Synthesis of novel (benzimidazolyl)isoquinolinols and evaluation as adenosine A1 receptor tools.

ABSTRACT: G protein-coupled receptors (GPCRs) constitute the largest family of transmembrane receptors in eukaryotes. The adenosine A₁ receptor (A₁AR) is a class A GPCR that is of interest as a therapeutic target particularly in the treatment of cardiovascular disease and neuropathic pain. Increased knowledge of the role A₁AR plays in mediating these pathophysiological processes will help realise the therapeutic potential of this receptor. There is a lack of enabling tools such as selective fluorescent probes to study A₁AR, therefore we designed a series of (benzimidazolyl)isoquinolinols conjugated to a fluorescent dye (31-35, 42-43). An improved procedure for the synthesis of isoquinolinols from tetrahydroisoquinolinols via oxidation with 2,3-dichl

SUBMITTER: Singh S 

PROVIDER: S-EPMC9080270 | biostudies-literature | 2018 Apr

REPOSITORIES: biostudies-literature