The AT1 receptor is involved in the classical physiological actions of Ang II: regulation of blood pressure, electrolyte and water balance, thirst, hormone secretion, and renal function. The AT1 receptor belongs to the G protein-coupled receptor (GPCR) superfamily, typically activates phospholipase C (PLC) through the heterotrimeric Gq protein and lacks intrinsic tyrosine kinase activity[1]. Angiotensin II (3-8), human is a less effective agonist at the angiotensin AT1 receptor. Human Angiotensin II (3-8) causes endothelium-dependent renal cortical vasodilatation, in anaesthetized rats. At doses up to 125 pmol/kg, human Angiotensin II (3-8) is without any cardiovascular effects, but with doses of 1.25 and 12.5 nmol/kg there are dose-dependent increases in mean arterial blood pressure and reductions in renal and mesenteric flows and vascular conductances[2]. Angiotensin II-(3-8)-hexapeptide, at the dose of 1 nmol given intracerebroventricularly, only slightly less than angiotensin II (the same dose and route) stimulated exploratory locomotor behaviour in an open field and electromagnetic motimeter. Equimolar doses of angiotensin II-(3-8)-hexapeptide and angiotensin II in improving processes related to learning and memory in rats, the effectiveness is almost identical. So it must be independent of specific angiotensin receptors in brain , which the hexapeptide binds with about 1000 times lower affinity than angiotensin II[3].
Angiotensin II (3-8), human 细胞实验
Cell Line
Concentration
Treated Time
Description
References
rat aortic rings
1-100 nM
Compare the contractile effects of AII, AIII, and AIV, finding that all three caused concentration-dependent contractions with similar maximal responses. AIII was approximately 4 times less potent than AII, and AIV was about 1000 times less active than AII.
Br J Pharmacol. 1995 Dec;116(7):2963-70
Rat isolated right atria
0.1-100 nM
All elicited concentration-dependent increases in frequency with maximal response of 34.3±0.4 beats/min
Br J Pharmacol. 1996 Aug;118(7):1653-8
Angiotensin II (3-8), human 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Long Evans rats
Conscious rats
Intravenous injection
0.125, 1.25, 12.5 nmol/kg
Single injection, separated by at least 20 minutes
To assess the regional haemodynamic effects of AII(3-8) in conscious rats. Results showed that AII(3-8) caused dose-dependent increases in mean arterial blood pressure and reductions in renal and mesenteric flows and vascular conductances, which were abolished by losartan.
Pure formKeep in dark place, inert atmosphere, store in freezer, under -20°C
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Angiotensin II (3-8), human | Angiotensin Receptor | AmBeed-信号通路专用抑制剂
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