Angiotensin receptor is a G protein coupled receptor with angiotensin as ligand, which can trigger various signal cascades after being activated. Eprosartan mesylate (SKF-108566J) is a nonpeptide angiotensin receptor antagonist[3]. In rat and human adrenal cortical membranes, rat mesenteric artery membranes and human liver membranes, Eprosartan Mesylate specifically displaced angiotensin receptor ligand, [125I] angiotensin II (AII), with IC50 of 9.2, 3.9, 1.5 and 1.7 nM, respectively[3]. In rabbit aortic smooth muscle cells, Eprosartan Mesylate caused a concentration-dependent inhibition of AII-induced increases in intracellular Ca2+ levels[3]. In vivo assay, administration of Eprosartan mesylate (3-10 mg/kg) intraduodenally or intragastrically to conscious normotensive rats resulted in a dose-dependent inhibition of the pressor response to AII (250 ng/kg, i.v.). At 10 mg/kg, i.d., significant inhibition of the pressor response to AII was observed for 3 hr[3].
Eprosartan mesylate/依普罗沙坦甲磺酸盐 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Rabbit ventricular myocytes
30 μM
10 minutes
Fully inhibited swelling-induced currents
Cardiovasc Res. 2008 Jan;77(1):73-80.
Bovine aortic endothelial cells
0.02, 0.2, 2, 20, 200 μM
30 minutes
To investigate the effect of Eprosartan on ATII-induced inhibition of insulin binding. Results showed that Eprosartan dose-dependently improved the insulin binding capacity reduced by ATII, with full restoration at 200 μM.
Diabetes Metab J. 2011 Jun;35(3):243-7.
Layer V pyramidal neurons of rat prefrontal cortex
1 µM
5 minutes
Eprosartan reversed the enhancement of NMDA currents by Ang II, indicating the involvement of AT1 receptors.
Int J Mol Sci. 2024 Nov 25;25(23):12644.
Human umbilical vein endothelial cells (HUVEC)
10 µM
7 days
Eprosartan had no effect on cell proliferation
Hypertension. 2009 Dec;54(6):1353-9.
Human coronary artery smooth muscle cells (HCASMC)
10 µM
7 days
Eprosartan had no effect on cell proliferation
Hypertension. 2009 Dec;54(6):1353-9.
Human aortic vascular smooth muscle cells (HA VSMC)
10 µM
7 days
Eprosartan had no effect on cell proliferation
Hypertension. 2009 Dec;54(6):1353-9.
Eprosartan mesylate/依普罗沙坦甲磺酸盐 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
AbPPswe/PS1dE9 (AbPP/PS1/Alzheimer’s disease) and wild-type C57BL/6J mice
Drinking water
0.35 mg/kg/day
Once daily for four weeks
To investigate the effects of Eprosartan mesylate (EM) on hypertension-induced changes in cerebral blood flow and functional connectivity. EM treatment restored systolic blood pressure in hypertensive mice, increased hippocampal cerebral blood flow, improved white matter integrity, and enhanced functional connectivity.
Triple transgenic mouse model of Alzheimer's disease
Drinking water
0.8g/l
Ad libitum for 2 months
To investigate the effect of Eprosartan on intraneuronal Aβ and oligomeric Aβ levels in the 3xTGAD mouse model of AD. Results showed that Eprosartan treatment had no significant effect on intraneuronal Aβ or oligomeric Aβ levels.
Am J Transl Res. 2011 Feb;3(2):197-208
Sprague-Dawley rats
Primary SCG neurons
In vitro culture
10 μM
48 hours
Eprosartan abolished the L-162,313-mediated increase in axonal levels of TH and DBH mRNA and protein.
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