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Imidapril HCl

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Chemical Structure| 89396-94-1 同义名 : 咪达普利盐酸盐 ;TA-6366;Imidapril (hydrochloride);Imidapril HCl
CAS号 : 89396-94-1
货号 : A132165
分子式 : C20H28ClN3O6
纯度 : 98%
分子量 : 441.906
MDL号 : MFCD00923828
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(113.15 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(113.15 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 38 mg/mL suspension

生物活性
靶点

  • ACE

    ACE, IC50:2.6 nM
描述 Angiotensin-converting enzyme (ACE) is responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII), which regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS) [4]. Imidapril hydrochloride (imidapril) is a long-acting, non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor, which has been used clinically in the treatment of hypertension, chronic congestive heart failure (CHF), acute myocardial infarction (AMI), and diabetic nephropathy [5]. After oral administration, imidapril is rapidly converted in the liver to its active metabolite imidaprilat. The plasma levels of imidaprilat gradually increase in proportion to the dose, and decline slowly. The time to reach the maximum plasma concentration (Tmax) is 2.0 h for imidapril and 9.3 h for imidaprilat. The elimination half-lives (t1/2) of imidapril and imidaprilat is 1.7 and 14.8 h, respectively [5]. In patients with hypertension, blood pressure was still decreased at 24 h after imidapril administration. The antihypertensive effect of imidapril was dose-dependent [5]. The maximal reduction of blood pressure and plasma ACE was achieved with imidapril, 10 mg once daily, and the additional effect was not prominent with higher doses. When administered to patients with AMI, imidapril improved left ventricular ejection fraction and reduced plasma brain natriuretic peptide (BNP) levels [5]. In patients with mild-to-moderate CHF [New York Heart Association (NYHA) functional class II–III], imidapril increased exercise time and physical working capacity and decreased plasma atrial natriuretic peptide (ANP) and BNP levels in a dose-related manner. In patients with diabetic nephropathy, imidapril decreased urinary albumin excretion [5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.31mL

2.26mL

1.13mL

22.63mL

4.53mL

2.26mL
参考文献

[1]Hosoya K, Ishimitsu T. Protection of the cardiovascular system by imidapril, a versatile angiotensin-converting enzyme inhibitor. Cardiovasc Drug Rev. 2002 Summer;20(2):93-110.

[2]Thoulon F, Woehrlé F, et al. Long-term tolerance of imidapril in the cat. J Vet Cardiol. 2003 May;5(1):29-34.

[3]Yamanaka K, Takehara N, et al. Pharmacokinetic and pharmacodynamic study of imidaprilat, an active metabolite of imidapril, a new angiotensin-converting enzyme inhibitor, in spontaneously hypertensive rats. J Pharm Biomed Anal. 1997 Aug;15(12):1851-9.

[4]Song JC. Clinical pharmacokinetics and selective pharmacodynamics of new angiotensin converting enzyme inhibitors: an update. Clin Pharmacokinet. 2002;41(3):207-24.

[5] Hosoya K, Ishimitsu T. Protection of the cardiovascular system by imidapril, a versatile angiotensin-converting enzyme inhibitor. Cardiovasc Drug Rev. 2002 Summer;20(2):93-110.