中文名称: | CGP48369 | ||||
---|---|---|---|---|---|
英文名称: | CGP48369 | ||||
CAS No: | 135689-23-5 | 分子式: | C26H30N6O | 分子量: | 442.56 |
CAS No: | 135689-23-5 | ||||
分子式: | C26H30N6O | ||||
分子量: | 442.56 |
包装规格:
100mg in glass bottle
产品简介:
一种血管紧张素 II 受体 (angiotensin II receptor) 拮抗剂,用于研究抗高血压疾病。
体外研究:
CGP 48369 binds to the ATl receptor (IC50 1.8 nM in vascular smooth musc1e cells, VSMC) and inhibits AII-induced contraction in rabbit aorta (IC50 8.7 nM).
体内研究:
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.
保存条件:
-20℃
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2、以上信息仅做参考交流之用。
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