Target intelligence / Profile preview

Fatty Acid Amide Hydrolase (FAAH)

Target
FAAH
Molecular classification
Enzyme, Serine hydrolase, Membrane protein
01

Overview

Fatty acid amide hydrolase (FAAH) is an integral membrane enzyme and a member of the serine hydrolase family. It plays a central role in the degradation of fatty acid amides, which are endogenous signaling lipids involved in various physiological processes. FAAH is particularly important for terminating the signaling actions of bioactive lipids such as anandamide (an endocannabinoid), oleamide (a sleep-inducing lipid), and other N-acylethanolamines. Because inhibition or genetic deletion increases endogenous cannabinoid tone without directly activating cannabinoid receptors, targeting FAAH is considered promising for developing analgesics or anxiolytics with potentially fewer side effects than direct receptor agonists.

Other names
Oleamide hydrolaseAnandamide amidohydrolase
02

Mechanism of action

Hydrolyzes fatty acid amides into their corresponding fatty acids and amines, thereby regulating their levels and biological activity. Inhibition of FAAH increases levels of bioactive fatty acid amides.

03

Biological functions

Hydrolysis of fatty acid amidesRegulation of endocannabinoid signalingModulation of pain sensationRegulation of sleepRegulation of inflammationNeuroprotection
04

Disease associations

PainAnxiety disordersSleep disordersNeurodegenerative diseasesInflammation
05

Safety considerations

Species differences between rodents and humans (FAAH2)Potential for off-target effectsCareful monitoring needed during clinical trials to evaluate potential side effects of increased endocannabinoid tone
06

Interacting drugs

Trifluoromethyl ketones

5 more in the full profile.

07

Biomarkers

Anandamide levelsOleamide levelsN-acylethanolamine levels

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