Fatty Acid amide hydrolase: a potential target
for next generation therapeutics
by
Maccarrone M.
Department of Biomedical Sciences,
University of Teramo,
Piazza A. Moro 45, I-64100 Teramo, Italy.
mmaccarrone@unite.it.
Curr Pharm Des. 2006;12(6):759-72.
ABSTRACTTndocannabinoids are amides, esters and ethers of long chain polyunsaturated fatty acids, which act as new lipid mediators. Anandamide (N-arachidonoylethanolamine; AEA) and 2-arachidonoylglycerol are the main endogenous agonists of cannabinoid receptors, able to mimic several pharmacological effects of Delta(9)-tetrahydrocannabinol, 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 specific membrane transporter, followed by intracellular degradation by a 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 therapeutic drugs of potential value for the treatment of pathologies in the central nervous system and in the periphery. Here, the potential applications of these inhibitors for human disease will be reviewed, with an emphasis on the properties of hydro(pero)xy-anandamides. In fact, these oxygenated derivatives of AEA are the most powerful inhibitors of FAAH of natural origin as yet discovered. In addition, new insights into the promoter region of FAAH gene will be presented, and the therapeutic potential of mimetics of transcription factors of this gene in the management of human infertility will be discussed.THC
Bliss
Aerosol
Memory
Anandamide
Just say know
Tolerant mice
Forgetful rodents
Endocannabinoids
Stoned as a newt?
The nectar of delight
Stoned chocaholics?
Cannabis Abuse Disorder
Cannabis and schizophrenia
Cannabinoids/Parkinson's disease
Cannabis, anandamide and 'runner's high'
Mechanism of action of cannabis and cannabinoids01 02 03 04 05 06 07 08 09 10 11 12 13 14 15
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