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135689-23-5

中文名稱 135689-23-5
英文名稱 CGP 48369
CAS 135689-23-5
分子式 C26H30N6O
分子量 442.56
MOL 文件 135689-23-5.mol
135689-23-5 結(jié)構(gòu)式 135689-23-5 結(jié)構(gòu)式

基本信息

中文別名
化合物 T14942
英文別名
CGP 48369
4(3H)-Pyrimidinone, 2,6-dibutyl-5-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-

物理化學(xué)性質(zhì)

沸點653.2±65.0 °C(Predicted)
密度1.22±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)4.17±0.10(Predicted)

常見問題列表

生物活性
CGP48369 是血管緊張素 II 受體 (angiotensin II receptor) 拮抗劑,用于研究抗高血壓疾病。
體外研究

CGP 48369 binds to the ATl receptor (IC 50 1.8 nM in vascular smooth musc1e cells, VSMC) and inhibits AII-induced contraction in rabbit aorta (IC 50 8.7 nM).

體內(nèi)研究

CGP48369 (10 mg/kg/day p.o.) decreases BP in two-kidney/one-clip renal hypertensive rats for at least 24 h. In arteries with endothelium, contractions induced by AII 3×10 -8 M do not differ in untreated spontaneously hypertensive rats (SHR) and WKY. All evoked significantly smaller contractions in SHR treated with CGP 48369 than in the other treated SHR. Antihypertensive treatment with benazepril or nifedipine, and to a lesser extent with CGP 48369, increases the sensitivity (pD2-va1ue) to intraluminal ACh. In arteries without endothelium, sensitivity to NE is identical in all groups, whereas maximal response in CGP 48369-treated SHR and in nifedipine treated SHR is slightly greater as compared with that in WKY. In SHR, antihypertensive therapy with either benazepril HCl, CGP 48369, valsartan, or nifedipine (each 10 mg/kg/d for 8 weeks) significantly increase endothelium-dependent relaxations evoked by acetylcholine.

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