Dually Labeled Neurotensin NTS₁R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays.

ABSTRACT: The determination of ligand-receptor binding affinities plays a key role in the development process of pharmaceuticals. While the classical radiochemical binding assay uses radioligands, fluorescence-based binding assays require fluorescent probes. Usually, radio- and fluorescence-labeled ligands are dissimilar in terms of structure and bioactivity, and can be used in either radiochemical or fluorescence-based assays. Aiming for a close comparison of both assay types, we synthesized tritiated fluorescent neurotensin receptor ligands ([³H]13, [³H]18) and their nontritiated analogues (13, 18). The labeled probes were studied in radiochemical and fluorescence-based (high-content imaging, flow cytometry, fluorescence anisotropy) binding assays.

SUBMITTER: Ertl FJ 

PROVIDER: S-EPMC11440508 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature