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Rimtuzalcap is a novel modulator of small-conductance calcium-activated potassium channels that is under investigation for the treatment of essential tremor.
Rimtuzalcap is a novel modulator of small-conductance calcium-activated potassium channels that is under investigation for the treatment of essential tremor.
Rimtuzalcap is a positive allosteric modulator of small-conductance calcium-activated K+ channels (SK channels). It is thought to exert its activity on essential tremor through increasing SK channel activity in the Purkinje cells of the cerebellar cortex resulting in hyperpolarization and consequently, a slower firing rate. These Purkinje cells have a glutamatergic excitatory input to deep cerebellar neurons in the dentate nucleus which themselves exert the same input on the ventral intermediate nucleus in the thalamocortical system. From there the ventral intermediate nucleus exerts excitatory input to the motor cortex, producing an effect on motor function. It is the decrease in the activity of this pathway through targeting Purkinje cell firing rate that is thought to have a beneficial impact on essential tremor.
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