The Synthesis and Structural Requirements for Measuring Glucocorticoid Receptor Expression In Vivo with (±)-¹¹C-YJH08 PET.

ABSTRACT: Noninvasive methods to study glucocorticoid receptor (GR) signaling are urgently needed to elaborate the complexity of GR signaling in normal physiology and human disorders, as well as to identify selective GR modulators to treat diseases. Here, we report evidence supporting translational studies with (±)-¹¹C-5-(4-fluorobenzyl)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno[3,4-f]-quinoline ((±)-¹¹C-YJH08), a radioligand for PET that engages the ligand binding domain on GR. Methods: (±)-¹¹C-YJH08 was synthesized by reacting the phenol precursor with ¹¹C-methyl iodide. The biodistribution was studied in vivo. Specific binding was tested in vivo with adrenalectomy and ligand competition. A library of analogs was synthesized and studied i

SUBMITTER: Huang Y 

PROVIDER: S-EPMC8844266 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature