military nerve agents that increase acetylcholine levels, trigger seizures, and cause excitotoxic damage in the brain. In rat hippocampal slice cultures, high-dose Pxn was applied resulting in a presynaptic vulnerability evidenced by a 64% reduction in synapsin IIb (syn IIb) levels, whereas the postsynaptic protein GluR1 was unchanged. Other signs of Pxn-induced cytotoxicity include the oxidative stress-related production of stable 4-hydroxynonenal (4-HNE)-protein adducts...
August 12, 2017: Journal of Molecular Neuroscience: MN
https://www.readbyqxmd.com/read/28803323/effect-of-footshock-stress-on-place-conditioning-produced-by-%C3%AE-9-tetrahydrocannabinol-and-the-fatty-acid-amide-hydrolase-faah-inhibitor-urb597-in-sprague-dawley-rats
#3
Marieka V DeVuono, Kiri L Wills, Danielle V MacPherson, Kelly M Hrelja, Linda A Parker
RATIONALE: Unlike other drugs of abuse, Δ(9)-tetrahydrocanabinol (THC) is generally aversive in rodent conditioned place preference models, but little is known about how stress may modify THC affective properties. OBJECTIVE: We evaluate the potential of footshock stress to enhance the rewarding effects of THC and the fatty acid amide hydrolase inhibitor, URB597, as it has been shown to enhance their anxiolytic effects. MATERIALS AND METHODS: The effect of footshock stress 24 h prior to each conditioning trial on the rewarding/aversive effects of THC (1, 0...
August 12, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28771697/effects-of-centrally-administered-endocannabinoids-and-opioids-on-orofacial-pain-perception-in-rats
#4
Marek Zubrzycki, Anna Janecka, Andreas Liebold, Mechthild Ziegler, Maria Zubrzycka
BACKGROUND AND PURPOSE: Endocannabinoids and opioids play a vital role in mediating pain-induced analgesia. The specific effects of these compounds within orofacial region are largely unknown. In this study we tried to determine whether the increase of cannabinoid and opioid concentration in cerebrospinal fluid affects impulse transmission between the motor centers localized in the vicinity of the third and fourth cerebral ventricles. EXPERIMENTAL APPROACH: The study objectives were realized on rats using the method allowing to record the amplitude of evoked tongue jerks (ETJ) in response to noxious tooth pulp stimulation...
August 3, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28768662/stimulation-of-diuresis-and-natriuresis-by-renomedullary-infusion-of-a-dual-inhibitor-of-fatty-acid-amide-hydrolase-and-monoacylglycerol-lipase
#5
Ashfaq Ahmad, Zdravka Daneva, Guangbi Li, Sara K Dempsey, Ningjun Li, Justin Poklis, Aron Lichtman, Pin-Lan Li, Joseph Kraft Ritter
The renal medulla, considered critical for the regulation of salt and water balance and long-term blood pressure control, is enriched in anandamide and two of its major metabolizing enzymes, cyclooxygenase-2 (COX-2) and fatty acid amide hydrolase (FAAH). Infusion of anandamide (15, 30 and 60 nmol/min/kg) into the renal medulla of C57BL/6J mice stimulated diuresis and salt excretion in a COX-2- but not COX-1-dependent manner. To determine if endogenous endocannabinoids in the renal medulla can elicit similar effects, the effects of intramedullary isopropyl dodecyl fluorophosphate (IDFP), which inhibits the two major endocannabinoid hydrolases, were studied...
