135689-23-5
| 中文名称 | 135689-23-5 |
|---|---|
| 中文同义词 | 化合物 T14942;化合物 CGP48369 |
| 英文名称 | CGP 48369 |
| 英文同义词 | CGP 48369;4(3H)-Pyrimidinone, 2,6-dibutyl-5-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-;CGP-48369,CGP48369 |
| CAS号 | 135689-23-5 |
| 分子式 | C26H30N6O |
| 分子量 | 442.56 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 135689-23-5.mol |
| 结构式 |  |
135689-23-5 性质
| 沸点 | 653.2±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.22±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 4.17±0.10(Predicted) |
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).
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.