Rimtuzalcap (CAD-1883) 是首创的，选择性的小电导钙激活钾通道 (SK 通道) 正变构调节剂。Rimtuzalcap 可用于运动障碍的研究，包括特发性震颤 (ET) 和脊髓小脑性共济失调 (SCA)。
Rimtuzalcap (CAD-1883) is a first-in-class selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels). Rimtuzalcap can be used for the research of movement disorders including essential tremor (ET) and spinocerebellar ataxia (SCA)[1].
Rimtuzalcap (Compound 1) is a small molecule modulator of potassium ion channels showing great therapeutic potential for treating a variety of diseases characterized by dysfunction of potassium ion channels and dysfunction from other causes which influence these potassium channels[1].
Rimtuzalcap (CAD-1883) reduces the firing rate of Purkinje cells by approximately 40%, consistent with the anticipated therapeutic mechanism of positive allosteric modulation of SK channels. Sequential bath application of 1 or 3 µM CAD-1883 results in a partial reversal of the increased coefficient of variation of the interspike interval which is seen in cerebellar slices from 11-month-old spinocerebellar ataxia-2 58Q mice[1].
[1]. Crystalline forms of potassium channel modulators. WO2020086456A1.
动态评分
0.0