Synthesis and biological activities of [β-malyl1]- and [β-Malyl1, Leu8]-angiotensin II analogues

1983 ◽  
Vol 39 (4) ◽  
pp. 353-355 ◽  
Author(s):  
P. Cordopatis ◽  
J. Matsoukas ◽  
A. Michel ◽  
J. Janen ◽  
D. Theodoropoulos
Keyword(s):  
Angiotensin Ii ◽  
Biological Activities ◽  
Angiotensin Ii Analogues

Synthesis and biological activities of [Aze7]- and [Pip7]-angiotensin II analogues

Peptides 1990 ◽  
1991 ◽  
pp. 659-660 ◽  
Author(s):  
J. Matsoukas ◽  
J. Hondrelis ◽  
G. Agelis ◽  
R. Yamdagni ◽  
R. C. Ganter ◽  
...  
Keyword(s):  
Angiotensin Ii ◽  
Biological Activities ◽  
Angiotensin Ii Analogues

Angiotensin II Analogues and Aldosterone Secretion in Sodium-Deficient Sheep

1976 ◽  
Vol 51 (s3) ◽  
pp. 325s-327s
Author(s):  
J. R. Blair-West ◽  
J. P. Coghlan ◽  
D. A. Denton ◽  
H. D. Niall ◽  
B. A. Scoggins ◽  
...  
Keyword(s):  
Angiotensin Ii ◽  
Enzyme Inhibitor ◽  
Agonist Activity ◽  
Converting Enzyme ◽  
Aldosterone Secretion ◽  
Arterial Infusion ◽  
Sodium Deficiency ◽  
Converting Enzyme Inhibitor ◽  
Angiotensin Ii Analogues ◽  
Permissive Role

1. The angiotensin analogues Sar1-Ala8-angiotensin II (AII), Sar1-Ile8-AII, Sar1-Leu8-AII, Sar1-Thr8-AII, [Des1-Asp]-Ile8-AII and [Des1-Asp]-Sar2-Ile8-AII and converting enzyme inhibitor (SQ 80221) infused by intra-adrenal arterial infusion had no effect on aldosterone secretion in sodium-deficient sheep at doses in excess of those shown to block exogenous angiotensin II or III infusion. 2. It is suggested that the intrinsic agonist activity of the analogues may fulfil the requirements for a permissive role for angiotensin in the aldosterone response to sodium deficiency.

The Pressor and Myotropic Effects and the Antagonistic Properties of Several Analogues of Angiotensin II

1972 ◽  
Vol 50 (2) ◽  
pp. 99-112 ◽  
Author(s):  
D. Regoli ◽  
W. K. Park
Keyword(s):  
Angiotensin Ii ◽  
Chemical Structure ◽  
Biological Activities ◽  
Unnatural Amino Acid ◽  
Intrinsic Activity ◽  
Rat Stomach ◽  
Response Curves ◽  
Isolated Organs ◽  
The Right ◽  
The Relationship

The substitution of an unnatural amino acid, 1-aminocyclopentanecarboxylic acid (Acpc), for each of the eight amino acids of angiotensin (AT) has been used to study the relationship between chemical structure and biological activities of angiotensin. The pressor and the myotropic activities of the various ATII derivatives have been tested on the rat blood pressure and on three isolated organs: rat isolated colon, rat stomach strip, and rabbit isolated kidney.The results indicate that 6-His and 8-Phe are essential for the activities of angiotensin II. Moreover, (8-Acpc)-ATII, but not (6-Acpc)-ATII, antagonizes the pressor and myotropic effects of ATII and ATI. αE and pD2 of all analogues have been estimated on the isolated rat stomach strip to evaluate intrinsic activity and affinity for the receptors. (1-, (2-, (3-, (4-, and (5-Acpc)-ATII have the same intrinsic activities as ATII, while those of (6-, (7-, and (8-Acpc)-ATII are much lower.Analogues of ATII substituted in position 8 antagonize specifically the myotropic and pressor effects of ATII and ATI. On the contrary, the effects of other smooth muscle stimulating agents (acetylcholine, 5-hydroxytryptamine, bradykinin, and vasopressin) are not modified.Log dose response curves of ATII and ATI are shifted to the right in the presence of antagonists, but remain parallel. The antagonism is rapidly reversible and may be competitive.

