Results 111 to 120 of about 8,951 (213)

Discovery of FAAH inhibitors by rational drug design [PDF]

, 2011
脂肪酰胺水解酶(FAAH)是调控内源性脂肪酰胺信使脂质分子代谢的主要酶。FAAH活性抑制即可以使体内内源性脂肪酰胺水平升高，达到镇痛、抗炎、协调运动机能的目的，过去十年间，具有FAAH抑制活性的大量化合物也得到报道，但是到目前为止，还没有成功上市的FAAH抑制剂，关键的原因就在于其选择性与抑制效率无法兼顾。本文在此基础上，展开了如下工作： 一、利用药效团构建软件DiscoveryStudio2.1构建定性的CommonFeature药效团和定量的3DQSAR药效团模型 ...
赵东升
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FAAH deficiency affects fuel storage.

, 2012
a. Fed triglycerides and glycogen of liver and skeletal muscle. Upper panel shows thin layer chromatography (TLC) for hepatic and intra-muscular triglycerides with corresponding densitometry.
Irwin J. Kurland (177409), Kirsten Hartil (177391), James E. Bruce (177406), Sherrye Glaser (177394), Bhavapriya Vaitheesvaran (177385), Li Yang (6520), Stephen Yazulla (177399)   +6 more
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Effect of DGPP 10 µM on FAAH activity and expression.

, 2013
Uterine strips from rats pregnant on day 5 of gestation were incubated for 6 h with DGPP 10 µM. FAAH activity was determine by radioconversion and FAAH mRNA and protein expression was analyzed by RT-PCR and Western Blot respectively.
Silvina Perez Martinez (304948), Elsa Zotta (304950), Maximiliano Cella (304946), Ana M. Franchi (284968), Micaela S. Sordelli (304944), Jimena S. Beltrame (304945), María Gracia Gervasi (304947), Juliana Burdet (304949), María Laura Ribeiro (304951)   +8 more
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PERIPHERALLY RESTRICTED FAAH INHIBITORS

, 2012
Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS).
Guillermo MORENO SANZ, Daniele PIOMELLI, Andrea DURANTI, Andrea TONTINI, MOR, Marco, Jason CLAPPER, Giorgio TARZIA   +6 more
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Expression of Fatty Acid Amide Hydrolase (FAAH) in Human, Mouse, and Rat Urinary Bladder and Effects of FAAH Inhibition on Bladder Function in Awake Rats.

, 2012
BACKGROUND: Cannabinoid receptor (CB)-mediated functions may be involved in the regulation of bladder function, but information on endocannabinoid signals during micturition is scarce.
Arianna Bettiga, Bettiga, A.,, Stief, C.,, Petter Hedlund, Christian Gratzke, Benigni, Fabio, Christian Stief, Colciago, Giorgia, Francesco Montorsi, Rigatti, Patrizio, Stief, Christian, Benigni, F.,, Hedlund, Petter,, Fabio Benigni, Strittmatter, Frank, Gratzke, C.,, Montorsi, Francesco, Gandaglia, Giorgio, Montorsi, F.,, Rigatti, P.,, Colciago, G.,, Hedlund, Petter, Frank Strittmatter, Giorgia Colciago, Gratzke, Christian, Strittmatter, F.,, Gandaglia, G.,, Bettiga, Arianna, Giorgio Gandaglia, Patrizio Rigatti   +29 more
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Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor

, 2016
Fatty acid amide hydrolase (FAAH) is an integral membrane serine hydrolase that degrades the fatty acid amide family of signaling lipids, including the endocannabinoid anandamide.
Tyzoon K. Nomanbhoy (2232289), Shobha N. Bhattachar (2232280), Mark Morris (1834648), Stephen J. Kesten (2232277), Kay Ahn (1523929), Sarah E. Smith (611984), Douglas S. Johnson (1534639), Lorraine K. Fay (2232295), David T. Dudley (2232271), Suzanne R. Kesten (2232286), David Beidler (2232292), Nalini Sadagopan (2232274), Marya B. Liimatta (2232283), Cory Stiff (2134888), Scott E. Lazerwith (1833898), Benjamin F. Cravatt (93774)   +15 more
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Inhibition of rat wild-type and FAAH^T488A by A.

, 2015
(R)-Flu-AM1 and B. carprofen. Samples were incubated for 18 h with inhibitor and substrate (0.5 μM [3H]AEA). The concentrations of lysates used were FAAHwt, 0.04 μg/assay, FAAHT488A, 0.4 μg/assay, empty vector 0.36 μg/assay.
F. Javier Luque (60532), Christopher J. Fowler (124329), Jessica Karlsson (604249), Carmine M. Morgillo (826081), Ettore Novellino (333902), Bruno Catalanotti (655615), Alessandro Deplano (800574), Giovanni Smaldone (739222), Emilia Pedone (655614), Mona Svensson (800575), Valentina Onnis (800578), Cenzo Congiu (800577)   +11 more
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FAAH better anxiolytics? [PDF]

Nature Reviews Drug Discovery, 2003
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Chiral 3-(4,5-dihydrooxazol-2-yl)phenyl alkylcarbamates as novel FAAH inhibitors: Insight into FAAH enantioselectivity by molecular docking and interaction fields

, 2020
Fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) are the main enzymes responsible for the hydrolysis of endogenous cannabinoids N-arachidonoylethanolamide (AEA) and 2-arachidonoylglycerol (2-AG), respectively.
Maija ; Saario, Ari M P, Poso S M, M J Myllymaki, Antti ; Koskinen, Lahtela-Kakkonen, user. Myllymaki Mikko J ; Kasnanen, A O Kataja, Antti O ; Lahtela-Kakkonen, Heikki ; Kataja, Susanna M ; Poso, M Saario, A Koskinen, H Kasnanen, A M P   +14 more
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Fenyylikarbamaattien kiraaliset oksatsoliinijohdannaiset potentiaalisina FAAH-inhibiittoreina: suunnittelu, synteesi ja karakterisointi

, 2007
Diplomityön tarkoituksena oli suunnitella ja valmistaa molekyylikirjasto, jonka yhdisteet olisivat potentiaalisia inhibiittoreita endogeenista kannabinoidia arakidonoyylietanoliamidia hydrolysoivalle FAAH-entsyymille.
Kataja, Antti
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