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https://www.readbyqxmd.com/read/28389107/ceramide-binding-to-anandamide-increases-its-half-life-and-potentiates-its-cytotoxicity-in-human-neuroblastoma-cells
#1
Coralie Di Scala, Morgane Mazzarino, Nouara Yahi, Karine Varini, Nicolas Garmy, Jacques Fantini, Henri Chahinian
Anandamide (AEA) is a ubiquitous lipid that exerts neurotransmitter functions but also controls important biological functions such as proliferation, survival, or programmed cell death. The latter effects are also regulated by ceramide, a lipid enzymatically generated from sphingomyelin hydrolysis by sphingomyelinase. Ceramide has been shown to increase the cellular toxicity of AEA, but the mechanisms controlling this potentiating effect remained unclear. Here we have used a panel of in silico, physicochemical, biochemical and cellular approaches to study the crosstalk between AEA and ceramide apoptotic pathways...
April 4, 2017: Chemistry and Physics of Lipids
https://www.readbyqxmd.com/read/28373843/antihyperalgesic-activities-of-endocannabinoids-in-a-mouse-model-of-antiretroviral-induced-neuropathic-pain
#2
Neha Munawar, Mabayoje A Oriowo, Willias Masocha
Background: Nucleoside reverse transcriptase inhibitors (NRTIs) are the cornerstone of the antiretroviral therapy for human immunodeficiency virus/acquired immune deficiency syndrome (HIV/AIDS). However, their use is sometimes limited by the development of a painful sensory neuropathy, which does not respond well to drugs. Smoked cannabis has been reported in clinical trials to have efficacy in relieving painful HIV-associated sensory neuropathy. Objectives: The aim of this study was to evaluate whether the expression of endocannabinoid system molecules is altered during NRTI-induced painful neuropathy, and also whether endocannabinoids can attenuate NRTI-induced painful neuropathy...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28349993/cannabinoid-receptor-type-1-and-mu-opioid-receptor-polymorphisms-are-associated-with-cyclic-vomiting-syndrome
#3
Andrzej Wasilewski, Urszula Lewandowska, Paula Mosinska, Cezary Watala, Martin Storr, Jakub Fichna, Thangam Venkatesan
OBJECTIVES: Cyclic vomiting syndrome (CVS) is a disorder defined by recurrent, unexplained episodes of severe nausea and vomiting. Our aim was to investigate whether CVS and pathophysiological mechanisms underlying this condition are associated with selected variations in genes encoding the components of the endogenous cannabinoid and opioid systems. METHODS: This case-control study included 65 patients with CVS-16 male and 49 female, and 1,092 healthy controls-525 male and 567 female from the 1000 Genomes Project...
March 28, 2017: American Journal of Gastroenterology
https://www.readbyqxmd.com/read/28291580/restored-plasma-anandamide-and-endometrial-expression-of-fatty-acid-amide-hydrolase-in-women-with-polycystic-ovary-syndrome-by-the-combination-use-of-diane-35-and-metformin
#4
Na Cui, Xiaoye Feng, Zhiming Zhao, Jie Zhang, Yueming Xu, Luning Wang, Guimin Hao
PURPOSE: Polycystic ovary syndrome (PCOS) is a metabolic and endocrinal disorder affecting a number of women of reproductive age. We aimed to reveal the correlation between the endocannabinoid system and PCOS, which may provide a new therapeutic target for PCOS treatment. METHODS: Serum levels of anandamide and 2-arachidonoylglycerol andexpression of cannabinoid receptors and fatty acid amide hydrolase (FAAH) in the endometrium were compared between women with PCOS and infertile women without PCOS, as well as women with PCOS before and after treatment with Diane-35 and metformin...
March 10, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28267914/activity-based-protein-profiling-leads-to-identification-of-novel-protein-targets-for-nerve-agent-vx
#5
Dan Carmany, Andrew J Walz, Fu-Lian Hsu, Bernard Benton, David Burnett, Jennifer Gibbons, Daan Noort, Trevor Glaros, Jennifer W Sekowski
Organophosphorus (OP) nerve agents continue to be a threat at home and abroad during the war against terrorism. Human exposure to nerve agents such as VX results in a cascade of toxic effects relative to the exposure level including ocular miosis, excessive secretions, convulsions, seizures, and death. The primary mechanism behind these overt symptoms is the disruption of cholinergic pathways. While much is known about the primary toxicity mechanisms of nerve agents, there remains a paucity of information regarding impacts on other pathways and systemic effects...
