Effective block by pirfenidone, an antifibrotic pyridone compound (5-methyl-1-phenylpyridin-2[H-1]-one), on hyperpolarization-activated cation current: An additional but distinctive target.

ABSTRACT: Pirfenidone (PFD), a pyridone compound, is well recognized as an antifibrotic agent tailored for the treatment of idiopathic pulmonary fibrosis. Recently, through its anti-inflammatory and anti-oxidant effects, PFD based clinical trial has also been launched for the treatment of coronavirus disease (COVID-19). To what extent this drug can perturb membrane ion currents remains largely unknown. Herein, the exposure to PFD was observed to depress the amplitude of hyperpolarization-activated cation current (I_h) in combination with a considerable slowing in the activation time of the current in pituitary GH₃ cells. In the continued presence of ivabradine or zatebradine, subsequent application of PFD decreased I_h amplitude further. The presence of PFD resulted in

SUBMITTER: Chang WT 

PROVIDER: S-EPMC7276140 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature