Disease relevance of Imidaprilat

• RESULTS: Imidaprilat and ramiprilat enhanced BK-induced hypotension comparably, and this effect was inhibited by Nomega-nitro-L-arginin-methylester (L-NAME, a nitric oxide synthetase inhibitor) [1].
• RESULTS: Plasma imidapril concentrations after single and, although less pronounced, after repeated dosing were higher in the liver disease patients, whereas imidaprilat concentrations were lower [2].
• Moreover, to examine the effect of imidaprilat on *OH formation by ischemia/reperfusion of the myocardium, the heart was subjected to myocardial ischemia for 15 min by occlusion of the left anterior descending coronary artery [3].

High impact information on Imidaprilat

• Although imidapril and spirapril have no effect on digoxin pharmacokinetics, the area under the concentration-time curve of imidapril and the peak plasma concentration of the active metabolite imidaprilat are decreased when imidapril is given together with digoxin [4].
• The effect of Ang I was attenuated by imidaprilat, confirming that it arose from conversion to Ang II [5].
• When either imidaprilat or cilazaprilat of 3 microg/kg/min was infused into the bypass tube for 10 min after reduction of coronary blood flow due to partial occlusion of the bypass tube, coronary blood flow increased from 31 +/- 1 to either 45 +/- 5 or 43 +/- 4 ml/100 g/min despite no changes in coronary perfusion pressure (43 +/- 2 mmHg) [6].
• The dialyzability of imidaprilat, an active metabolite of the angiotensin-converting enzyme (ACE) inhibitor imidapril, was determined and compared with those of enalaprilat and quinaprilat in hypertensive patients on chronic hemodialysis [7].
• METHODS: Cmax, tmax, t1/2 and AUC of imidapril and imidaprilat were obtained [8].

Chemical compound and disease context of Imidaprilat

• Comparison of the effect of imidaprilat and ramiprilat on broncho-constriction and hypotension induced by bradykinin in guinea pigs [1].

Biological context of Imidaprilat

• AUC of the active moiety imidaprilat averaged 211 (101 s.d.) ng ml(-1) h after the first dose and 240 (55 s.d.) ng ml(-1) h at the steady state investigation [8].
• Plasma concentration of imidaprilat, systolic blood pressure (SBP), and plasma ACE activity were determined periodically [9].
• In conscious deoxycorticosterone acetate (DOCA) salt-hypertensive dogs, the angiotensin-converting enzyme (ACE) inhibitors captopril and imidaprilat significantly decreased mean arterial pressure (MAP) and significantly increased urine flow rate, effective renal plasma flow (ERPF), glomerular filtration rate, and urinary sodium excretion [10].

Anatomical context of Imidaprilat

• Protective effect of imidaprilat, an angiotensin-converting enzyme inhibitor on *OH generation in rat myocardium [3].

Associations of Imidaprilat with other chemical compounds

• Pharmacokinetic and pharmacodynamic study of imidaprilat, an active metabolite of imidapril, a new angiotensin-converting enzyme inhibitor, in spontaneously hypertensive rats [9].
• Effects of angiotensin-converting enzyme (ACE) inhibitors, enalaprilat and imidaprilat, on bradykinin (BK) metabolizing enzymes, aminopeptidase P (APP), neutral endopeptidase (NEP) and carboxypeptidase N (CPN), were examined [11].
• We examined the effect of non-SH-containing angiotensin converting enzyme (ACE) inhibitor imidaprilat on hydroxyl radical (.OH) generation using microdialysis [12].

Gene context of Imidaprilat

• Consistently, sympatho-facilitation by Ang I, which could be abolished by the angiotensin converting enzyme (ACE) inhibitor imidaprilat, was apparently greater than that of Ang II in SHR, despite no difference in WKY [13].
• Either imidaprilat or cilazaprilat increased CBF, FS, and LER with increases in cardiac bradykinin and NO levels [14].
• After incubating with the various plasma samples, imidapril was mainly metabolized to the pharmacologically active metabolite, 6366 A (M1, CAS 89371-44-8), in rat plasma; on the other hand, the ester bond of imidapril was not hydrolyzed in dog, monkey, and human plasma [15].

Analytical, diagnostic and therapeutic context of Imidaprilat

• A radioimmunoassay (RIA) was investigated for the determination of imidapril and its active metabolite, imidaprilat, in human plasma and urine [16].
• The antihypertensive action in subcutaneous infusion of imidapril was as potent as that in oral administration at the same dose, although the maximum plasma concentration of imidaprilat in subcutaneous infusion was one-eightieth times of that in oral administration [9].

References