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      Angiotensin Tachyphylaxis in the Isolated Rabbit Aorta

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          The effect of modifications of the N-terminal end of the angiotensin II (AII) molecule on its ability to induce tachyphylaxis in the isolated rabbit aorta was studied by analyzing the effects of several analogs of AIL No tachyphylaxis to AII was observed, but (1-sarcosine)-AII, (1-guanido-acetic)-AII and (1-glycine)-AII induced marked tachyphylaxis. (1-Betaine)-AII, (2-lysine)-AII, (2-ornithine)-AII and (1-sarcosine,2-lysine)-AII were unable to induce tachyphylaxis in the rabbit aorta. A positively charged N terminus and the guanidino group of the Arg<sup>2</sup> side chain appear to be needed for the manifestation of the tachyphylactic property, while the Asp<sup>1</sup> side chain is responsible for the absence of tachyphylaxis to AII. It is proposed that the analogs that are able to induce tachyphylaxis, after binding to the receptor to produce the agonistic response, induce a slow conversion of the hormone-receptor complex into a tachyphylactic state, and that this conversion is promoted by the interaction of the N terminus and the guanidino group of the analog with their complementary sites.

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          Author and article information

          J Vasc Res
          Journal of Vascular Research
          S. Karger AG
          23 September 2008
          : 21
          : 2
          : 72-79
          Department of Biophysics, Escola Paulista de Medicina, São Paulo, Brazil
          158497 Blood Vessels 1984;21:72–79
          © 1984 S. Karger AG, Basel

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          Page count
          Pages: 8
          Research Paper


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