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2014 ; 43
(19
): 6859-69
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gab.com Text
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Chemical approaches to therapeutically target the metabolism and signaling of the
endocannabinoid 2-AG and eicosanoids
#MMPMID24676249
Kohnz RA
; Nomura DK
Chem Soc Rev
2014[Oct]; 43
(19
): 6859-69
PMID24676249
show ga
The endocannabinoid system, most popularly known as the target of the
psychoactive component of marijuana, ?(9)-tetrahydrocannabinol (THC), is a
signaling network that modulates a diverse range of physiological processes
including nociception, behavior, cognitive function, appetite, metabolism, motor
control, memory formation, and inflammation. While THC and its derivatives have
garnered notoriety in the eyes of the public, the endocannabinoid system consists
of two endogenous signaling lipids, 2-arachidonoylglycerol (2-AG) and
N-arachidonoylethanolamine (anandamide), which activate cannabinoid receptors CB1
and CB2 in the nervous system and peripheral tissues. This review will focus on
the recent efforts to chemically manipulate 2-AG signaling through the
development of inhibitors of the 2-AG-synthesizing enzyme diacylglycerol lipase
(DAGL) or the 2-AG-degrading enzyme monoacylglycerol lipase (MAGL), and assessing
the therapeutic potential of DAGL and MAGL inhibitors in pain, inflammation,
degenerative diseases, tissue injury, and cancer.
|Animals
[MESH]
|Arachidonic Acids/chemistry/*metabolism
[MESH]
|Dronabinol/chemistry/pharmacology/therapeutic use
[MESH]
|Eicosanoids/*metabolism
[MESH]
|Endocannabinoids/chemistry/*metabolism
[MESH]
|Enzyme Inhibitors/chemistry/pharmacology/therapeutic use
[MESH]