References of 2-[[1-[2-[[2-[[2-[[2-[[5-(diaminomethylideneamino)-2-[[2-(methylamino)
acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-
hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]-3-(1H-imidazol-5-
yl)propanoyl]pyrrolidine-2-carbonyl]amino]propanoic acid
Title: Saralasin
CAS Registry Number: 34273-10-4
CAS Name: 1-(
N-Methylglycine)-5-L-valine-8-L-alanineangiotensin II
Synonyms: N-[1-[
N-[
N-[
N-[
N-[
N2-(
N-methylglycyl)-L-arginyl]-L-valyl]-L-tyrosyl]-L-valyl]-L-histidyl]-L-prolyl]-L-alanine; 1-sar-8-ala-angiotensin II
Molecular Formula: C42H65N13O10
Molecular Weight: 912.05
Percent Composition: C 55.31%, H 7.18%, N 19.96%, O 17.54%
Literature References: A specific antagonist of angiotensin II. Prepn: Sipos
et al., DE 2127393 corresp to
US 3751404 (1972, 1973 to Norwich Pharmacal). Activity studies: Pals
et al., Circ. Res. 29, 673 (1971); Pals, Fulton,
Arch. Int. Pharmacodyn. Ther. 204, 20 (1973); Solomon, Buckley,
J. Pharm. Sci. 63, 1109 (1974); Streeten
et al., N. Engl. J. Med. 292, 657 (1975). Comprehensive review of the acetate: C. T. Huang
et al., in
Pharmacological and Biochemical Properties of Drug Substances vol. 3, M. E. Goldberg, Ed. (Am. Pharm. Assoc., Washington, DC, 1981) pp 176-225.
Derivative Type: Hydrated acetate
CAS Registry Number: 39698-78-7
Synonyms: Saralasin acetate
Manufacturers' Codes: P-113
Trademarks: Sarenin (Procter & Gamble)
Properties: Described as C42H65N13O10.
xC2H4O2.
xH2O. Fluffy white powder, mp 256°. Sol in water, 5% aq dextrose, 90-95% aq alcohol. LD50 i.v. in male mice: 1171 mg/kg (Huang).
Melting point: mp 256°
Toxicity data: LD50 i.v. in male mice: 1171 mg/kg (Huang)
Therap-Cat: Antihypertensive, diagnostic aid (renin-dependent hypertension).
Keywords: Antihypertensive; Diagnostic Aid.