product name Eprosartan Mesylate
Description: Eprosartan is a nonpeptide angiotensin II receptor antagonist with IC50 of 9.2 and 3.9 nM in rat and human adrenal cortical membranes, respectively. It is used for the treatment of high blood pressure. Eprosartan is sometimes co-formulated with hydrochlorothiazide to treat hypertension.It acts on the renin-angiotensin system to decrease total peripheral resistance in two ways. First, it blocks the binding of angiotensin II to AT1 receptors in vascular smooth muscle, causing vascular dilatation. Second, it inhibits sympathetic norepinephrine production, further reducing blood pressure.
References: Drugs. 2000 Jul;60(1):177-201; Pharmacology. 1997 Nov;55(5):244-51.
520.62
Formula
C23H24N2O4S.CH4O3S
CAS No.
144143-96-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 104 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (7.7 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Eprosartan inhibits [125I]-angiotensin II binding with IC50 1.4 nM to 3.9 nM in human tissues (adrenal cortex, liver, cloned AT1 receptor) and 1.5 nM to 9.2 nM in rat tissues (e.g. mesenteric artery, adrenal cortex, renal glomerulus). Eprosartan (100 nM), but not an AT2 antagonist, completely blocks angiotensin II-induced isotonic fluid absorption in rabbit isolated perfused proximal convoluted tubules. Kinase Assay: Cell Assay: |
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| In Vivo | Eprosartan (3 mg/kg-10 mg/kg, administered by duodenal or gastric catheter) also produces a dose-dependent inhibition of the pressor response to angiotensin II in conscious normotensive rats. Eprosartan (10 mg/kg) dose-dependently reduces blood pressure and antihypertensive activity is maintained for 1.5 hours in renin-dependent hypertensive rats. Eprosartan (60 mg/kg/day, intraperitoneally) is associated with no mortality (0 of 20 rats) after 18 weeks compared with a 100% mortality rate by week 9 among 20 vehicle-treated rats. Eprosartan (10 mg/kg) dose-dependently reduces mean arterial pressure and does not cause reflex tachycardia in dogs. Eprosartan (0.3 mg/kg) inhibits the pressor response induced by electronic stimulation of the spinal cord in the pithed rat. Eprosartan inhibits amino acid-induced glomerular hyperfiltration in rats. Eprosartan (0.3 mg/kg i.v.) inhibits the pressor response induced by spinal cord stimulation in a manner similar to that observed with the peptide antagonist, Sar1, Ile8[angiotensin II] in the pithed rat. Eprosartan is more effective in inhibiting sympathetic nervous system activity compared to other chemically distinct nonpeptide angiotensin II receptor antagonists. |
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| Formulation & Dosage | |
| References | Drugs. 2000 Jul;60(1):177-201; Pharmacology. 1997 Nov;55(5):244-51. |
