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  • 标题:Evidence for the AT1 Subtype of the Angiotensin II Receptor in the Rat Submandibular Gland
  • 本地全文:下载
  • 作者:Shigeru MATSUBARA ; Kiyoshige SAITO ; Yasuo KIZAWA
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2000
  • 卷号:23
  • 期号:10
  • 页码:1185-1188
  • DOI:10.1248/bpb.23.1185
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:We have characterized angiotensin II (Ang II) receptor subtypes on rat submandibular gland membranes using a radioligand binding assay. [3H]Ang II binding to the membrane fractions exhibited both high (Kd=0.08 nM, Bmax=2.19 fmol/mg protein) and low (Kd=4.19 nM, Bmax=13.7 fmol/mg protein) affinity. Ang II, Ang III and saralasin completely displaced the [3H]Ang II binding, whereas CV-11974, an AT1 receptor antagonist and PD123319, an AT2 receptor antagonist maximally displaced up to approximately 87 and 13% of the total binding, respectively. [3H]DuP753 binding to the membrane fractions exhibited a single population of binding site with a Kd of 4.22 nM and Bmax of 3.77 pmol/mg protein. Ang II, Ang III and CV-11974 completely displaced the [3H]DuP753 binding with slope factors near unity, but PD123319 did not. These findings suggest that rat submandibular gland membranes contain predominantly the AT1 receptor subtype.
  • 关键词:angiotensin II;AT1 receptor subtype;DuP753;CV-11074;submandibular gland
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