Development and molecular modeling studies of new thiadiazole piperazine urea derivatives as potential fatty acid amide hydrolase inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200082
Abstract: A series of novel piperazine urea derivatives with thiadiazole moieties were designed, synthesized, and investigated for their inhibition potential against human fatty acid amide hydrolase (hFAAH). The urea derivatives possessing p‐chlorophenylthiadiazole and benzylpiperazine fragments (19–22)… read more here.
Keywords: amide hydrolase; acid; piperazine urea; acid amide ... See more keywords
Inactivation Mechanism of the Fatty Acid Amide Hydrolase Inhibitor BIA 10‐2474
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DOI: 10.1002/cbic.202200166
Abstract: BIA 10‐2474 is a time‐dependent inhibitor of fatty acid amide hydrolase (FAAH) that was under clinical development for the treatment of neurological conditions when the program was terminated after one subject died and four were… read more here.
Keywords: amide hydrolase; inhibitor; acid amide; bia 2474 ... See more keywords
Discovery of a Potent, Long‐Acting, and CNS‐Active Inhibitor (BIA 10‐2474) of Fatty Acid Amide Hydrolase
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DOI: 10.1002/cmdc.201800393
Abstract: Fatty acid amide hydrolase (FAAH) can be targeted for the treatment of pain associated with various medical conditions. Herein we report the design and synthesis of a novel series of heterocyclic‐N‐carboxamide FAAH inhibitors that have… read more here.
Keywords: acid amide; bia 2474; long acting; fatty acid ... See more keywords
Effects of fatty acid amide hydrolase inhibitor URB597 in a rat model of trauma-induced long-term anxiety
Sign Up to like & getrecommendations! Published in 2018 at "Psychopharmacology"
DOI: 10.1007/s00213-018-5020-7
Abstract: RationaleThe endocannabinoid neurotransmitter, anandamide, has been implicated in the central modulation of stress responses. Previous animal experiments have shown that inhibitors of the anandamide-degrading enzyme, fatty acid amide hydrolase (FAAH), enhance the ability to cope… read more here.
Keywords: acid amide; anxiety; fatty acid; amide hydrolase ... See more keywords
Tetrazolylpropan-2-ones as inhibitors of fatty acid amide hydrolase: Studies on structure-activity relationships and metabolic stability.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.10.021
Abstract: A series of derivatives of 1-(4-octylphenoxy)-3-(2H-tetrazol-2-yl)propan-2-one (3) and 1-(4-octylphenoxy)-3-(1H-tetrazol-1-yl)propan-2-one (4) was synthesized and tested for fatty acid amide hydrolase (FAAH) inhibitory potency and phase I metabolic stability. Introduction of certain substituents like 4-chlorophenyl, 4-methoxycarbonylphenyl and… read more here.
Keywords: acid amide; metabolic stability; fatty acid; amide hydrolase ... See more keywords
A perspective review on fatty acid amide hydrolase (FAAH) inhibitors as potential therapeutic agents.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111953
Abstract: Fatty acid amide hydrolase (FAAH) is an important enzyme creditworthy of hydrolyzing endocannabinoids and related-amidated signalling lipids, discovery of which has pioneered novel arena of pharmacological canvasses to unwrap its curative potency in various diseased… read more here.
Keywords: acid amide; faah; fatty acid; amide hydrolase ... See more keywords
Development of N-(1-Adamantyl)benzamides as Novel Anti-Inflammatory Multitarget Agents Acting as Dual Modulators of the Cannabinoid CB2 Receptor and Fatty Acid Amide Hydrolase.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01084
Abstract: Cannabinoid type 2 receptor (CB2R), belonging to the endocannabinoid system, is overexpressed in pathologies characterized by inflammation, and its activation counteracts inflammatory states. Fatty acid amide hydrolase (FAAH) is an enzyme responsible for the degradation… read more here.
Keywords: amide hydrolase; adamantyl benzamides; anti inflammatory; acid amide ... See more keywords
The fatty-acid amide hydrolase inhibitor URB597 inhibits MICA/B shedding
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DOI: 10.1038/s41598-020-72688-y
Abstract: MICA/B proteins are expressed on the surface of various types of stressed cells, including cancer cells. Cytotoxic lymphocytes expressing natural killer group 2D (NKG2D) receptor recognize MICA/B and eliminate the cells. However, cancer cells evade… read more here.
Keywords: mica; acid amide; inhibitor; fatty acid ... See more keywords
A genetic variant of fatty acid amide hydrolase (FAAH) exacerbates hormone-mediated orexigenic feeding in mice
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DOI: 10.1101/2022.08.09.503403
Abstract: Fatty acid amide hydrolase (FAAH) degrades the endocannabinoid anandamide. A polymorphism in FAAH (FAAH C385A) reduces FAAH expression, increases anandamide levels, and increases the risk of obesity. Nevertheless, some studies have found no association between… read more here.
Keywords: amide hydrolase; faah; acid amide; mice ... See more keywords
Ethanol‐induced alterations in endocannabinoids and relevant neurotransmitters in the nucleus accumbens of fatty acid amide hydrolase knockout mice
Sign Up to like & getrecommendations! Published in 2018 at "Addiction Biology"
DOI: 10.1111/adb.12695
Abstract: Deletion of fatty acid amide hydrolase (FAAH), enzyme responsible for degrading endocannabinoids, increases alcohol consumption and preference. However, there is a lack of data on neurochemical events in mice exposed to alcohol in the absence… read more here.
Keywords: acid amide; fatty acid; amide hydrolase; faah mice ... See more keywords
Fatty acid amide hydrolase is lower in young cannabis users
Sign Up to like & getrecommendations! Published in 2020 at "Addiction Biology"
DOI: 10.1111/adb.12872
Abstract: We have recently shown that levels of fatty acid amide hydrolase (FAAH), the enzyme that metabolizes the endocannabinoid anandamide, are lower in the brains of adult cannabis users (CUs) (34 ± 11 years of age),… read more here.
Keywords: cannabis; acid amide; fatty acid; 11c curb ... See more keywords