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08/15/2018 - 03:48

What is JZL 195?

A almighty inhibitor of both FAAH and MAGL (IC50 = 2 and 4 nM, respectively); ailing inhibits added academician serine hydrolases|Fatty acerbic amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) arbitrate the hydrolysis of the endocannabinoids arachidonoyl ethanolamide (AEA) and 2-arachidonoylglycerol (2-AG), respectively. JZL 195 is a almighty inhibitor of both FAAH and MAGL (IC50 = 2 and 4 nM, respectively). It ailing inhibits neuropathy ambition esterase and ABHD6 and does not arrest added academician serine hydrolases.
JZL 195 displays time-dependent inhibition of FAAH and MAGL in vivo, constant with a covalent apparatus of activation. The in vivo inhibitory accomplishments of JZL 195 adjoin FAAH and MAGL are commensurable to those of the careful inhibitors PF-3845 (Item No. 13279) and JZL 184 (Item No. 13158), respectively.
Through its inhibitory actions, JZL 195 accompanying augments academician levels of AEA and 2-AG, bearing antinociceptive, cataleptic, and hypomotility furnishings like those produced by absolute CB1 agonists.

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