PF-04447943 is a potent, selective brain penetrant PDE9 inhibitor (Ki of 2.8, 4.5 and 18 nM) for human, rhesus and rat recombinant PDE9 respectively and high selectivity for PDE9 versus PDEs1-8 and 10-11.
Edelinontrine 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Male C57BL/6 mice
Aged mouse model
Intraperitoneal injection
1 mg/kg/day
Once daily for 10 days
To evaluate the effects of PF-04447943 on left ventricular function and pulmonary vascular resistance in aged mice. Results showed that PF-04447943 treatment significantly reduced pulmonary vascular resistance in aged mice but had no significant effect on left ventricular systolic or diastolic function.
Geroscience. 2024 Oct;46(5):5191-5202
Female C57BL/6 mice
DSS-induced colitis model
Oral gavage
3 mg/kg, 10 mg/kg, 30 mg/kg
Once daily for 7 days
To evaluate the protective effect of PF-04447943 on DSS-induced colitis, results showed that PF-04447943 attenuated colitis by suppressing oxidative stress and inflammation as well as reversing the Treg/Th17 cells imbalance.
Front Pharmacol. 2021 Apr 8;12:643215
Rats
BACHD transgenic rats (TG5)
Subcutaneous injection
3.2 mg/kg
Single administration, recording lasted 30-180 minutes
To assess the impact of PF-04447943 on corticostriatal transmission in WT and TG5 rats. Results showed that PF-04447943 significantly decreased the onset latency of cortically-evoked spikes in MSNs recorded in WT and TG5 rats and reversed deficits in spike probability observed in TG5 rats.
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