| Chemical Properties | Back Directory | [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 | Back Directory | [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]
| [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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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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