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ACS Med Chem Lett. 2014 Aug 18;5(10):1129-32. doi: 10.1021/ml500278g. eCollection 2014 Oct 9.

Saralasin and Sarile Are AT2 Receptor Agonists.

Author information

1
Service of Endocrinology and Department of Physiology and Biophysics, Faculty of Medicine, Université de Sherbrooke , Sherbrooke, J1H 5N4 Quebec, Canada.
2
Beijer Laboratory, Department of Pharmaceutical Biosciences, BMC, Uppsala University , SE-751 24 Uppsala, Sweden.
3
Department of Medicinal Chemistry, BMC, Uppsala University , SE-751 23 Uppsala, Sweden.

Abstract

Saralasin and sarile, extensively studied over the past 40 years as angiotensin II (Ang II) receptor blockers, induce neurite outgrowth in a NG108-15 cell assay to a similar extent as the endogenous Ang II. In their undifferentiated state, these cells express mainly the AT2 receptor. The neurite outgrowth was inhibited by preincubation with the AT2 receptor selective antagonist PD 123,319, which suggests that the observed outgrowth was mediated by the AT2 receptor. Neither saralasin nor sarile reduced the neurite outgrowth induced by Ang II proving that the two octapeptides do not act as antagonists at the AT2 receptor and may be considered as AT2 receptor agonists.

KEYWORDS:

AT2 receptor agonist; C21/M024; Saralasin; peptide ligands; sarile

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