Development of Fluorescent Probes that Target Serotonin 5-HT_2B Receptors.

ABSTRACT: Some 5-HT_2B fluorescent probes were obtained by tagging 1-(2,5-dimethoxy-4-iodophenyl)-propan-2-amine (DOI) with a subset of fluorescent amines. Some of the resulting fluorescent ligands showed excellent affinity and selectivity profiles at the 5-HT_2B receptors (e.g. 12b), while retain the agonistic functional behaviour of the model ligand (DOI). The study highlighted the most salient features of the structure-activity relationship in this series and these were substantiated by a molecular modelling study based on a receptor-driven docking model constructed on the basis of the crystal structure of the human 5-HT_2B receptor. One of the fluorescent ligands developed in this work, compound 12i, specifically labelled CHO-K1 cells expressing 5-HT_2B re

SUBMITTER: Azuaje J 

PROVIDER: S-EPMC5589878 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature