Functional assessment of angiotensin II and bradykinin analogues containing the paramagnetic amino acid TOAC

International Immunopharmacology
Edson L SantosJoão B Pesquero

Abstract

This study characterized pharmacologically the functional responses to agonists angiotensin II (AngII) and bradykinin (BK) derivatives containing the TOAC (2,2,6,6-tetramethylpiperidine-N-oxyl-4-amino-4-carboxylic acid) spin label at the N-terminal (TOAC1-AngII and TOAC0-BK) and internal (TOAC3-AngII and TOAC3-BK) positions of these vasoactive peptides. Affinity constants of the ligands for AT1 and B2 receptors were evaluated in vitro by binding assays and biological effects by extracellular acidification rates and in vivo by blood pressure responses. In contrast to internally labeled analogues (TOAC3-AngII or TOAC3-BK), the TOAC1-AngII and TOAC0-BK derivatives dose-dependently increased the extracellular acidification rate in adherent cultured Chinese hamster ovary (CHO) cells expressing AT1 or B2 receptors, respectively. In addition, TOAC(1)-AngII induced an increase in blood pressure when injected intravenously in awaken rats although with a potency four times smaller when compared to native AngII. Similarly to BK, TOAC0-BK dose-dependently decreased blood pressure when injected intra-arterially in rats with a lower potency when compared to the native peptide. On the contrary, TOAC3-AngII or TOAC3-BK did not provoke any alte...Continue Reading

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Citations

Nov 19, 2008·International Journal of Radiation Biology·Daniela T NardiClovis R Nakaie
Jan 24, 2016·Journal of Pharmacological and Toxicological Methods·Renan P MartinSuma I Shimuta
Jun 25, 2009·Biochemical Pharmacology·Edson Lucas SantosJoão Bosco Pesquero
Mar 23, 2011·Hypertension·Paola B GuimarãesJoão B Pesquero
Jun 7, 2014·Chemical Reviews·Qingjun LiuPing Wang

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