Preclinical Evaluation of Novel Positron Emission Tomography (PET) Probes for Imaging Leucine-Rich Repeat Kinase 2 (LRRK2).

ABSTRACT: Parkinson's disease (PD) is one of the most highly debilitating neurodegenerative disorders, which affects millions of people worldwide, and leucine-rich repeat kinase 2 (LRRK2) mutations have been involved in the pathogenesis of PD. Developing a potent LRRK2 positron emission tomography (PET) tracer would allow for in vivo visualization of LRRK2 distribution and expression in PD patients. In this work, we present the facile synthesis of two potent and selective LRRK2 radioligands [¹¹C]3 ([¹¹C]PF-06447475) and [¹⁸F]4 ([¹⁸F]PF-06455943). Both radioligands exhibited favorable brain uptake and specific bindings in rodent autoradiography and PET imaging studies. More importantly, [¹⁸F]4 demonstrated significantly highe

SUBMITTER: Chen Z 

PROVIDER: S-EPMC10895652 | biostudies-literature | 2024 Feb

REPOSITORIES: biostudies-literature