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
Non-clinical toxicology evaluation of BIA 10-2474
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DOI: 10.1080/10408444.2020.1867821
Abstract: Abstract In 2016, one subject died and four were hospitalized with neurological symptoms during a clinical trial with the fatty acid amide hydrolase (FAAH) inhibitor BIA 10-2474. The present paper reviews the regulatory toxicology studies… read more here.
Keywords: clinical trial; clinical toxicology; bia 2474; non clinical ... See more keywords
Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474
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DOI: 10.1126/science.aaf7497
Abstract: A clue to a drug's neurotoxicity? The drug BIA 10-2474 inhibits fatty acid amide hydrolase (FAAH), a lipase that degrades a specific endocannabinoid. On the basis of this activity, BIA 10-2474 was being developed as… read more here.
Keywords: bia 2474; activity based; target; drug ... See more keywords