Literature DB >> 1323478

The selective endothelin ETA receptor antagonist BQ123 antagonizes endothelin-1-mediated mitogenesis.

E H Ohlstein1, A Arleth, H Bryan, J D Elliott, C P Sung.   

Abstract

The mitogenic effects of endothelin isopeptides and the selective ETA receptor antagonist BQ123 were evaluated in rat aortic vascular smooth muscle cells. Endothelin-1 (ET-1) and endothelin-3 (ET-3) produced concentration-dependent increases in [3H]thymidine incorporation (EC50 = 0.1 and 25 nM, respectively). The ETB-selective agonist sarafotoxin 6c did not produce significant effects on [3H]thymidine incorporation. BQ123 produced selective and concentration-dependent inhibition of ET-1-mediated [3H]thymidine incorporation. These data demonstrate that ET-1-mediated mitogenesis in vascular smooth muscle is mediated by ETA receptors.

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Year:  1992        PMID： 1323478     DOI： 10.1016/0922-4106(92)90109-9

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN： 0014-2999            Impact factor:   4.432


  20 in total

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