August 2, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28756656/targeting-fatty-acid-amide-hydrolase-with-prodrugs-for-cns-selective-therapy
#6
J Matthew Meinig, Skylar J Ferrara, Tania Banerji, Tapasree Banerji, Hannah S Sanford-Crane, Dennis Bourdette, Thomas S Scanlan
The blood-brain barrier (BBB) can be a substantial impediment to achieving therapeutic levels of drugs in the CNS. Certain chemical functionality such as the carboxylic acid is a general liability for BBB permeability preventing significant CNS distribution of a drug from a systemic dose. Here, we report a novel strategy for CNS-selective distribution of the carboxylic acid containing thyromimetic sobetirome using prodrugs targeted to fatty-acid amide hydrolase (FAAH), which is expressed in the brain. Two amide prodrugs of sobetirome were shown to be efficient substrates of FAAH with Vmax/KM values comparable to the natural endocannabinoid FAAH substrate anandamide...
July 30, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28754373/cannabidiol-disrupts-the-consolidation-of-specific-and-generalized-fear-memories-via-dorsal-hippocampus-cb1-and-cb2-receptors
#7
Cristina A J Stern, Thiago R da Silva, Ana M Raymundi, Camila P de Souza, Vinicius A Hiroaki-Sato, Luiza Kato, Francisco S Guimarães, Roberto Andreatini, Reinaldo N Takahashi, Leandro J Bertoglio
Pharmacological interventions able to modulate a fear memory while it is consolidated could have therapeutic value in tempering those maladaptively overconsolidated. Animal and human studies have shown the intensity of unconditioned stimulus delivered during fear conditioning influences qualitative and quantitative aspects of the memory to be established. By varying the shock intensity used for contextual pairing in rats, here we induced specific and more generalized long-term fear memories to investigate whether, how and where in the brain the cannabidiol (CBD; 3...
July 25, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28750800/lipidomics-a-corrective-lens-for-enzyme-myopia
#8
Heather B Bradshaw, Emma Leishman
Classifications and characterizations of specific proteins, such as enzymes, not only allow us to understand biosynthetic and metabolic pathways but they also help to drive our understanding of protein structure and function. How those characterizations are evaluated, however, may change our interpretations and lead us into broader and novel directions in research. Here, we will make the argument that using lipidomics as a tool for characterizing enzymatic function over more traditional toolkit options allows for these types of revelations...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28749428/cannabinoid-receptor-1-and-fatty-acid-amide-hydrolase-contribute-to-operant-sensation-seeking-in-mice
#9
Alexander I Helfand, Christopher M Olsen, Cecilia J Hillard
A large body of evidence in humans and preclinical models supports a role for the endocannabinoid system in the proper execution of motivated or goal-directed behaviors. Operant sensation seeking (OSS) is a task that uses varied sensory stimuli as a reinforcer to maintain operant responding in mice. The purpose of the studies in this report was to begin to explore the role of endocannabinoid signaling in OSS utilizing cannabinoid receptor 1 (CB1R) and fatty acid amide hydrolase (FAAH) knock out mice. Compared to wild type littermate controls, CB1R knock out mice exhibited significantly fewer active responses and earned significantly fewer reinforcers in fixed ratio and progressive ratio schedules...
July 27, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28743542/the-endocannabinoid-system-expression-in-the-female-reproductive-tract-is-modulated-by-estrogen
#10
J Maia, M Almada, A Silva, G Correia-da-Silva, N Teixeira, S I Sá, B M Fonseca
The endocannabinoid system (ECS) is involved in several physiological events that resulted in a growing interest in its modulation. Moreover, the uterine levels of anandamide (AEA), the major endocannabinoid, must be tightly regulated to create proper embryo implantation conditions. However, there are no evidences about the regulation of AEA in uterus by estrogen. Thus, the aim of this study is to elucidate whether estradiol benzoate (EB) and tamoxifen (TAM) administration to ovariectomized (OVX) rats can induce changes in the expression of cannabinoid receptors and AEA-metabolic enzymes in uterus by evaluating gene transcription and protein levels by qPCR, Western blot and immunohistochemistry...
