Zandatrigine is a selective inhibitor of the voltage-gated sodium channel NaV1.6 (SCN8A), exhibiting potent activity at the blood-brain barrier. By non-covalently binding to the VSD4 region of NaV1.6, Zandatrigine effectively blocks sodium influx, thereby mitigating persistent currents associated with pathological conditions. This compound has demonstrated a significant ability to reduce neuronal hyperexcitability and decrease the frequency of epileptic seizures. With 134-756-fold selectivity over other sodium channel isoforms such as NaV1.1 and NaV1.2, Zandatrigine serves as a valuable tool in research focused on SCN8A-related developmental epileptic encephalopathy (SCN8A-DEE) and adult focal epilepsy.
Zandatrigine is a selective inhibitor of the voltage-gated sodium channel NaV1.6 (SCN8A), exhibiting potent activity at the blood-brain barrier. By non-covalently binding to the VSD4 region of NaV1.6, Zandatrigine effectively blocks sodium influx, thereby mitigating persistent currents associated with pathological conditions. This compound has demonstrated a significant ability to reduce neuronal hyperexcitability and decrease the frequency of epileptic seizures. With 134-756-fold selectivity over other sodium channel isoforms such as NaV1.1 and NaV1.2, Zandatrigine serves as a valuable tool in research focused on SCN8A-related developmental epileptic encephalopathy (SCN8A-DEE) and adult focal epilepsy.
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