Isovaleramide is isolated from the most active fraction of Valeriana pavonii. Isovaleramide (300 μM) exhibits a 42% of inhibition of the binding of 3H-FNZ to its sites in the in vitro assay. Isovaleramide is without effect at concentrations up to 1000 μM in a variety of in vitro neurotransmitter binding or uptake assays, suggesting that its action does not involve a direct receptor-mediated effect at those systems studied. Isovaleramide (0.15%) induces the formation of nitrile hydratase in Rhodococcus sp. YH 3-3.
体内研究:Isovaleramide (100 mg/Kg, p.o) evidences a 90% index protection against the maximal electroshock seizure in mice (MES). Isovaleramide produces a consistent pattern of signs at relatively high doses in extensive safety studies in rats, rabbits, and dogs. Isovaleramide shows a significantly lower potential for reproductive toxicity than VPA in several reproductive toxicity studies conducted in mice, rats and rabbits.