8372. Saralasin

Nomenclature

CAS number: 34273-10-4
1-(N-Methylglycine)-5-l-valine-8-l-alanineangiotensin II; 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.
C42H65N13O10; mol wt 912.05.
C 55.31%, H 7.18%, N 19.96%, O 17.54%.

Description and 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.

Chemical structure

Derivative

Hydrated acetate.

Nomenclature

CAS number: 39698-78-7
Saralasin acetate; P-113; 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).

Therapeutic Category

Antihypertensive, diagnostic aid (renin-dependent hypertension).

Keywords

Antihypertensive; Diagnostic Aid