Premium
A novel ET A antagonist (BQ‐123) inhibits endothelin‐1‐induced phosphoinositide breakdown and DNA synthesis in rat vascular smooth muscle cells
Author(s) -
Eguchi Satoru,
Hirata Yukio,
Ihara Masaki,
Yano Mitsuo,
Marumo Fumiaki
Publication year - 1992
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(92)80451-l
Subject(s) - vascular smooth muscle , dna synthesis , inositol , endothelin 1 , antagonist , endothelin receptor , endocrinology , medicine , biology , microbiology and biotechnology , receptor antagonist , pentapeptide repeat , endothelins , inositol phosphate , receptor , chemistry , dna , biochemistry , smooth muscle , peptide
The effects of a novel cyclic pentapeptide (BQ‐123), an endothelin (ET) antagonist selective for the ET A receptor subtype, on phosphoinositide breakdown and DNA synthesis stimulated by ET‐1 were studied in cultured rat vascular smooth muscle cells (VSMC). BQ‐123 competitively inhibited the binding of [ 125 I]ET‐1 to VSMC with the apparent K i of 4 × 10 −9 M. BQ‐123 dose‐dependently inhibited formation of inositol‐1,4,5‐trisphosphate and [ 3 H]thymidine uptake stimulated by ET‐1. These data suggest that the ET‐1‐induced DNA synthesis in VSMC is mainly mediated by ET A receptor subtype.