Sodium Valproate (1069-66-5)

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The mechanisms of therapeutic actions Valproic Acid (VPA) are not well understood. It may act by increasing gamma-aminobutyric acid levels in the brain or by altering the properties of voltage dependent sodium channels.
VPA, or its sodium salt, dissociates to the valproate ion in the gastrointestinal tract or in the blood and then binds to and inhibits GABA transaminase. Therefore, the drug’s anticonvulsant activity may be, at least partly, related to increased brain concentrations of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter in the CNS, by inhibiting enzymes that catabolize GABA or block the reuptake of GABA into glia and nerve endings. Both these actions increase concentrations of GABA in the brain. A second major hypothesis for VPA’s action is that it enhances neuronal responsiveness to GABA. All these actions result in potentiation of the synaptic actions of GABA.
Other actions that may contribute to VPA’s therapeutic effects include a decrease in dopamine turnover, a decrease in the activity of the NMDA-glutamate receptors and also a decrease in the concentration of somatostatin in the CSF.
VPA may also work by suppressing repetitive neuronal firing through inhibition of voltage-sensitive sodium channels, thereby creating a direct membrane-stabilizing effect. Some studies suggest that VPA may also affect potassium channels.
VPA is also likely to produce its anti-manic effects through its GABAergic effects, where VPA leads to a rise in cerebral and cerebellar levels of GABA, possibly by inhibiting GABA degradative enzymes, such as GABA transaminase and succinate-semialdehyde dehydrogenase, and also by inhibiting the re-uptake of GABA by neuronal cells.

Packaging: Polyethylene nylon plastic bag

Storage conditions: Preserve in an airtight container.

CAS Number:  1069-66-5

Formula:  C8H15NaO2

Molecular Weight:  166.2 g/mol

Method of Analysis: BP Monograph


Valproic acid is a branched short-chain fatty acid and a derivative of valeric or pentanoic acid which is a straight-chain alkyl carboxylic acid. Valproate, and its sodium valproate and valproate semisodium forms, are medications primarily used to treat epilepsy and bipolar disorder and to prevent migraine headaches. In epilepsy, Valproate has a broad spectrum of anticonvulsant activity, but is primarily used as a first-line treatment for tonic-clonic seizures, absence seizures and myoclonic seizures and as a second-line treatment for partial seizures and infantile spasms. It has also been successfully given intravenously to treat status epilepticus. In bipolar disorder, Valproate products are also used to treat manic or mixed episodes of bipolar disorder. Valproic acid is also a histone deacetylase inhibitor 1 (HDAC1). HDAC1 is needed for HIV to remain in infected cells and, therefore, the drug is under investigation for treatment of HIV as well as various cancers.