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Literature summary for 3.5.1.99 extracted from

  • Giacovazzo, G.; Bisogno, T.; Piscitelli, F.; Verde, R.; Oddi, S.; Maccarrone, M.; Coccurello, R.
    Different routes to inhibit fatty acid amide hydrolase do all roads lead to the same place? (2019), Int. J. Mol. Sci., 20, E4503 .
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine there is evidence indicating that enhancing the endocannabinoid (eCB) tone has therapeutic potential in several brain disorders. The inhibition of endocannabinoid degradation by fatty acid amide hydrolase blockade, is the best-known option to increase N-acyl-ethanolamines-mediated signaling. By showing the efficacy of intranasal FAAH inhibition, evidence is provided that nose-to-brain delivery is a suitable alternative to enhance brain endocannabinoid tone for the treatment of neurodegenerative disorders and improve patients' compliance Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
PF-04457845 potently inhibits the enzyme regardless the route selected Mus musculus
URB597 less effective inhibitor in the brain after oral administration while it reaches similar effects by intranasal (i.n.) and intraperitoneal routes. Intranasal URB597 delivery always increased N-acyl-ethanolamine levels in brain areas, whereas a parallel increase is not observed in the liver. By showing the efficacy of intranasal FAAH inhibition, evidence is provided that nose-to-brain delivery is a suitable alternative to enhance brain endocannabinoid tone for the treatment of neurodegenerative disorders and improve compliance of the patients Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus O08914
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Source Tissue

Source Tissue Comment Organism Textmining
brain
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Mus musculus
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-arachidonoylethanolamine + H2O
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Mus musculus arachidonic acid + ethanolamine
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