THPP-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

THPP-1 是一种有效的口服生物可利用的 PDE10A 抑制剂（人和大鼠 PDE10A 的 Ki 值分别为 1 nM 和 1.3 nM）。

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). 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.

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THPP-1 (0.1-1.0 mg/kg, p.o.) shows novel object recognition in rats.THPP-1 (p.o., 1-30 mg/kg) dose-dependently increases phosphorylation of GluR1 S845 in the rat striatum whereas the total levels of GluR1 in the striatum are not affected. Administration of THPP-1 also results in an associated increase in the pGluR1/GluR1 ratios at all doses examined in this study.THPP-1 (1, 3, 10 mg/kg, p.o.) significantly attenuated the stimulant effects in stimulant-induced motor activity (SIMA) in monkey. Animal Model:Male Wistar Hannover rats ranging from 200 to 300 g.Dosage:0.1-1.0 mg/kg.Administration:P.O.Result:Showed novel object recognition.Animal Model:Eleven monkeys were surgically implanted with subcutaneous telemetric devices to permit the simultaneous recording of electrocorticogram (ECoG), electrooculogram (EOG), and electromyogram (EMG) activit Dosage:1, 3, 10 mg/kg. Administration:P.O.Result:Significantly attenuated the stimulant effects in SIMA.Animal Model:Male Wistar Hannover rats ranging from 200 to 300 g.Dosage:1-30 mg/kg.Administration:P.O. (10% Tween 80/90% water) 2 h prior to tissue collection (Pharmacokinetic Analysis).Result:Dose-dependently increases phosphorylation of GluR1 S845.

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Angiogenesis

PDE

PDE10A

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1257051-63-0

464.9

C23H21ClN6O3

>98% (HPLC)

DMSO:31 mg/mL (66.68 mM; Need ultrasonic)

COCCOC1=C2CN(CCC2=NC(=N1)C1=CC=C(Cl)N=C1)C(=O)C1=C2C=CC=CN2C=N1

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(-20℃)

With Ice Pack

≥ 2 years