Malamas, Michael S.; Lamani, Manjunath; Farah, Shrouq I.; Mohammad, Khadijah A.; Miyabe, Christina Yume; Rajarshi, Girija; Wu, Simiao; Zvonok, Nikolai; Chandrashekhar, Honrao; Wood, JodiAnne; Makriyannis, Alexandros published the artcile< Design and Synthesis of Highly Potent and Specific ABHD6 Inhibitors>, Related Products of 893566-75-1, the main research area is design synthesis biol activity ABHD6 inhibitor SAR; monoacylglycerol lipase; neuroinflammation.; neuroprotection; α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid; α/β-hydrolase domain containing 6.
Fine-tuning than complete disruption of 2-arachidonoylglycerol (2-AG) metabolism in the brain represents a promising pharmacol. approach to limit potential untoward effects associated with complete blockade of monoacylglycerol lipase (MGL), the primary hydrolase of 2-AG. This could be achieved through a/b-hydrolase domain containing 6 (ABHD6) inhibition, which will provide a smaller and safer contribution to 2-AG regulation in the brain. Pharmacol. studies with ABHD6 inhibitors have recently been reported, where modulation of ABHD6 activity either through CB1R-dependent or CB1R-independent processes showed promise in preclin. models of epilepsy, neuropathic pain and inflammation. Furthermore in the periphery, ABHD6 modulates 2-AG and other fatty acid monoacylglycerols (MAGs) and is implicated in Type-2 diabetes, metabolic syndrome and potentially other diseases. Herein, we report the discovery of single-digit nanomolar potent and highly specific ABHD6 inhibitors with >1000-fold selectivity against MGL and FAAH. The new ABHD6 inhibitors provide early leads to develop therapeutics for neuroprotection and the treatment of inflammation and diabetes.
ChemMedChem published new progress about Brain. 893566-75-1 belongs to class tetrahydroisoquinoline, and the molecular formula is C14H18BrNO2, Related Products of 893566-75-1.
Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem