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

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 se...

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Bibliographic Details
Published inJournal of medicinal chemistry Vol. 47; no. 6; pp. 1536 - 1546
Main Authors 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
Format Journal Article
LanguageEnglish
Published WASHINGTON Amer Chemical Soc 11.03.2004
Subjects
Chemistry, Medicinal
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Science & Technology
POTENT
SERIES
AFFINITY
TYPE-2 RECEPTOR
ANGIOTENSIN-II AT
BINDING INHIBITOR
ANTAGONISTS
DISCOVERY
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm031031i