产品说明书

	同义名 :	HOE 498 diacid;Ramipril diacid;HOE498 diacid, HOE-498 diacid, Ramipril diacid
	CAS号 :	87269-97-4
	货号 :	A586852
	分子式 :	C21H28N2O5
	纯度 :	95%
	分子量 :	388.457
	MDL号 :	MFCD00865787
	存储条件：	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Ramiprilat, the active metabolite of Ramipril, is a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Ramiprilat inhibits ACE with a Ki value of 7 pmol/l. It is both a slow- and tight-binding inhibitor; the mode of inhibition is fully competitive. Binding of ramiprilat to ACE proceeds by a two-step mechanism E + I in equilibrium EI in equilibrium EI in which the inhibitor rapidly binds to enzyme to form an initial enzyme-inhibitor complex, which then undergoes a slow isomerization[1]. The angiotensin-converting enzyme inhibitor ramiprilat (30 or 100 microM) has a protective effect on isolated cardiac myocytes exposed to hypoxia/reoxygenation and that this effect is most likely related to a local action of bradykinin on the cardiac myocyte via the activation of the kinin B2 receptor[2]. An acute infusion of ramiprilat significantly prevents the development of coronary endothelial dysfunction[3]. After an IV bolus of ramiprilat, the only changes in renal-impaired dogs were a 14 and 49% decrease in clearance of the free fraction of ramiprilat and free plasma concentration required to produce 50% of the maximal effect, respectively[4].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.57mL 0.51mL 0.26mL	12.87mL 2.57mL 1.29mL	25.74mL 5.15mL 2.57mL

参考文献

[1]Bünning P. Kinetic properties of the angiotensin converting enzyme inhibitor ramiprilat. J Cardiovasc Pharmacol. 1987;10 Suppl 7:S31-5 [2]Wall TM, Linseman DA, Hartman JC. Ramiprilat attenuates hypoxia/reoxygenation injury to cardiac myocytes via a bradykinin-dependent mechanism. Eur J Pharmacol. 1996 Jun 13;306(1-3):165-74 [3]Martorana PA, Ruetten H, Goebel B, Koehl D, Roegner B, Schoelkens BA, Keil M. Ramiprilat prevents the development of acute coronary endothelial dysfunction in the dog. Basic Res Cardiol. 1999 Aug;94(4):238-45 [4]Lefebvre HP, Jeunesse E, Laroute V, Toutain PL. Pharmacokinetic and pharmacodynamic parameters of ramipril and ramiprilat in healthy dogs and dogs with reduced glomerular filtration rate. J Vet Intern Med. 2006 May-Jun;20(3):499-507