March 16, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28254462/fatty-acid-amide-hydrolase-inhibitor-treatment-in-men-with-chronic-prostatitis-chronic-pelvic-pain-syndrome-an-adaptive-double-blind-randomized-controlled-trial
#6
Florian M E Wagenlehner, J W Olivier van Till, Jos G A Houbiers, Reynaldo V Martina, Dirk P Cerneus, Joost H J M Melis, Antoni Majek, Egils Vjaters, Michael Urban, Henrikas Ramonas, Daniel A Shoskes, J Curtis Nickel
OBJECTIVE: To examine the effect of a peripherally active fatty acid amide hydrolase (FAAH) inhibitor ASP3652 on safety and efficacy outcomes in chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS). Inhibition of FAAH is hypothesized to reduce the excitability of urinary tract afferents including nociceptors. MATERIALS AND METHODS: In this adaptive, randomized, double-blind, placebo-controlled study, adult male patients with moderate to severe CP/CPPS were treated for 12 weeks with an oral dose of ASP3652 (25, 75, 150, or 300 mg twice daily, or 300 mg once daily), or placebo...
February 27, 2017: Urology
https://www.readbyqxmd.com/read/28243972/genetic-interaction-of-dgat2-and-faah-in-the-development-of-human-obesity
#7
Tinglu Ning, Yaoyu Zou, Minglan Yang, Qianqian Lu, Maopei Chen, Wen Liu, Shaoqian Zhao, Yingkai Sun, Juan Shi, Qinyun Ma, Jie Hong, Ruixin Liu, Jiqiu Wang, Guang Ning
PURPOSE: DGAT2 is the critical catalyzing enzyme for triglyceride biosynthesis, and excess triglyceride accumulation in fat tissues is a fundamental process for obesity. Mutations in DGAT2 or other genes interacting with DGAT2 associated with adiposity have not been reported in human to date. METHODS: DGAT2 mutation was identified based on our in-home database-exome sequencing 227 young obese subjects (body-mass index (BMI), 35.1-61.7 kg/m(2)) and 219 lean controls (BMI, 17...
February 27, 2017: Endocrine
https://www.readbyqxmd.com/read/28240187/the-endocannabinoid-system-modulating-levels-of-consciousness-emotions-and-likely-dream-contents
#8
Eric Murillo-Rodriguez, José Carlos Pastrana-Trejo, Mireille Salas-Crisóstomo, Miriel de-la-Cruz
Cannabinoids are derivatives that are either compounds occurring naturally in the plant, Cannabis sativa or synthetic analogs of these molecules. The first and most widely investigated of the cannabinoids is ∆9-tetrahydrocannabinol (Δ9-THC), which is the main psychotropic constituent of cannabis and undergoes significant binding to cannabinoid receptors. These cannabinoid receptors are seven-transmembrane receptors that received their name from the fact that they respond to cannabinoid compounds, including Δ9-THC...
February 23, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28237711/pharmacological-inhibition-of-faah-modulates-tlr-induced-neuroinflammation-but-not-sickness-behaviour-an-effect-partially-mediated-by-central-trpv1
#9
Rebecca J Henry, Daniel M Kerr, Lisa E Flannery, Marykate Killilea, Edel M Hughes, Louise Corcoran, David P Finn, Michelle Roche
Aberrant activation of toll-like receptors (TLRs), key components of the innate immune system, has been proposed to underlie and exacerbate a range of central nervous system disorders. Increasing evidence supports a role for the endocannabinoid system in modulating inflammatory responses including those mediated by TLRs, and thus this system may provide an important treatment target for neuroinflammatory disorders. However, the effect of modulating endocannabinoid tone on TLR-induced neuroinflammation in vivo and associated behavioural changes is largely unknown...
February 22, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28209423/constitutive-increases-in-amygdalar-corticotropin-releasing-factor-and-fatty-acid-amide-hydrolase-drive-an-anxious-phenotype
#10
Luis A Natividad, Matthew W Buczynski, Melissa A Herman, Dean Kirson, Christopher S Oleata, Cristina Irimia, Ilham Polis, Roberto Ciccocioppo, Marisa Roberto, Loren H Parsons
BACKGROUND: Corticotropin-releasing factor (CRF) mediates anxiogenic responses by activating CRF type 1 (CRF1) receptors in limbic brain regions. Anxiety is further modulated by the endogenous cannabinoid (eCB) system that attenuates the synaptic effects of stress. In the amygdala, acute stress activates the enzymatic clearance of the eCB N-arachidonoylethanolamine via fatty acid amide hydrolase (FAAH), although it is unclear whether chronic dysregulation of CRF systems induces maladaptive changes in amygdalar eCB signaling...
