Divalproex Sodium 结合并抑制 γ-氨基丁酸 (GABA) 转氨酶,其抗惊厥活性可通过增加 GABA 脑浓度和抑制分解 GABA 或阻止 GABA 再摄取到神经胶质和神经末梢的酶来发挥。它也是一种 HDAC 抑制剂。它是一种稳定的配位化合物,由丙戊酸钠和丙戊酸组成,具有抗惊厥和抗癫痫活性。 Divalproex 还可以通过抑制电压敏感的钠通道来抑制重复的神经元放电。
产品描述
Divalproex Sodium binds to and inhibits gamma-aminobutyric acid (GABA) transaminase and its anticonvulsant activity may be exerted by increasing brain concentration of GABA and by inhibiting enzymes that catabolize GABA or block the reuptake of GABA into glia and nerve endings. It also is an HDAC inhibitor. Divalproex Sodium is a stable coordination compound comprised of sodium valproate and valproic acid with anticonvulsant and antiepileptic activities. Divalproex may also work by suppressing repetitive neuronal firing through inhibition of voltage-sensitive sodium channels.
体外活性
Divalproex sodium enhances apoptosis, IM-induced cell growth inhibition and cell cycle arrest in K562-G and K562-S cells. It enhances the inhibitory effects of IM on SIRT1 expression in K562-G and K562-S cells. Divalproex sodium enhances the effect of IM on apoptosis in K562-G cells partly through SIRT1.
体内活性
Divalproex (500 mg/kg) significantly increases dopamine (DA) and acetylcholine (ACh) efflux in the rat hippocampus, and DA, but not ACh, efflux in the rat medial prefrontal cortex (mPFC), whereas 50 mg/kg has no effect on DA or ACh in either region. Divalproex (50 mg/kg) combined with the atypical APDs Olanzapine (1.0 mg/kg) or Aripiprazole (0.3 mg/kg) significantly potentiates the effect of both antipsychotic drugs (APDs) on DA, but not ACh efflux in the HIP and mPFC.
Cas No.
76584-70-8
分子式
C16H31NaO4
分子量
310.41
别名
Epival;双丙戊酸钠;Valproate semisodium
储存和溶解度
DMSO:58 mg/mL (186.8 mM)
H2O:57 mg/mL (183.6 mM)
Ethanol:58 mg/mL (186.8 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years