July 22, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28730283/blockade-of-alcohol-escalation-and-relapse-drinking-by-pharmacological-faah-inhibition-in-male-and-female-c57bl-6j-mice
#11
Yan Zhou, Benjamin I Schwartz, Joanna Giza, Steven S Gross, Francis S Lee, Mary Jeanne Kreek
BACKGROUND: Anandamide (AEA)-dependent signaling is regulated by the catabolic enzyme fatty acid amide hydrolase (FAAH). Several lines of evidence have demonstrated that FAAH and AEA are involved in the behavioral effects of alcohol. Therefore, we investigated whether a selective FAAH inhibitor, URB597 (cyclohexylcarbamic acid 3'-[aminocarbonyl]-[1,1'-biphenyl]-3-yl ester), altered alcohol intake in mice in a voluntary alcohol drinking model. METHODS: Mice, subjected to 3 weeks of chronic intermittent access (IA) in a two-bottle choice paradigm with 24-h access every other day, developed rapid escalation of alcohol intake and high preference...
July 20, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28726298/faah-but-not-magl-inhibition-modulates-acute-tlr3-induced-neuroimmune-signaling-in-the-rat-independent-of-sex
#12
Lisa E Flannery, Rebecca J Henry, Daniel M Kerr, David P Finn, Michelle Roche
Toll-like receptor (TLR)3 is a key component of the innate immune response to viral infection. The present study firstly examined whether sex differences exist in TLR3-induced inflammatory, endocrine, and sickness responses. The data revealed that TLR3-induced expression of interferon- or NFkB-inducible genes (IFN-α/β, IP-10, or TNF-α), either peripherally (spleen) or centrally (hypothalamus), did not differ between male and female rats, with the exception of TLR3-induced IFN-α expression in the spleen of female, but not male, rats 8 hr post TLR3 activation...
July 20, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28695708/targeting-fatty-acid-amide-hydrolase-and-transient-receptor-potential-vanilloid-1-simultaneously-to-modulate-colonic-motility-and-visceral-sensation-in-the-mouse-a-pharmacological-intervention-with-n-arachidonoyl-serotonin-aa-5-ht
#13
M Bashashati, J Fichna, F Piscitelli, R Capasso, A A Izzo, A Sibaev, J-P Timmermans, N Cenac, N Vergnolle, V Di Marzo, M Storr
BACKGROUND: Endocannabinoid anandamide (AEA) inhibits intestinal motility and visceral pain, but it may also be proalgesic through transient receptor potential vanilloid-1 (TRPV1). AEA is degraded by fatty acid amide hydrolase (FAAH). This study explored whether dual inhibition of FAAH and TRPV1 reduces diarrhea and abdominal pain. METHODS: Immunostaining was performed on myenteric plexus of the mouse colon. The effects of the dual FAAH/TRPV1 inhibitor AA-5-HT on electrically induced contractility, excitatory junction potential (EJP) and fast (f) and slow (s) inhibitory junction potentials (IJP) in the mouse colon, colonic propulsion and visceromotor response (VMR) to rectal distension were studied...
July 11, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28673548/inhibition-of-the-endocannabinoid-regulating-enzyme-monoacylglycerol-lipase-elicits-a-cb1-receptor-mediated-discriminative%C3%A2-stimulus-in-mice
#14
Robert A Owens, Mohammed A Mustafa, Bogna M Ignatowska-Jankowska, M Imad Damaj, Patrick M Beardsley, Jenny L Wiley, Micah J Niphakis, Benjamin F Cravatt, Aron H Lichtman
Substantial challenges exist for investigating the cannabinoid receptor type 1 (CB1)-mediated discriminative stimulus effects of the endocannabinoids, 2-arachidonoylglycerol (2-AG) and N-arachidonoylethanolamine (anandamide; AEA), compared with exogenous CB1 receptor agonists, such as Δ(9)-tetrahydrocannabinol (THC) and the synthetic cannabinoid CP55,940. Specifically, each endocannabinoid is rapidly degraded by the respective hydrolytic enzymes, monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH)...
June 30, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28667676/cannabinoids-prevent-the-differential-long-term-effects-of-exposure-to-severe-stress-on-hippocampal-and-amygdala-dependent-memory-and-plasticity
#15
Noa Shoshan, Amir Segev, Hila Abush, Tomer Mizrachi Zer-Aviv, Irit Akirav
Exposure to excessive or uncontrolled stress is a major factor associated with various diseases including posttraumatic stress disorder (PTSD). The consequences of exposure to trauma are affected not only by aspects of the event itself, but also by the frequency and severity of trauma reminders. It was suggested that in PTSD, hippocampal-dependent memory is compromised while amygdala-dependent memory is strengthened. Several lines of evidence support the role of the endocannabinoid (eCB) system as a modulator of the stress response...
July 1, 2017: Hippocampus
https://www.readbyqxmd.com/read/28663121/the-effects-of-enhancing-endocannabinoid-signaling-and-blocking-corticotrophin-releasing-factor-receptor-in-the-amygdala-and-hippocampus-on-the-consolidation-of-a-stressful-event
#16
Nurit Aisenberg, Lidia Serova, Esther L Sabban, Irit Akirav
Current clinical and pre-clinical data suggest that both cannabinoid agents and blockage of CRF through corticotrophin releasing factor receptor type 1 (CRFr1) may offer therapeutic benefits for post-traumatic stress disorder (PTSD). Here we aim to determine whether they are more effective when combined when microinjected into the basolateral amygdala (BLA) or CA1 area of the hippocampus after exposure to a stressful event in the shock/reminders rat model for PTSD. Injection of the fatty acid amide hydrolase (FAAH) inhibitor URB597 after the shock into either the BLA or CA1 facilitated extinction, and attenuated startle response and anxiety-like behavior...
June 26, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28660903/finding-fault-with-bial-s-fatal-faah-inhibitor
#17
Asher Mullard
No abstract text is available yet for this article.
June 29, 2017: Nature Reviews. Drug Discovery
https://www.readbyqxmd.com/read/28660730/fatty-acid-amide-hydrolase-faah-inactivation-confers-enhanced-sensitivity-to-nicotine-induced-dopamine-release-in-the-mouse-nucleus-accumbens
#18
Francisco J Pavon, Antonia Serrano, Nimish Sidhpura, Ilham Polis, David Stouffer, Fernando Rodriguez de Fonseca, Benjamin F Cravatt, Rémi Martin-Fardon, Loren H Parsons
Nicotine exerts its rewarding effects by promoting an increase in dopamine (DA) release in the nucleus accumbens (NAc), and this process is influenced by the endocannabinoid system. Fatty acid amide hydrolase (FAAH) is the main enzyme responsible for the degradation of the endocannabinoid anandamide and other non-cannabinoid N-acylethanolamines. Previous research has reported that both genetic deletion and pharmacological inhibition of FAAH enhance nicotine-induced conditioned place preference at low doses...
June 29, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28633967/the-effects-of-chronic-faah-inhibition-on-myocardial-lipid-metabolism-in-normotensive-and-doca-salt-hypertensive-rats
#19
Agnieszka Polak, Ewa Harasim-Symbor, Barbara Malinowska, Irena Kasacka, Anna Pędzińska-Betiuk, Jolanta Weresa, Adrian Chabowski
AIMS: There is significant evidence that the endocannabinoid system (ECS) takes part in the regulation of the cardiovascular system in hypertension. It is quite well established that hypertension causes several changes in the heart metabolism, but it is still unknown whether the ECS affects this process. Therefore, we investigated the influence of prolonged ECS activation on myocardial lipid metabolism in deoxycorticosterone acetate (DOCA)-salt hypertensive rats by chronic fatty acid amide hydrolase (FAAH) inhibition...
August 15, 2017: Life Sciences
https://www.readbyqxmd.com/read/28611585/role-of-n-arachidonoyl-serotonin-aa-5-ht-in-sleep-wake-cycle-architecture-sleep-homeostasis-and-neurotransmitters-regulation
#20
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
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