2-hydroxy Atorvastatin is an active metabolite of the HMG-CoA reductase inhibitor atorvastatin .1 2-hydroxy Atorvastatin is formed from atorvastatin by the cytochrome P450 (CYP) isoform CYP3A4. It inhibits lipid hydroperoxide formation and copper sulfate-induced thiobarbituric acid reactive substances (TBARS) formation in 1,2-dilinoleoyl-sn-glycero-3-PC vesicles and human LDL, respectively, in a concentration-dependent manner.2 2-hydroxy Atorvastatin reduces cell death induced by oxygen-glucose deprivation (OGD) in primary rat cortical neurons and increases phosphorylation of cAMP-response-element-binding protein (CREB) in GABAergic neurons when used at a concentration of 600 nM following OGD.3
1.Park, J.-E., Kim, K.-B., Bae, S.K., et al.Contribution of cytochrome P450 3A4 and 3A5 to the metabolism of atorvastatinXenobiotica38(9)1240-1251(2008) 2.Mason, R.P., Walter, M.F., Day, C.A., et al.Active metabolite of atorvastatin inhibits membrane cholesterol domain formation by an antioxidant mechanismJ. Biol. Chem.281(14)9337-9345(2006) 3.Guirao, V., Martí-Sistac, O., DeGregorio-Rocasolano, N., et al.Specific rescue by ortho-hydroxy atorvastatin of cortical GABAergic neurons from previous oxygen/glucose deprivation: Role of pCREBJ. Neurochem.143(3)359-374(2017)