Synthesis and pharmacological activity of a potent inhibitor of the biosynthesis of the endocannabinoid 2-arachidonoylglycerol.
Biosynthesis Inhibition: O-5596, a new inhibitor of the biosynthesis of the endocannabinoid, 2-arachidonoylglycerol, was synthesized and found to be potent (IC(50)=100 nM) and selective versus other proteins and enzymes of the endocannabinoid system in vitro and active in vivo at reducing food intake in mice.
Bisogno
Tiziana
T
Endocannabinoid Research Group, Institute of Biomolecular Chemistry, Consiglio Nazionale delle Ricerche, Via Campi Flegrei 34, Comprensorio Olivetti, Pozzuoli (NA), Italy.
Burston
James J
JJ
Rai
Ravi
R
Allarà
Marco
M
Saha
Bijali
B
Mahadevan
Anu
A
Razdan
Raj K
RK
Wiley
Jenny L
JL
Di Marzo
Vincenzo
V
D000475:Alkenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001095:Arachidonic Acids / Q000096:biosynthesis* / Q000737:chemistry; D002460:Cell Line; D004355:Drug Stability; D004435:Eating / Q000187:drug effects; D063388:Endocannabinoids; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005989:Glycerides / Q000096:biosynthesis* / Q000737:chemistry; D006801:Humans; D008071:Lipoprotein Lipase / Q000037:antagonists & inhibitors / Q000378:metabolism; D051379:Mice; D009943:Organophosphorus Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D043885:Receptor, Cannabinoid, CB2 / Q000037:antagonists & inhibitors / Q000378:metabolism
D000475:Alkenes; D001095:Arachidonic Acids; D063388:Endocannabinoids; D004791:Enzyme Inhibitors; D005989:Glycerides; C542537:O-5596; D009943:Organophosphorus Compounds; D043884:Receptor, Cannabinoid, CB1; D043885:Receptor, Cannabinoid, CB2; C094503:glyceryl 2-arachidonate; C480280:DAGLA protein, human; D008071:Lipoprotein Lipase