Biomaterial Database

Soluble pepstatins: a new approach to blockade in vivo of the renin-angiotensin system. 1978

G Evin, and J Gardes, and C Kreft, and B Castro, and P Corvol, and J Menard

1. Synthesis of several pepstatin A derivatives was performed with the aim of increasing water solubility without altering the capacity to inhibit the renin-angiotensinogen reaction. 2. Pepstatinyl-arginine-O-methyl ester was studied in vitro and in vivo and compared with pepstatin A and with the arginine salt of pepstatin A. 3. This compound inhibited in vitro the reaction between purified hog renin and the synthetic renin N-acetyl-tetradecapeptide or the natural rat renin substrate. The inhibitory constant was of the same order of magnitude as that of pepstatin A. 4. In renal hypertensive rats, the bolus injection of pepstatinyl-arginine-O-methyl-ester or of the arginine salt of pepstatin decreased blood pressure to the same extent as a bolus injection of Sar1, Ala8-angiotensin II.

UI	MeSH Term	Description	Entries
D006978	Hypertension, Renovascular	Hypertension due to RENAL ARTERY OBSTRUCTION or compression.	Hypertension, Goldblatt,Goldblatt Syndrome,Goldblatt Hypertension,Renovascular Hypertension,Syndrome, Goldblatt
D008297	Male		Males
D009842	Oligopeptides	Peptides composed of between two and twelve amino acids.	Oligopeptide
D010436	Pepstatins	N-acylated oligopeptides isolated from culture filtrates of Actinomycetes, which act specifically to inhibit acid proteases such as pepsin and renin.
D012083	Renin	A highly specific (Leu-Leu) endopeptidase that generates ANGIOTENSIN I from its precursor ANGIOTENSINOGEN, leading to a cascade of reactions which elevate BLOOD PRESSURE and increase sodium retention by the kidney in the RENIN-ANGIOTENSIN SYSTEM. The enzyme was formerly listed as EC 3.4.99.19.	Angiotensin-Forming Enzyme,Angiotensinogenase,Big Renin,Cryorenin,Inactive Renin,Pre-Prorenin,Preprorenin,Prorenin,Angiotensin Forming Enzyme,Pre Prorenin,Renin, Big,Renin, Inactive
D004195	Disease Models, Animal	Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	Animal Disease Model,Animal Disease Models,Disease Model, Animal
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D012504	Saralasin	An octapeptide analog of angiotensin II (bovine) with amino acids 1 and 8 replaced with sarcosine and alanine, respectively. It is a highly specific competitive inhibitor of angiotensin II that is used in the diagnosis of HYPERTENSION.	1-Sar-8-Ala Angiotensin II,1-Sarcosine-8-Alanine Angiotensin II,(Sar(1),Ala(8))ANGII,(Sar1,Val5,Ala8)Angiotensin II,Angiotensin II, Sar(1)-Ala(8)-,Angiotensin II, Sarcosyl(1)-Alanine(8)-,Sar-Arg-Val-Tyr-Val-His-Pro-Ala,Saralasin Acetate,Saralasin Acetate, Anhydrous,Saralasin Acetate, Hydrated,1 Sar 8 Ala Angiotensin II,1 Sarcosine 8 Alanine Angiotensin II,Angiotensin II, 1-Sar-8-Ala,Angiotensin II, 1-Sarcosine-8-Alanine,Anhydrous Saralasin Acetate,Hydrated Saralasin Acetate
D012995	Solubility	The ability of a substance to be dissolved, i.e. to form a solution with another substance. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)	Solubilities
D051381	Rats	The common name for the genus Rattus.	Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus