Trifluoperazine dihydrochloride is a synthetic high affinity KV4.3 blocker and is also an inhibitor of D1 and D2 dopamine receptors. Trifluoperazine dihydrochloride has an effective concentration of 5-300 μM with an IC50 of 8 μM on cloned KV4.3 channels. Trifluoperazine is hypothesized to block KV4.3 channel directly (and not through other protein mediation) and preferably in its open state. This is assumed due to findings showing Trifluoperazine decreaseing peak amplitude of KV4.3 but at the same time accelerating the apparent inactivation rate and the time-to-peak of the channel. Trifluoperazine is a widely used substance for the management of schizophrenia and other mental illnesses. Its anti-psychotic therapeutic effect is achieved through the blocking of post-synaptic D2 receptors in dopaminergic neurons.
产品描述
A Blocker of KV4.3 channel and an Inhibitor of D1 and D2 Dopamine Receptors
