First reported nonpeptide AT1 receptor agonist (L-162,313) acts as an AT2 receptor agonist in vivo

• In this investigation, it is demonstrated that the first nonpeptide AT(1) 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 AT(2) receptor antagonist PD-123,319. The data strongly suggest that 1 is an AT(2) 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 AT(2) receptor.

Ämnesord

MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)

MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)

Nyckelord

Angiotensin II Type 1 Receptor Blockers

Animals

Binding

Competitive

Biphenyl Compounds/*pharmacology

Duodenum/drug effects/secretion

Female

Imidazoles/*pharmacology

Intestinal Mucosa/drug effects/secretion

Male

Myometrium/metabolism

Pyridines/Pharmacology

Radioligand Assay

Rats

Rats

Sprague-Dawley

Receptor

Angotnsin

Type 1/agonists

Receptor

Angiotensin

Type 2/*agonists/antagonists & inhibitors

Swine

Angiotensin II Type 1 Receptor Blockers

Publikations- och innehållstyp

ref (ämneskategori)

art (ämneskategori)