Cilazapril Monohydrate 是一种血管紧张素转化酶抑制剂,能够作用于高血压和充血性心力衰竭的研究。
产品描述
Cilazapril Monohydrate is an angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and congestive heart failure.
体外活性
BML-190 has 50-fold selectivity for CB2 receptors over CB1 receptors. In HEK-293 cells stably expressing the human CB2 receptor, BML-190 potentiates the forskolin-stimulated accumulation of cAMP. BML-190 reduces the basal levels of inositol phosphate production in cells expressing the CB2 receptor. 10 μM of BML-190 decreases inositol phosphates accumulation by 38%. [1] BML-190 is an aminoalkylindole. BML-190 is found to yield at least 15 metabolic products. [2] BML-190 diminishes LPS-induced NO and IL-6 production in a concentration-dependent manner. BML-190 also inhibits LPS-induced PGE2 production and COX-2 induction. [3]
体内活性
Cilazapril (1 mg/kg, daily) tends to decrease and the higher dose (10 mg/kg, daily) significantly decreases systolic blood pressure (SBP) in subtotal nephrectomized rats. Cilazapril attenuates the further development of protein uria in a dose-dependent manner in subtotal nephrectomized rats. Cilazapril attenuates the increase in plasma fibrinogen concentration and serum albumin concentration in a dose-dependent manner. Cilazapril reduces serum MCP-1 concentration in the nephrectomized rats. Cilazapril decreases hepatic fibrinogen synthesis through the alleviation of the local inflammatory process and the improvement of hypoalbuminemia. [1] Cilazapril normalizes systolic arterial pressure to 121 mm Hg (SD) in the treated SHR-SP rats. Cilazapril decreases systolic arterial pressure to a nearly normal level and prevents hypertensive retinal vascular changes, probably by improving endothelial function. [2] Cilazapril results in a marked decrease in the Kd of the renal arginine vasopressin (AVP) receptor and an increase in the plasma AVP level in the spontaneously hypertensive rat. [3] Cilazapril exerts a rapid, complete, and persistent antihypertensive effect in the spontaneously hypertensive rats (SHR) in vivo but has no effect on SAP in the normotensive Sprague-Dawley rat. Cilazapril treatment depresses heart performance (28-35%) in SHR but has no effect in the Sprague-Dawley rats. [4] Cilazapril decreases blood pressure to control values and reduces HW:BW in hyperthyroid rats. [5]
Cas No.
92077-78-6
分子式
C22H33N3O6
分子量
435.521
别名
西拉普利水合物;Justor;Ro 31-2848 monohydrate;西拉普利
储存和溶解度
Ethanol:81 mg/mL (186 mM)
H2O:<1 mgml
DMSO:81 mg/mL (186 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years