Select Page

Aasraw Biochemical Technology Co. Ltd, a cerified steroids raw powder manufacturer with ISO9001 in China  brings to you “JZL195, 1210004-12-8” a potent dual inhibitor of Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), enzymes that degrade the endocannabinoids 2-arachidonoylglycerol (2-AG) and anandamide (AEA), the endogenous ligands for the cannabinoid G-protein coupled receptors CB1 and CB2. IC50 values are 2 nM for MAGL and4 nM for FAAH. JZL195 has been shown to inhibit endocannabinoid hydrolysis andelevate 2-AG and AEA levels in vivo.

 

The white solid dual FAAH/MAGL inhibitor JZL195 has enhanced effects on endocannabinoid transmission and motor behavior in rats as compared to those of the MAGL inhibitorJZL184. It has a molecular Weight of 433.457 and -20°C as melting point, its molecular Formula is C24H23N3O5.

The biological actions of the endocannabinoids anandamide and 2-arachidonoyl glycerol (2-AG) are terminated by enzymatic hydrolysis of these lipids via fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL), respectively. While several selective FAAH inhibitors have been developed and characterized in vitro and in vivo, none of the initial MAGL blockers have shown adequate potency and specificity for in vivo applications. More recently, a selective MAGL inhibitor, JZL184, has been shown to produce a long-lasting elevation of brain 2-AG, as well as cannabinoid-like behavioral responses in mice. However, its effectiveness in rats remains controversial. Indeed, although JZL184 can elicit behavioral responses that are mediated, at least in part, via activation of cannabinoid CB1 receptors, several reports indicate that this compound does not alter 2-AG levels in this species.

In a study, Aasraw compared the behavioral and neurochemical effects of JZL 184 with those of the dual FAAH/MAGL inhibitor JZL195, and showed that systemic administration of the former can selectively elevate brain 2-AG in rats and produce motor suppression through a CB1-independent mechanism. These findings indicate that, despite its lower potency against rat MAGL, JZL184 can be used to enhance 2-AG transmission and elicit behavioral responses in rodents. As their research, in contrast to JZL195, which decreased motor activity at all doses tested, JZL184 was effective only at the highest dose (30 mg/kg, p<0.05). The motor effects of both JZL compounds are also presented as time course over a 60 min period.

JZL195, 1210004-12-8 is a potent inhibitor of both FAAH andMAGL (IC50s = 2 and 4 nM, respectively).1 It poorly inhibits neuropathy target esterase and ABHD6 and does not inhibit other brain serine hydrolases. JZL 195 displays time-dependent inhibition of FAAH and MAGL in vivo, consistent with a covalent mechanism of activation.1 The in vivo inhibitory actions of JZL 195 against FAAHand MAGL are comparable to those of the selective inhibitors PF-3845 (Item No. 13279) and JZL 184 (Item No. 13158), respectively.1 Through its inhibitory actions, JZL 195 simultaneously augments brain levels of AEA and 2-AG, producing antinociceptive, cataleptic, and hypomotility effects like those produced by direct CB1 agonists. JZL 195 is also offered as part of the Tocriscreen Plus.

About Aasraw Biochemical Technology Co. Ltd

Aasraw Biochemical Technology Co.,ltd was reorganized by a Shanghai based Biochemical Engineering Laboratory in 2008, which was built by 5 Chinese Ph. Doctors, who are majored at Chemical Engineering in University of Tulsa, Oklahoma, USA. The new born AASraw gained more investment and attracted more top genius guys in the biochemical industry. There are more advantaged equipment and instruments to be being adopted for analyzing, testing, Synthesis, etc, for example, DSC, GV, HPLC, UV, RV, etc. Till now, there are more than 20 key technology engineers. The fixed assets is more than USD30 million. Beside the long term stable cooperation projects, the yearly scheduled new projects will be 5-8 and the newly adopted technology patent will be 1-2. There are more than 100 kinds of goods for bulk production. And, more than 80 of them are owned and can be produced directly, and more than 20 of them are Synthetic Product Technology. These goods are for more than 30 famous pharmacy companies around the world.

For more information please visit http://www.aasraw.com/ or send a mail to king@aasraw.com to inquire more.

Media Contact
Company Name: Aasraw Biochemical Technology Co. Ltd
Contact Person: Aasraw
Email: king@aasraw.com
Phone: (132) 040-2669
Address: 1838 Fairway Cir Dr, San Marcos
Country: United States
Website: http://www.aasraw.com

%d bloggers like this: