Nonpeptide angiotensin II receptor antagonists

An Essential Role of Angiotensin II Receptor Type 1a in Recipient Kidney, Not in Transplanted Peripheral Blood Leukocytes, in Progressive Immune-Mediated Renal Injury

“…Accumulating evidence indicates that AII also has nonhemodynamic actions, promoting cell growth and extracellular matrix protein synthesis (Matsusaka et al, 1996;Owens, 1989). These biologic actions of AII are mediated predominantly by AT1 subtype receptors (Griendling et al, 1996;Timmermans et al, 1991). In rodents, AT1 exists as two isoforms, AT1a and AT1b, encoded by two different genes (Iwai and Inagami, 1992;Sasamura et al, 1992); AT1a has predominantly physiologic roles in the mouse (Burson et al, 1994).…”

“…A ngiotensin II (AII), a bioactive peptide in the reninangiotensin system, plays a key role in hemodynamic regulation such as the control of blood pressure, salt, and fluid homeostasis (Griendling et al, 1996;Hall and Guyton, 1990;Timmermans et al, 1991). Accumulating evidence indicates that AII also has nonhemodynamic actions, promoting cell growth and extracellular matrix protein synthesis (Matsusaka et al, 1996;Owens, 1989).…”

Identification of atypical (non‐AT1, non‐AT2) angiotensin binding sites with high affinity for angiotensin I on IEC‐18 rat intestinal epithelial cells

“…4). However, neither the ATl-specific antagonist, DuP 753 [13 15], nor the AT2-specific antagonist, PD 123319 [13][14][15], had any effect on [~25I]Ang I binding to IEC-18 cells, even when these agents were present at micromolar concentrations (Fig. 4) [20]) with an IDs0 of ~ 3 nM (data not shown).…”

Angiotensin II receptor pharmacology and AT1-receptor blockers

“…This was the basis for the further development of highly specific and selective angiotensin AT 1 -receptor binding substances such as losartan, [16][17][18][19] valsartan, [20][21][22][23] irbesartan, [24][25][26][27] candesartan, 28 eprosartan, 29 telmisartan, 30 and others (overview 31 ), and AT 2 -receptor ligands/antagonists, for example, PD123177, PD123319, and CGP42112. 32,33 Ang II receptor subtypes…”