7.2. Angiotensin II Receptor Blockers (ARB)

Table 2: Adverse Reactions Occurring in ≥ 4% of Patients Treated with Angiotensin II and ≥ 1.5% More Often than in Placebo-treated Patients in ATHOS-3

Nonpeptide angiotensin II receptor antagonists. 2. …

Ang II is formed by cleavage of Ang I by the angiotensin-converting enzyme (ACE) or chymases.

Synthesis angiotensin 2 | erunfeticorliynerahornore

Matsumoto E, Sasaki S, Kinoshita H, KitoT, Ohta H, Konishi M, Kuwahara K, Nakao K and Itoh N: AngiotensinII-induced cardiac hypertrophy and fibrosis are promoted in micelacking Fgf16. Genes Cells. 18:544–553. 2013. : :

Angiotensin 1/2 (1-7) amide|Vasoconstrictor

Matsumoto E, Sasaki S, Kinoshita H, KitoT, Ohta H, Konishi M, Kuwahara K, Nakao K and Itoh N: AngiotensinII-induced cardiac hypertrophy and fibrosis are promoted in micelacking Fgf16. Genes Cells. 18:544–553. 2013. : :

T1 - Regulation of vascular proteoglycan synthesis by angiotensin II type 1 and type 2 receptors

Renoprotective Effect of the Angiotensin-Receptor Antagonist

A series of non-sulfhydryl modified dipeptides related to CI-906, CI-907, and enalapril was prepared in which various isosteric moieties (O, S, SO, SO2) have been substituted for the amino group and in which the proline residue has been replaced with various hydrophobic amino acids. The compounds were evaluated in vitro for inhibition of angiotensin-converting enzyme and in vivo for antihypertensive activity. Compound 7c, the most potent member of this series, had an in vitro IC50 of 1.4 × 10-8 M and showed modest oral antihypertensive activity at 30 mg/kg in conscious, two kidney, one clip Goldblatt hypertensive rats. Structure-activity relationships are discussed.

T1 - Angiotensin II Type 2 receptors stimulate collagen synthesis in cultured vascular smooth muscle cells

Renin–angiotensin system - Wikipedia

ACE-mediated cleavage of Angiotensin I appears to occur constitutively and is not a subject to regulation; however, inhibition of ACE does represent an important locus of pharmacological modulation of the RAAS.

T1 - Synthesis and biological activity of modified peptide inhibitors of angiotensin-converting enzyme

Reductive Amination of Aldehydes and Ketones ..

N2 - A concise enantiospecific synthesis of the angiotensin converting enzyme inhibitor (-)-A58365A (7) has been achieved following a strategy in which a vinylogous Mannich reaction and a lactone-lactam rearrangement served as the key transformations. The trimethylsilyloxyfuran derived from 25, which was prepared from the known sulfoxide 16, served as the nucleophilic partner in a vinylogous Mannich reaction with the chiral N-acyliminium ion that was generated in situ from the aminal 26. Addition of a further quantity of TMSOTf cleaved the N-Boc group from the adducts 27 to give a mixture of diastereomeric amino butenolides 28. Treatment of this mixture with LiOMe/MeOH furnished 10, and acid-catalyzed hydrolysis of the methyl ester groups delivered (-)-A58365A in 37% overall yield over the longest linear sequence of eight steps.

Concomitant use of angiotensin converting enzyme (ACE) inhibitors may increase the response to angiotensin II.

Angiotensin-Receptor Blockade versus …

AB - Xenopus laevis oocytes were injected with poly(A)+ mRNA isolated from rat brain and superfused in a medium containing either serotonin, angiotensin II or bradykinin. Applications of serotonin or angiotensin II to injected oocytes elicited, in a dose-dependent manner, changes in membrane potential. The angiotensin II receptor was desensitized fairly rapidly in the continued presence of the agonist. No response was obtained with bradykinin. The selectivity of the angiotensin II-induced response was demonstrated by the finding that the angiotensin II antagonist ([Sar1,Ala8]angiotensin II, saralasin) blocked the angiotensin II-induced response. It is concluded that an appropriate fraction of brain mRNA is capable of directing the synthesis and correct insertion of functional angiotensin II receptors in the Xenopus oocyte membrane.