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Fatty acid amide hydrolase: a gate-keeper of the endocannabinoid system.
Subcell Biochem 2008; 49:101-32SB

Abstract

The family of endocannabinoids contains several polyunsaturated fatty acid amides such as anandamide (AEA), but also esters such as 2-arachidonoylglycerol (2-AG). These compounds are the main endogenous agonists of cannabinoid receptors, able to mimic several pharmacological effects of Delta9-tetrahydrocannabinol (Delta9-THC), the active principle of Cannabis sativa preparations like hashish and marijuana. The activity of AEA at its receptors is limited by cellular uptake, through a putative membrane transporter, followed by intracellular degradation by fatty acid amide hydrolase (FAAH). Growing evidence demonstrates that FAAH is the critical regulator of the endogenous levels of AEA, suggesting that it may serve as an attractive therapeutic target for the treatment of human disorders. In particular, FAAH inhibitors may be next generation therapeutics of potential value for the treatment of pathologies of the central nervous system, and of peripheral tissues. Investigations into the structure and function of FAAH, its biological and therapeutic implications, as well as a description of different families of FAAH inhibitors, are the topic of this chapter.

Authors+Show Affiliations

Department of Experimental Medicine and Biochemical Sciences, University of Rome, Rome, Italy.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

18751909

Citation

Fezza, Filomena, et al. "Fatty Acid Amide Hydrolase: a Gate-keeper of the Endocannabinoid System." Sub-cellular Biochemistry, vol. 49, 2008, pp. 101-32.
Fezza F, De Simone C, Amadio D, et al. Fatty acid amide hydrolase: a gate-keeper of the endocannabinoid system. Subcell Biochem. 2008;49:101-32.
Fezza, F., De Simone, C., Amadio, D., & Maccarrone, M. (2008). Fatty acid amide hydrolase: a gate-keeper of the endocannabinoid system. Sub-cellular Biochemistry, 49, pp. 101-32. doi:10.1007/978-1-4020-8831-5_4.
Fezza F, et al. Fatty Acid Amide Hydrolase: a Gate-keeper of the Endocannabinoid System. Subcell Biochem. 2008;49:101-32. PubMed PMID: 18751909.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Fatty acid amide hydrolase: a gate-keeper of the endocannabinoid system. AU - Fezza,Filomena, AU - De Simone,Chiara, AU - Amadio,Daniele, AU - Maccarrone,Mauro, PY - 2008/8/30/pubmed PY - 2008/12/25/medline PY - 2008/8/30/entrez SP - 101 EP - 32 JF - Sub-cellular biochemistry JO - Subcell. Biochem. VL - 49 N2 - The family of endocannabinoids contains several polyunsaturated fatty acid amides such as anandamide (AEA), but also esters such as 2-arachidonoylglycerol (2-AG). These compounds are the main endogenous agonists of cannabinoid receptors, able to mimic several pharmacological effects of Delta9-tetrahydrocannabinol (Delta9-THC), the active principle of Cannabis sativa preparations like hashish and marijuana. The activity of AEA at its receptors is limited by cellular uptake, through a putative membrane transporter, followed by intracellular degradation by fatty acid amide hydrolase (FAAH). Growing evidence demonstrates that FAAH is the critical regulator of the endogenous levels of AEA, suggesting that it may serve as an attractive therapeutic target for the treatment of human disorders. In particular, FAAH inhibitors may be next generation therapeutics of potential value for the treatment of pathologies of the central nervous system, and of peripheral tissues. Investigations into the structure and function of FAAH, its biological and therapeutic implications, as well as a description of different families of FAAH inhibitors, are the topic of this chapter. SN - 0306-0225 UR - https://www.unboundmedicine.com/medline/citation/18751909/Fatty_acid_amide_hydrolase:_a_gate_keeper_of_the_endocannabinoid_system_ L2 - https://www.lens.org/lens/search?q=citation_id:18751909 DB - PRIME DP - Unbound Medicine ER -