Fluorescent A_2A and A₃ adenosine receptor antagonists as flow cytometry probes.

ABSTRACT: Adenosine receptor (AR) ligands are being developed for metabolic, cardiovascular, neurological, and inflammatory diseases and cancer. The ease of drug discovery is contingent on the availability of pharmacological tools. Fluorescent antagonist ligands for the human A_2A and A₃ARs were synthesized using two validated pharmacophores, 1,3-dipropyl-8-phenylxanthine and triazolo[1,5-c]quinazolin-5-yl)amine, which were coupled to eight reporter fluorophores: AlexaFluor, JaneliaFluor (JF), cyanine, and near infrared (NIR) dyes. The conjugates were first screened using radioligand binding in HEK293 cells expressing one of the three AR subtypes. The highest affinities at A_2AAR were K_i 144-316 nM for 10, 12, and 19, and at A₃AR affinity of K

SUBMITTER: Toti KS 

PROVIDER: S-EPMC10539269 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature