[¹⁸F]F13640: a selective agonist PET radiopharmaceutical for imaging functional 5-HT_1A receptors in humans.

ABSTRACT:

Purpose

F13640 (a.k.a. befiradol, NLX-112) is a highly selective 5-HT_1A receptor ligand that was selected as a PET radiopharmaceutical-candidate based on animal studies. Due to its high efficacy agonist properties, [¹⁸F]F13640 binds preferentially to functional 5-HT_1A receptors, which are coupled to intracellular G-proteins. Here, we characterize brain labeling of 5-HT_1A receptors by [¹⁸F]F13640 in humans and describe a simplified model for its quantification.

Methods

PET/CT and PET-MRI scans were conducted in a total of 13 healthy male volunteers (29 ± 9 years old), with arterial input functions (AIF) (n = 9) and test-retest protocol (n = 8). Several kinetic models were compared (one tissue compartment model, two-tissue

SUBMITTER: Courault P 

PROVIDER: S-EPMC10119077 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature