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]
References
External links
- Saralasin at the U.S. National Library of Medicine Medical Subject Headings (MeSH)
- Olsson M, Annerbrink K, Hedner J, Eriksson E (2004). "Intracerebroventricular administration of the angiotensin II receptor antagonist saralasin reduces respiratory rate and tidal volume variability in freely moving Wistar rats". Psychoneuroendocrinology. 29 (1): 107–12. doi:10.1016/S0306-4530(02)00147-6. PMID 14575733. S2CID 44451942.
- Ip S, Tsang S, Wong T, Che C, Leung P (2003). "Saralasin, a nonspecific angiotensin II receptor antagonist, attenuates oxidative stress and tissue injury in cerulein-induced acute pancreatitis". Pancreas. 26 (3): 224–9. doi:10.1097/00006676-200304000-00003. PMID 12657946. S2CID 28646144.
- Tsang S, Ip S, Wong T, Che C, Leung P (2003). "Differential effects of saralasin and ramiprilat, the inhibitors of renin-angiotensin system, on cerulein-induced acute pancreatitis". Regul Pept. 111 (1–3): 47–53. doi:10.1016/S0167-0115(02)00226-4. PMID 12609748. S2CID 2150707.