The Enzymatic Degradation of Angiotensin II Analogues by proteolytic enzyme in vitro

1972 ◽  
Vol 50 (2) ◽  
pp. 113-118 ◽  
Author(s):  
M. C. Carrara ◽  
D. Regoli ◽  
W. K. Park
Keyword(s):  
Amino Acids ◽  
Angiotensin Ii ◽  
Unnatural Amino Acids ◽  
Enzymatic Degradation ◽  
Leucine Aminopeptidase ◽  
Receptor Interaction ◽  
Angiotensin I ◽  
Peptide Receptor ◽  
Angiotensin Ii Analogues

Angiotensin II (ATII), angiotensin I (ATI), and Acpc analogues of ATII, 8-Achc-ATII, 8-D-Phe-ATII, and 8-Ala-ATII, were incubated in vitro with carboxypeptidase, chymotrypsin, and leucine-aminopeptidase in order to study the influence of unnatural amino acids (Acpc, Achc, and D-Phe) and of L-Ala on the activity of peptidases.Fragments occurring during the breakdown of peptides were demonstrated by paper chromatography in an ascending system.ATII and ATI are rapidly inactivated by carboxypeptidase and chymotrypsin, while the degradation by leucine-aminopeptidase is slower.Substitution of L-Phe with Acpc, Achc, D-Phe, or L-Ala in position 8 prevents the degradation by carboxypeptidase. Chymotrypsin degrades 3-Acpc-ATII and 5-Acpc-ATII but not 4-Acpc-ATII. The action of leucine-aminopeptidase is not influenced by substituting Acpc to each one of the first five amino acids composing the molecule of angiotensin.The possible implications of these findings for the peptide-receptor interaction is discussed.

ChemInform Abstract: PHOTOAFFINITY LABELING OF THE ANGIOTENSIN II RECEPTOR. PART 1. SYNTHESIS AND BIOLOGICAL ACTIVITIES OF THE LABELING PEPTIDES

1979 ◽  
Vol 10 (8) ◽  
Author(s):  
E. H. F. ESCHER ◽  
THI MAI DUNG NGUYEN THI MAI DUNG NGUYEN ◽  
H. ROBERT ◽  
S. A. ST-PIERRE ◽  
D. C. REGOLI
Keyword(s):  
Angiotensin Ii ◽  
Biological Activities ◽  
Photoaffinity Labeling ◽  
Angiotensin Ii Receptor

Design, synthesis and biological evaluation of cyclic angiotensin II analogues with 3,5 side-Chain bridges

2002 ◽  
Vol 12 (18) ◽  
pp. 2627-2633 ◽  
Author(s):  
Panagiota Roumelioti ◽  
Ludmila Polevaya ◽  
Panagiotis Zoumpoulakis ◽  
Nektarios Giatas ◽  
Ilze Mutule ◽  
...  
Keyword(s):  
Angiotensin Ii ◽  
Biological Evaluation ◽  
Side Chain ◽  
Design Synthesis ◽  
Angiotensin Ii Analogues ◽  
Synthesis And Biological Evaluation

ChemInform Abstract: Synthesis of Angiotensin II Analogues Containing α-Alanine.

ChemInform ◽  
1987 ◽  
Vol 18 (22) ◽  
Author(s):  
R. PARUSZEWSKI ◽  
R. MATUSIAK ◽  
P. JAWORSKI ◽  
S. GUMULKA ◽  
I. WISNIEWSKA
Keyword(s):  
Angiotensin Ii ◽  
Angiotensin Ii Analogues
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