Eprosartan|133040-01-4|安捷凯

Background

Angiotensin II, as part of the renin-angiotensin-aldosterone system, facilitates a sympathetic nervous system response mediated by the angiotensin II type 1 (AT₁) receptor, causing vasoconstriction and subsequent increase in blood pressure. It potentiates noradrenaline release from sympathetic nerve terminals at the presynaptic level as well as amplifies the α-adrenoceptor-mediated vasoconstrictor response to endogenous noradrenaline. Angiotensin II receptor blockers (ARBs) are a major class of therapeutics designed to lower blood pressure and to provide cardiovascular protection.^1,2 Eprosartan (mesylate) is a competitive AT₁ receptor antagonist with IC₅₀ values ranging from 1.4 – 3.9 nM and an elimination half-life of five to seven hours.³ Eprosartan is structurally distinct from other noncompetitive ARBs in that it does not contain a biphenyl, tetrazole moiety and blocks angiotensin II receptors on both sympathetic nerve terminals and blood vessels.²

1.Munger, M.A.Use of angiotensin receptor blockers in cardiovascular protection: Current evidence and future directionsPT36(1)22-40(2011) 2.Blankestijn, P.J., and Rupp, H.Clinical profile of eprosartan: A different angiotensin II receptor blockerCardiovasc. Hematol. Agents Med. Chem.6(4)253-257(2008) 3.Burnier, M.Angiotensin II type 1 receptor blockersCirculation103(6)904-912(2001)

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Eprosartan

Eprosartan详情

Background

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