Synthesis and In Vitro and In Vivo Evaluation of [3H]LRRK2-IN-1 as a Novel Radioligand for LRRK2.

摘要: Purpose LRRK2 (leucine-rich repeat kinase 2) has recently been proven to be a promising drug target for Parkinson’s disease (PD) due an apparent enhanced activity caused by mutations associated with familial PD. To date, there have no reports in which LRRK2 inhibitor radiolabeled and used vitro or vivo studies of LRRK2. In the present study, we ligand, LRRK-IN-1, purposes performing (IC50, Kd, Bmax, autoradiography) (biodistribution, blocking experiments) evaluations rodents human striatum tissues.