keyword
MENU ▼
Read by QxMD icon Read
search

FAAH

keyword
https://www.readbyqxmd.com/read/28209423/constitutive-increases-in-amygdalar-corticotropin-releasing-factor-and-fatty-acid-amide-hydrolase-drive-an-anxious-phenotype
#1
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
#2
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...
February 10, 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
#3
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...
February 10, 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
#4
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 multi-target-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...
February 9, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28157650/urb597-reduces-biochemical-behavioral-and-morphological-alterations-in-two-neurotoxic-models-in-rats
#5
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...
January 31, 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
#6
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
#7
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
#8
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
#9
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...
January 29, 2017: Neuroscience
https://www.readbyqxmd.com/read/28132572/decreased-expression-of-fatty-acid-amide-hydrolase-in-women-with-polycystic-ovary-syndrome
#10
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
#11
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
https://www.readbyqxmd.com/read/28114819/n-aryl-2-aryloxyacetamides-as-a-new-class-of-fatty-acid-amide-hydrolase-faah-inhibitors
#12
Naresh Sunduru, Mona Svensson, Mariateresa Cipriano, Sania Marwaha, C David Andersson, Richard Svensson, Christopher J Fowler, Mikael Elofsson
Fatty acid amide hydrolase (FAAH) is a promising target for the development of drugs to treat neurological diseases. In search of new FAAH inhibitors, we identified 2-(4-cyclohexylphenoxy)-N-(3-(oxazolo[4,5-b]pyridin-2-yl)phenyl)acetamide, 4g, with an IC50 of 2.6 µM as a chemical starting point for the development of potent FAAH inhibitors. Preliminary hit-to-lead optimisation resulted in 2-(4-phenylphenoxy)-N-(3-(oxazolo[4,5-b]pyridin-2-yl)phenyl)acetamide, 4i, with an IC50 of 0.35 µM.
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28112243/a-chemical-genetic-screen-uncovers-a-small-molecule-enhancer-of-the-n-acylethanolamine-degrading-enzyme-fatty-acid-amide-hydrolase-in-arabidopsis
#13
Bibi Rafeiza Khan, Lionel Faure, Kent D Chapman, Elison B Blancaflor
N-Acylethanolamines (NAEs) are a group of fatty acid amides that play signaling roles in diverse physiological processes in eukaryotes. Fatty acid amide hydrolase (FAAH) degrades NAE into ethanolamine and free fatty acid to terminate its signaling function. In animals, chemical inhibitors of FAAH have been used for therapeutic treatment of pain and as tools to probe deeper into biochemical properties of FAAH. In a chemical genetic screen for small molecules that dampened the inhibitory effect of N-lauroylethanolamine (NAE 12:0) on Arabidopsis thaliana seedling growth, we identified 6-(2-methoxyphenyl)-1,3-dimethyl-5-phenyl-1H-pyrrolo[3,4-d]pyrimidine-2,4(3 H,6 H)-dione (or MDPD)...
January 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28106377/chemical-proteomics-maps-brain-region-specific-activity-of-endocannabinoid-hydrolases
#14
Marc P Baggelaar, Annelot van Esbroeck, Eva van Rooden, Bogdan I Florea, Herman S Overkleeft, Giovanni Marsicano, Francis Chaouloff, Mario van der Stelt
The biosynthetic and catabolic enzymes of the endocannabinoids tightly regulate endocannabinoid-mediated activation of the cannabinoid CB1 receptor. Monitoring the activities of these endocannabinoid hydrolases in different brain regions is, therefore, key to gain insight in spatiotemporal control of CB1 receptor-mediated physiology. We have employed a comparative chemical proteomics approach to quantitatively map the activity profile of endocannabinoid hydrolases in various mouse brain regions at the same time...
January 20, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28104279/effect-of-inhibition-of-fatty-acid-amide-hydrolase-on-mptp-induced-dopaminergic-neuronal-damage
#15
J M Viveros-Paredes, R E Gonzalez-Castañeda, A Escalante-Castañeda, A R Tejeda-Martínez, F Castañeda-Achutiguí, M E Flores-Soto
INTRODUCTION: Parkinson's disease (PD) is a neurodegenerative disorder characterised by balance problems, muscle rigidity, and slow movement due to low dopamine levels and loss of dopaminergic neurons in the substantia nigra pars compacta (SNpc). The endocannabinoid system is known to modulate the nigrostriatal pathway through endogenous ligands such as anandamide (AEA), which is hydrolysed by fatty acid amide hydrolase (FAAH). The purpose of this study was to increase AEA levels using FAAH inhibitor URB597 to evaluate the modulatory effect of AEA on dopaminergic neuronal death induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)...
January 16, 2017: Neurología: Publicación Oficial de la Sociedad Española de Neurología
https://www.readbyqxmd.com/read/28092019/urb597-and-the-cannabinoid-win55-212-2-reduce-behavioral-and-neurochemical-deficits-induced-by-mptp-in-mice-possible-role-of-redox-modulation-and-nmda-receptors
#16
Angel Escamilla-Ramírez, Esperanza García, Guadalupe Palencia-Hernández, Ana Laura Colín-González, Sonia Galván-Arzate, Isaac Túnez, Julio Sotelo, Abel Santamaría
Several physiological events in the brain are regulated by the endocannabinoid system (ECS). While synthetic cannabinoid receptor (CBr) agonists such as WIN55,212-2 act directly on CBr, agents like URB597, a fatty acid amide hydrolase (FAAH) inhibitor, induce a more "physiological" activation of CBr by increasing the endogenous levels of the endocannabinoid anandamide (AEA). Herein, we compared the pre- and post-treatment efficacy of URB597 and WIN55,212-2 on different endpoints evaluated in the toxic model produced by the mitochondrial toxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in mice...
January 14, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28069688/up-regulation-of-cb2-receptors-in-reactive-astrocytes-in-canine-degenerative-myelopathy-a-disease-model-of-amyotrophic-lateral-sclerosis
#17
María Fernández-Trapero, Francisco Espejo-Porras, Carmen Rodríguez-Cueto, Joan R Coates, Carmen Pérez-Díaz, Eva de Lago, Javier Fernández-Ruiz
Targeting the CB2 receptor afforded neuroprotection in SOD1(G93A) mutant mice, a model of amyotrophic lateral sclerosis (ALS). The neuroprotective effects of CB2 receptors were facilitated by their up-regulation in the spinal cord in SOD1(G93A) mutant mice. Herein, we have investigated whether a similar CB2 receptor up-regulation, as well as parallel changes in other endocannabinoid elements, are evident in the spinal cord of dogs with degenerative myelopathy (DM), caused from mutations in the superoxide dismutase 1 gene (SOD1)...
January 9, 2017: Disease Models & Mechanisms
https://www.readbyqxmd.com/read/28065729/n-acylethanolamine-hydrolyzing-acid-amidase-and-fatty-acid-amide-hydrolase-inhibition-differentially-affect-n-acylethanolamine-levels-and-macrophage-activation
#18
Mireille Alhouayek, Pauline Bottemanne, Alexandros Makriyannis, Giulio G Muccioli
N-acylethanolamines (NAEs) such as N-palmitoylethanolamine and anandamide are endogenous bioactive lipids having numerous functions, including the control of inflammation. Their levels and therefore actions can be controlled by modulating the activity of two hydrolytic enzymes, N-acylethanolamine-hydrolyzing acid amidase (NAAA) and fatty acid amide hydrolase (FAAH). As macrophages are key to inflammatory processes, we used lipopolysaccharide-activated J774 macrophages, as well as primary mouse alveolar macrophages, to study the effect of FAAH and NAAA inhibition, using PF-3845 and AM9053 respectively, on macrophage activation and NAE levels measured by HPLC-MS...
January 6, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27999963/identification-of-an-endocannabinoid-system-in-the-rat-pars-tuberalis-a-possible-interface-in-the-hypothalamic-pituitary-adrenal-system
#19
Arsalan Jafarpour, Faramarz Dehghani, Horst-Werner Korf
Endocannabinoids (ECs) are ubiquitous endogenous lipid derivatives and play an important role in intercellular communication either in an autocrine/paracrine or in an endocrine fashion. Recently, an intrinsic EC system has been discovered in the hypophysial pars tuberalis (PT) of hamsters and humans. In hamsters, this EC system is under photoperiodic control and appears to influence the secretion of hormones such as prolactin from the adenohypophysis. We investigate the EC system in the PT of the rat, a frequently used species in endocrine research...
December 20, 2016: Cell and Tissue Research
https://www.readbyqxmd.com/read/27997038/inflammation-of-peripheral-tissues-and-injury-to-peripheral-nerves-induce-diferring-effects-in-the-expression-of-the-calcium-sensitive-anandamide-synthesising-enzyme-and-related-molecules-in-rat-primary-sensory-neurons
#20
João Sousa-Valente, Angelika Varga, Jose Vicente Torres Perez, Agnes Jenes, John Wahba, Ken Mackie, Benjamin Cravatt, Natsuo Ueda, Kazuhito Tsuboi, Peter Santha, Gabor Jancso, Hiren Tailor, António Avelino, Istvan Nagy
Elevation of intracellular Ca(2+) concentration induces the synthesis of N-arachydonoylethanolamine (anandamide) in a sub-population of primary sensory neurons. N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) is the only known enzyme, which synthesises anandamide in a Ca(2+) -dependent manner. NAPE-PLD mRNA, as well as anandamide's main targets, the excitatory transient receptor potential vanilloid type 1 ion channel (TRPV1) and the inhibitory cannabinoid type 1 (CB1) receptor and the main anandamide-hydrolysing enzyme fatty acid amide hydrolase (FAAH) are all expressed by sub-populations of nociceptive primary sensory neurons...
December 20, 2016: Journal of Comparative Neurology
keyword
keyword
49659
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"