Title : Targeting Fatty-Acid Amide Hydrolase with Prodrugs for CNS-Selective Therapy.

Pub. Date : 2017 Nov 15

PMID : 28756656






4 Functional Relationships(s)
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1 Here, we report a strategy for CNS-selective distribution of the carboxylic acid containing thyromimetic sobetirome using prodrugs targeted to fatty-acid amide hydrolase (FAAH), which is expressed in the brain. GC 1 compound fatty acid amide hydrolase Mus musculus
2 Two amide prodrugs of sobetirome were shown to be efficient substrates of FAAH with Vmax/KM values comparable to the natural endocannabinoid FAAH substrate anandamide. GC 1 compound fatty acid amide hydrolase Mus musculus
3 Two amide prodrugs of sobetirome were shown to be efficient substrates of FAAH with Vmax/KM values comparable to the natural endocannabinoid FAAH substrate anandamide. GC 1 compound fatty acid amide hydrolase Mus musculus
4 The increased delivery of sobetirome to the brain from the prodrug was diminished by both pharmacological inhibition and genetic deletion of FAAH in vivo. GC 1 compound fatty acid amide hydrolase Mus musculus