PFE-360 , also known as PF-06685360, is a potent, selective, brain-penetrating and orally active LRRK2 inhibitor with an in vivo mean IC50 value of 2.3 nM[1][2].
PFE-360 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Sprague Dawley rats
RAAV2/1-mediated A53T-αsynuclein overexpression model
Oral
10 mg/kg
Twice daily for 28 days
To evaluate the neuroprotective effects of PFE-360 against dopaminergic neurodegeneration caused by A53T-αsynuclein overexpression, results showed PFE-360 failed to provide neuroprotection.
Brain Res. 2021 May 15;1759:147372
Female Sprague Dawley rats
AAV-α-synuclein overexpression rat model
Oral gavage
7.5 mg/kg
Twice daily for 10-12 weeks
To evaluate the effect of chronic LRRK2 inhibition on α-synuclein-induced neuronal dysfunction. Results showed that PFE-360 induced only a marginal effect on motor function but had no significant effect on STN burst firing, DAergic neurodegeneration, α-synuclein expression or phosphorylation.
eNeuro. 2019 Dec 19;6(6):ENEURO
PFE-360 动物研究
Animal study
Administered orally, BID, for 10-12 weeks at doses of 4 mg/kg and 7.5 mg/kg, PFE-360 effectively reduced the LRRK2-pSer935/ total LRRK2 ratio without significant adverse effects[1][2].
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