Development of angiotensin II antagonists with equipotent affinity for human AT1 and AT2 receptor subtypes.

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Abstract

The quinazoline sulfonylcarbamate L-163,579 (9) is a potent, balanced antagonist of the binding of angiotensin II (Ang II) to human AT1 and AT2 receptors. This antagonist produces a long-lasting blockade of Ang II-induced pressor response in both rats and dogs after oral administration.

L-163,579 is an Ang II antagonists with equipotent binding to both AT1 and AT2 human receptor subtypes. In vivo characterization of L-163,579 in rats and dogs showed sustained balanced activity and good efficacy by both i.v. and oral administration.

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References (18)

  • T.W. Glinka et al.

    Biorganic and Med. Chem. Lett.

    (1994)
    E.M. Naylor et al.

    Biorganic Med Chem. Lett.

    (1994)
  • P.K.S. Siegl et al.

    J. Pharm. Exp. Ther.

    (1992)
  • R.R. Wezler et al.

    Am. J. Hypertension

    (1992)
  • P.B.M.W.M. Timmermans et al.

    J. Hypertension

    (1992)
  • P.B.M.W.M. Timmermans et al.

    Am. J. Hypertension

    (1992)
  • Y. Christen et al.

    Circulation

    (1991)
  • S.E. de Laszlo et al.

    Bioorganic and Med. Chem. Lett.

    (1993)
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