| 产品描述： | 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 |
| 靶点： |
IC50: 1-1.3 nM (PDE10A) |
| 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. |
| 参考文献： |
1. Smith SM, et al. The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey. Neuropharmacology. 2013 Jan;64:215-23. 2. Vardigan JD, et al. Behavioral and qEEG effects of the PDE10A inhibitor THPP-1 in a novel rhesus model of antipsychotic activity. Psychopharmacology (Berl). 2016 Jul;233(13):2441-50. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.151 ml |
10.755 ml |
21.51 ml |
| 5 mM |
0.43 ml |
2.151 ml |
4.302 ml |
| 10 mM |
0.215 ml |
1.076 ml |
2.151 ml |
| 50 mM |
0.043 ml |
0.215 ml |
0.43 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京