CyPPA 是hSK2和hSK3的阳性调节剂,其EC50值分别为 5.6 μM 和14 μM。它对 hSK1 和 hIK 通道无活性。
产品描述
CyPPA, a subtype-selective positive modulator of SK channels, decreased spontaneous firing rate, increased the duration of the apamin-sensitive afterhyperpolarization.
体外活性
CyPPA, a positive modulator of SK2 and SK3, reduces the activity of dopaminergic neurons and inhibits dopamine release with EC50 values of 14 μM and 5.6 μM, repectively. CyPPA counteracts hyperdopaminergic behaviors induced by methylphenidate.
体内活性
In vivo studies revealed that systemic administration of CyPPA attenuated methylphenidate-induced hyperactivity and stereotypic behaviors in mice. CyPPA induces a concentration-dependent increase in the apparent Ca2+ sensitivity of channel activation, changing the EC50 (Ca2+) from 429 nM to 59 nM
Cas No.
73029-73-9
分子式
C16H23N5
分子量
285.4
储存和溶解度
DMSO:99 mg/mL (346.89 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years