LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzymes serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .
性状
Solid
体内研究(In Vivo)
LY2183240 (3-30mg/kg; i.p.) dose-dependently attenuates formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male Sprague-Dawley rats (Formalin Pain Model)
Dosage:
3, 10, 30 mg/kg
Administration:
I.p.
Result:
Dose-dependently attenuated formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms.