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编 号:F328530
分子式:C42H65N13O10
分子量:912.05
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生物活性:
Saralasin ([Sar1,Ala8] Angiotensin II) is an octapeptide analog of angiotensin II. Saralasin is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension.

体内研究:
Saralasin (intravenous injection, 5-50μg/kg, a single dose) ameliorates the oxidative stress and tissue injury in cerulein-induced pancreatitis.Saralasin (subcutaneous injection, 10 and 30 mg/kg, a single dose) increases serum renin activity (SRA) in normal, conscious rats, without markedly altering blood pressure or heart rate.Animal Model:Cerulein-induced acute pancreatitis rats model
Dosage:5, 10, 20, and 50 μg/kg, a single dose.
Administration:Intravenous injection
Result:Restored the pancreatic morphological characteristics to the control level.Reduced pancreatic injury and suppressed the glutathione depletion induced by cerulean.
Animal Model:Male Sprague-Dawley rats
Dosage:10 and 30 mg/kg, a single dose.
Administration:Subcutaneous injection
Result:Stimulated renin release without altering blood pressure or heart rate at the time of measuring serum renin levels 20 minutes after injection.

体外研究:
Saralasin (1 nM, 48 or 72 h) inhibits cell growth in 3T3 and SV3T3 cells.Saralasin (5 μM, 2h) restores Ito, fast (Fast-Inactivating Transient Outward K+ Current in Mouse Ventricle) and I K, slow (Slow-Inactivating Transient Outward K+ Current in Mouse Ventricl) to control levels in myocytes.Saralasin (0.1-10 nM, 40 min) inhibits binding of FITC-Ang II to rat liver membrane preparation (used as the source of angiotensin receptors) with a Ki value of 0.32 nM for 74% of the binding sites and 2.7 nM for the remaining binding sites.Saralasin (1 μM, perfused rat ovary in vitro) inhibits the ovulation rate versus control and reduces prostaglandin E2 and 6-keto-prostaglandin F1α levels.
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