Exploration of (R)-[¹¹C]YH168 as a PET tracer for imaging monoacylglycerol lipase in the brain: from mice to non-human primates.

ABSTRACT:

Purpose

The monoacylglycerol lipase (MAGL) plays a pivotal role in modulating the endocannabinoid system and is considered an attractive therapeutic target for diseases in both the central nervous system and periphery. The current study aimed to develop and evaluate a suitable carbon-11 labeled tracer for imaging MAGL in preclinical studies.

Methods

(R)-YH168 was synthesized via a multi-step pathway and its half-maximal inhibitory concentration (IC₅₀) values were measured using an enzymatic assay. Radiosynthesis of (R)-[¹¹C]YH168 was accomplished by ¹¹C-methylation via Suzuki cross-coupling of a pinacol boron precursor. In vitro autoradiography was performed using brain tissues from MAGL knockout and the corresponding wild-type mice. The meta

SUBMITTER: He Y 

PROVIDER: S-EPMC11839854 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature