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Updated: Jun 1, 2026
11:01
Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase
Published on: November 23, 2016
Fatty acid amide hydrolase inhibitors--progress and potential
Ish K Khanna1, Christopher W Alexander
1Kareus Therapeutics S.A., Norcross, GA 30071, USA. ikhanna@kareustherapeutics.com
CNS & Neurological Disorders Drug Targets
|June 3, 2011
Summary
Fatty acid amide hydrolase (FAAH) inhibitors elevate anandamide (AEA) to modulate pain and neurodegenerative disorders. This review covers current FAAH inhibitor strategies, enzyme interactions, and therapeutic potential.
Area of Science:
- Biochemistry
- Pharmacology
- Neuroscience
Background:
- Fatty acid amide hydrolase (FAAH) regulates endocannabinoids like anandamide (AEA).
- AEA plays a role in pain modulation and neurodegenerative disorders.
- Inhibiting FAAH increases AEA levels.
Purpose of the Study:
- To review recent advancements in diverse structural classes of reversible and irreversible FAAH inhibitors.
- To discuss ligand-enzyme interactions and mechanisms of enzyme inactivation.
- To explore novel FAAH inhibitor development and therapeutic utility.
Main Methods:
- Literature review of FAAH inhibitors.
- Analysis of structural classes and mechanisms of action.
- Discussion of ongoing research and therapeutic challenges.
Main Results:
- Diverse structural classes of reversible and irreversible FAAH inhibitors have been developed.
- Understanding of ligand-enzyme active site interactions and inactivation mechanisms is advancing.
- Emerging approaches aim to enhance the therapeutic utility of FAAH inhibitors.
Conclusions:
- FAAH inhibitors represent a promising therapeutic strategy for pain and neurodegenerative disorders.
- Continued research is crucial for optimizing FAAH inhibitor design and addressing current limitations.
- Novel approaches are being explored to improve the clinical efficacy of FAAH inhibitors.
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