ChemicalBook CAS DataBase List 1257051-63-0

1257051-63-0

Name	THPP-1
CAS	1257051-63-0
Molecular Formula	C23H21ClN6O3
Molecular Weight	464.9
MOL File	1257051-63-0.mol

Chemical Properties

density	1.45±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO: 31.25 mg/mL (67.22 mM)
form	A solid
pka	4.70±0.30(Predicted)
color	Off-white to light yellow

Hazard Information

Uses

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[1].

Biological Activity

THPP-1, a chemical probe recommended by SGC, is a potent and orally active inhibitor of phosphodiesterase 10A (PDE10A) with Ki values of 1 nM and 1.3 nM for human and rat, respectively. THPP-1 has good pharmacological properties.

in vivo

THPP-1 (0.1-1.0 mg/kg, p.o.) shows novel object recognition in rats^[1].
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^[1].
THPP-1 (1, 3, 10 mg/kg, p.o.) significantly attenuated the stimulant effects in stimulant-induced motor activity (SIMA) in monkey^[2].

Animal Model:	Male Wistar Hannover rats ranging from 200 to 300 g^[1].
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^[1].
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.

target

IC50: 1-1.3 nM (PDE10A).

IC 50

PDE10

storage

Store at -20°C

References

[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. DOI:10.1016/j.chembiol.2019.11.004
[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. DOI:10.1007/s00213-016-4290-1

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