THPP-1 是一种 SGC 推荐的化学探针, 是一种口服具有活性的磷酸二酯酶10A抑制剂,其对人和大鼠的Ki分别为 1 nM 和 1.3 nM。它的药理学特性良好。
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描述
THPP-1 is a potent and orally bioavailable inhibitor of PDE10A(Ki of 1 nM and 1.3 nM for human and rat PDE10A, respectively).
体内活性
Consistent with rodent data, both THPP-1 and risperidone significantly attenuated the stimulant effects in SIMA when administered alone, though some differences were noted.?Combination therapy with a low dose of risperidone produced significantly more robust effects.?THPP-1 and risperidone also produced a marked reduction of wake cycle time and gamma frequency power in EEG.?However, THPP-1 differed from risperidone by reducing spectral power of lower frequencies[1].
Cas No.
1257051-63-0
分子式
C23H21ClN6O3
分子量
464.9
储存和溶解度
DMSO:31 mg/mL (66.68 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years