Lipid peroxidation inhibitor 1

Lipid peroxidation inhibitor 1 is a lipid peroxidation inhibitor with an IC50 of 0.07 μM.

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

IC50: 0.07μM (lipid peroxidation)[1]

Among the compounds synthesized, Lipid peroxidation inhibitor 1 (26n) exhibits potent effects in the inhibition of lipid peroxidation, with an IC50 of 0.07 μM[1].

Basic molecules 8a and 27 exhibit significant effects against (methamphetamine) MAP-induced hypermotility. Except in these compounds, a phenyl group adjacent to the methyl group in position 2 at a distance seems to be indispensable (compare compounds 26m, o, p with compounds Lipid peroxidation inhibitor 1 (26n), q, r). Among these compounds, Lipid peroxidation inhibitor 1 which has a phenylpiperidinyl group in position 2 is found to be most effective[1].

To rat liver microsomes (S-9) (0.3 mg of protein/40 mM Tris-malate buffer (pH 7.4), 2.4 mL) (2.4 mL) is added a mixture (1:1; 0.1 mL) of aqueous FeCl2 solution (0.25 mM) and NADPH (3 mM). After incubation of the homogenate for 1 h at 37 °C, peroxide production is determined by the thiobarbituric acid method. The inhibitory activities on lipid peroxidation are expressed as IC50 values or percent inhibition as compare with the amount of production in the vehicle (DMSO) group[1].

Five-week old male mice (25 to 35 g) are used. Following a 90 min acclimation period, the test compounds (including Lipid peroxidation inhibitor 1) suspended in 5% gum arabic are injected intraperitoneally in a volume of 20 mL/kg. Thirty minutes after treatment with test compounds, methamphetamine dissolved in saline is injected intraperitoneally at a dose of 1 mg/kg in a volume of 20 mL/kg. Immediately after methamphetamine injection, spontaneous motor activity is monitored for 90 min[1].

[1]. Ohkawa S, et al. 5-aminocoumarans: dual inhibitors of lipid peroxidation and dopamine release with protectiveeffects against central nervous system trauma and ischemia. J Med Chem. 1997 Feb 14;40(4):559-73.

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