1257051-63-0
1257051-63-0 structure
- Name: THPP-1
- Chemical Name: THPP-1
- CAS Number: 1257051-63-0
- Molecular Formula: C23H21ClN6O3
- Molecular Weight: 464.90
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
- Create Date: 2020-01-24 01:01:51
- Modify Date: 2025-08-24 19:48:27
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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].
| Name | THPP-1 |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
IC50: 1-1.3 nM (PDE10A)[1]. |
| 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. |
| References |
| Molecular Formula | C23H21ClN6O3 |
|---|---|
| Molecular Weight | 464.90 |