Saralasin
Chemical compound / From Wikipedia, the free encyclopedia
Saralasin is a competitive angiotensin II receptor antagonist with partial agonistic activity. The aminopeptide sequence for saralasin differs from angiotensin II at three sites:
- At position 1, sarcosine replaces aspartic acid, thereby increasing the affinity for vascular smooth muscle AT II receptors and making sara resistant to degradation by aminopeptidases.[1]
- At position 5, isoleucine is replaced by valine
- At position 8, phenylalanine is replaced by alanine which leads to a smaller stimulatory effect. Saralasin was used to distinguish renovascular hypertension from essential hypertension before its discontinuation in January 1984 because of many false-positive and false-negative reports.[2]
Quick Facts Names, Identifiers ...
Names | |
---|---|
IUPAC name
(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-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 | |
Other names
Sar-Arg-Val-Tyr-Val-His-Pro-Ala | |
Identifiers | |
3D model (JSmol) |
|
ChEMBL | |
ChemSpider |
|
PubChem CID |
|
UNII | |
CompTox Dashboard (EPA) |
|
| |
| |
Properties | |
C42H65N13O10 | |
Molar mass | 912.05 g/mol |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
|
Close