January 13, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28193523/faah-inhibition-produces-antidepressant-like-efforts-of-mice-to-acute-stress-via-synaptic-long-term-depression
#11
Ying Wang, Xia Zhang
Recent studies have shown that inhibition of fatty acid amide hydrolase (FAAH), the major degradative enzyme of the endocannabinoid N-arachidonoylethanolamine (AEA), produced antidepressant behavioral responses, but its underlying mechanism is not clear. Here we find that a systemic administration of the FAAH inhibitor PF3845 or an intra-CA1 application of AEA elicits an in vivo long-term depression (LTD) at excitatory glutamatergic CA3-CA1 synapses of the hippocampus. The PF3845- and/or AEA-elicited LTD are abolished by the LTD-blocking peptide Tat-GluR2...
May 1, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28192193/differential-expression-of-endocannabinoid-system-related-genes-in-the-dorsal-hippocampus-following-expression-and-reinstatement-of-morphine-conditioned-place-preference-in-mice
#12
Wei Li, Cong-Li Zhang, Zheng-Guo Qiu
The endocannabinoid signaling plays a critical role in mediating rewarding effects to morphine. The relative stability for the expression and reinstatement of morphine conditioned place preference (CPP) suggests the involvement of differential neuroadaptations in learned associations between environmental cues and morphine. Changes in gene expression in hippocampus through the endogenous cannabinoid system (eCB) may accompany and mediate the development of such neuroadaptations to repeated morphine stimulation...
March 16, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28182408/design-synthesis-structure-activity-relationship-studies-and-three-dimensional-quantitative-structure-activity-relationship-3d-qsar-modeling-of-a-series-of-o-biphenyl-carbamates-as-dual-modulators-of-dopamine-d3-receptor-and-fatty-acid-amide-hydrolase
#13
Alessio De Simone, Debora Russo, Gian Filippo Ruda, Alessandra Micoli, Mariarosaria Ferraro, Rita Maria Concetta Di Martino, Giuliana Ottonello, Maria Summa, Andrea Armirotti, Tiziano Bandiera, Andrea Cavalli, Giovanni Bottegoni
We recently reported molecules designed according to the multitarget-directed ligand paradigm to exert combined activity at human fatty acid amide hydrolase (FAAH) and dopamine receptor subtype D3 (D3R). Both targets are relevant for tackling several types of addiction (most notably nicotine addiction) and other compulsive behaviors. Here, we report an SAR exploration of a series of biphenyl-N-[4-[4-(2,3-substituted-phenyl)piperazine-1-yl]alkyl]carbamates, a novel class of molecules that had shown promising activities at the FAAH-D3R target combination in preliminary studies...
March 2, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28157650/urb597-reduces-biochemical-behavioral-and-morphological-alterations-in-two-neurotoxic-models-in-rats
#14
Marisol Maya-López, Hipolito A Ruiz-Contreras, María de Jesús Negrete-Ruíz, Julián Elías Martínez-Sánchez, Juan Benítez-Valenzuela, Ana Laura Colín-González, Juana Villeda-Hernández, Laura Sánchez-Chapul, Carmen Parra-Cid, Edgar Rangel-López, Abel Santamaría
BACKGROUND: URB597 is a compound largely linked to the inhibition of fatty acid amide hydrolase (FAAH), an enzyme responsible for the metabolic degradation of the endocannabinoid anandamide (AEA). Despite this pharmacological property accounts for its modulatory profile demonstrated in some neurotoxic paradigms, the possible protective properties of this agent have been poorly investigated, and deserve exploration in different neurotoxic models. In this study, we explored the effects of URB597 on oxidative damage to lipids and other major endpoints of toxicity in two neurotoxic models in vivo in rats (the first one produced by the mitochondrial neurotoxin 3-nitropropionic acid [3-NP], and the other generated by the striatal injection of the pro-oxidant toxin 6-hydroxidopamine [6-OHDA]) in order to provide further supporting evidence of its modulatory profile...
April 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28155016/power-of-screening-tests-for-colorectal-cancer-enhanced-by-high-levels-of-m2-pk-in-addition-to-fobt
#15
Cristina Zaccaro, Ilaria Maria Saracino, Giulia Fiorini, Natale Figura, John Holton, Valentina Castelli, Valeria Pesci, Luigi Gatta, Dino Vaira
Colorectal cancer (CRC) is a multistep process that involves adenoma-carcinoma sequence. CRC can be prevented by routine screening, which can detect precancerous lesions. The aim of this study is to clarify whether faecal occult blood test (i-FOBT), tumor M2 pyruvate kinase (t-M2-PK), and endocannabinoid system molecules (cannabinoid receptors type 1-CB1, type 2-CB2, and fatty acid amide hydrolase-FAAH) might represent better diagnostic tools, alone or in combination, for an early diagnosis of CRC. An immunochemical FOB test (i-FOBT) and quantitative ELISA stool test for t-M2-PK were performed in 127 consecutive patients during a 12 month period...
February 2, 2017: Internal and Emergency Medicine
https://www.readbyqxmd.com/read/28150397/severity-of-alcohol-dependence-is-associated-with-the-fatty-acid-amide-hydrolase-pro129thr-missense-variant
#16
Matthew E Sloan, Joshua L Gowin, Jia Yan, Melanie L Schwandt, Primavera A Spagnolo, Hui Sun, Colin A Hodgkinson, David Goldman, Vijay A Ramchandani
The endocannabinoid system plays an important role in reward and addiction. One of the two main endocannabinoid neurotransmitters, anandamide, is metabolized by fatty acid amide hydrolase, an enzyme with a functional genetic polymorphism (FAAH Pro129Thr, rs324420). The Thr129 allele has been linked to problem drug and alcohol use, but the association has not been widely replicated and may be stronger for clinical measures of severity rather than categorical diagnosis. In the present study, we sought to determine whether the Thr129 allele was associated with both alcohol dependence (AD) diagnosis and severity in a sample of 1434 European American and African American individuals, 952 of whom were diagnosed with lifetime AD...
February 1, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28148494/upregulation-of-fatty-acid-amide-hydrolase-faah-in-the-dorsal-periaqueductal-gray-is-associated-with-neuropathic-pain-and-reduced-heart-rate-in-rats
#17
Caron Dean, Cecilia J Hillard, Jeanne L Seagard, Francis A Hopp, Quinn H Hogan
Nerve damage can induce a heightened pain response to noxious stimulation, which is termed hyperalgesia. Pain itself acts as a stressor, initiating autonomic and sensory effects through the dorsal periaqueductal gray (dPAG) to induce both sympathoexcitation and analgesia, which prior studies have shown to be affected by endocannabinoid signaling. The present study addressed the hypothesis that neuropathic pain disrupts autonomic and analgesic regulation by endocannabinoid signaling in the dPAG. Endocannabinoid contents, transcript levels of endocannabinoid signaling components, and catabolic enzyme activity were analyzed in the dPAG of rats at 21 days after painful nerve injury...
February 1, 2017: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/28147243/song-associated-reward-correlates-with-endocannabinoid-related-gene-expression-in-male-european-starlings-sturnus-vulgaris
#18
Allison H Hahn, Devin P Merullo, Jeremy A Spool, Caroline S Angyal, Sharon A Stevenson, Lauren V Riters
Vocal communication is required for successful social interactions in numerous species. During the breeding season, songbirds produce songs that are reinforced by behavioral consequences (e.g., copulation). However, some songbirds also produce songs not obviously directed at other individuals. The consequences maintaining or reinforcing these songs are less obvious and the neural mechanisms associated with undirected communication are not well-understood. Previous studies indicate that undirected singing is intrinsically rewarding and mediated by opioid or dopaminergic systems; however, endocannabinoids are also involved in regulating reward and singing behavior...
March 27, 2017: Neuroscience
https://www.readbyqxmd.com/read/28132572/decreased-expression-of-fatty-acid-amide-hydrolase-in-women-with-polycystic-ovary-syndrome
#19
Na Cui, Yang Yang, Yueming Xu, Jie Zhang, Lei Jiang, Guimin Hao
This study aimed to investigate the correlation between endocannabinoids and polycystic ovary syndrome (PCOS), and the expression levels of endocannabinoids in different phases of menstruation. The expression of cannabinoid receptors (CB1) and fatty acid amide hydrolase (FAAH) in the endometrium were immunohistochemically stained and compared between women with PCOS and the control group. Integrated optical density (IOD) was assessed to analyze their expression levels. The CB1 and FAAH were expressed in endometrial epithelial cytoplasm...
January 28, 2017: Gynecological Endocrinology
https://www.readbyqxmd.com/read/28129982/specificity-and-mechanism-of-mandelamide-hydrolase-catalysis
#20
S A Adediran, Pan-Fen Wang, Abbas G Shilabin, Charles A Baron, Michael J McLeish, R F Pratt
The best-studied amidase signature (AS) enzyme is probably fatty acid amide hydrolase (FAAH). Closely related to FAAH is mandelamide hydrolase (MAH), whose substrate specificity and mechanism of catalysis are described in this paper. First, we developed a convenient chromogenic substrate, 4-nitrophenylacetamide, for MAH. The lack of reactivity of MAH with the corresponding ethyl ester confirmed the very limited size of the MAH leaving group site. The reactivity of MAH with 4-nitrophenyl acetate and methyl 4-nitrophenyl carbonate, therefore, suggested formation of an "inverse" acyl-enzyme where the small acyl-group occupies the normal leaving group site...
January 24, 2017: Archives of Biochemistry and Biophysics
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