产品
编 号：F098101
分子式：C23H21ClN6O3
分子量：464.9
分子式：C23H21ClN6O3
分子量：464.9
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1257051-63-0
产品详情
生物活性：
THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.
体内研究：
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 monkeyswere 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.
THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.
体内研究：
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 monkeyswere 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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