Effects of 4(1H)-quinolinone derivative, a novel non-nucleotide allosteric purinergic P2Y ₂ agonist, on cardiomyocytes in neonatal rats.

ABSTRACT: Purinergic P2Y ₂ receptors, G-protein coupled receptors that primarily couple with Gα_q/11-proteins, are activated equipotently by adenosine-5'-triphosphate (ATP) and uridine-5'-triphosphate. Evidence suggests that P2Y ₂ agonists make potential drug candidates for the treatment of cardiovascular diseases. However, selective non-nucleotide, small-molecule P2Y ₂ agonists have yet to be developed. In this report, we discuss Compound 89, a novel non-nucleotide allosteric P2Y ₂ agonist that was active in signal transduction and gene induction, and in our in vitro cardiac hypertrophy model. Compound 89 exhibited selective P2Y ₂ agonistic activity and potentiated responses to the endogenous agonist ATP, while exhibiting no agonistic

SUBMITTER: Sakuma K 

PROVIDER: S-EPMC5519634 | biostudies-literature | 2017 Jul

REPOSITORIES: biostudies-literature