Synthesis and Evaluation of Benzylic ¹⁸F-Labeled N-Biphenylalkynyl Nipecotic Acid Derivatives for PET Imaging of GABA Transporter 1.

ABSTRACT: As the main inhibitory neurotransmission system, the GABAergic system poses an interesting yet underutilized target for molecular brain imaging. While PET imaging of postsynaptic GABAergic neurons has been accomplished using radiolabeled benzodiazepines targeting the GABA_A receptor, the development of presynaptic radioligands targeting GABA transporter 1 (GAT1) has been unsuccessful thus far. Therefore, we developed a novel GAT1-addressing radioligand and investigated its applicability as a PET tracer in rodents. We selected a lipophilic nipecotic acid scaffold that is known to bind selectively to GAT1 as the basis for our radioligand. To obtain the desired candidate radiotracer [¹⁸F]4, ester-protected radioligands [¹⁸F

SUBMITTER: Knippenberg N 

PROVIDER: S-EPMC11843609 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature