THPP-1

生物活性靶点体内研究 THPP-1 试剂级价格

THPP-1

CAS号:1257051-63-0
英文名:THPP-1
中文名:THPP-1
CBNumber:CB06127943
分子式:C23H21ClN6O3
分子量:464.9
MOL File:1257051-63-0.mol

THPP-1化学性质

密度 :1.45±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO: 31.25 mg/mL (67.22 mM)
形态 :A solid
酸度系数(pKa) :4.70±0.30(Predicted)
颜色 :Off-white to light yellow

THPP-1性质、用途与生产工艺

生物活性 THPP-1 是SGC推荐的一个化学探针，是有效的、具有口服活性的磷酸二酯酶10A (PDE10A) 的抑制剂，其对人和大鼠的 Ki 值分别为 1 nM 和 1.3 nM。THPP-1 具有良好的药理学特性。
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.