First reported nonpeptide AT(1) receptor agonist (L-162,313) acts as an AT(2) receptor agonist in vivo

作者:Wan YQ; Wallinder C; Johansson B; Holm M; Mahalingam AK; Wu XY; Botros M; Karlen A; Pettersson A; Nyberg F; Fandriks L; Hallberg A; Alterman M*
来源:Journal of Medicinal Chemistry, 2004, 47(6): 1536-1546.
DOI:10.1021/jm031031i

摘要

In this investigation, it is demonstrated that the first nonpeptide AT, receptor agonist L-162,313 (1), disclosed in 1994, also acts as an agonist at the AT(2) receptor. In anesthetized rats, administration of compound 1 intravenously or locally in the duodenum increased duodenal mucosal alkaline secretion, effects that were sensitive to the selective AT2 receptor antagonist PD-123,319. The data strongly suggest that 1 is an AT2 receptor agonist in vivo. To the best of our knowledge, this substance is the first nonpeptidic low-molecular weight compound with an agonistic effect mediated through the AT2 receptor.

  • 出版日期2004-3-11