Development of a triazolobenzodiazepine-based PET probe for subtype-selective vasopressin 1A receptor imaging.

ABSTRACT:

Objectives

To enable non-invasive real-time quantification of vasopressin 1A (V1A) receptors in peripheral organs, we sought to develop a suitable PET probe that would allow specific and selective V1A receptor imaging in vitro and in vivo.

Methods

We synthesized a high-affinity and -selectivity ligand, designated compound 17. The target structure was labeled with carbon-11 and tested for its utility as a V1A-targeted PET tracer by cell uptake studies, autoradiography, in vivo PET imaging and ex vivo biodistribution experiments.

Results

Compound 17 (PF-184563) and the respective precursor for radiolabeling were synthesized in an overall yield of 49% (over 7 steps) and 40% (over 8 steps), respectively. An inhibitory constant of 0.9 nM towards the V1A receptors was measu

SUBMITTER: Haider A 

PROVIDER: S-EPMC8581590 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature