产品说明书
(+)-cis-Diltiazem HCl
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同义名 : | 盐酸地尔硫卓 ;CRD-401;Diltiazem (hydrochloride);(+)-cis-Diltiazem;RG 83606 HCl;Diltiazem HCl;Diltiazem hydrochloride |
| CAS号 : | 33286-22-5 | |
| 货号 : | A198057 | |
| 分子式 : | C22H27ClN2O4S | |
| 纯度 : | 95% | |
| 分子量 : | 450.979 | |
| MDL号 : | MFCD00069252 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
H2O: 30 mg/mL(66.52 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
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| 靶点 |
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| 描述 | Diltiazem hydrochloride, a benzothiazepine derivative, is antagonist of the calcium ion. Diltiazem caused a dose-dependent inhibiton of contractions as well as Ca++ influx stimulated by alpha adrenoceptor activation and high-K+ depolarization. There was a close relationship between diltiazem inhibition of Ca++ influx and inhibition of contraction when either 40 mM K+ or 10(-8) M NE (norepinephrine) was applied, but not when 10(-6) M NE was used. Also, diltiazem produced a noncompetitive inhibition of Ca++-induced contractions of depolarized rabbit aorta[3]. In conscious and anesthetized normotensive rats, intravenous administration of diltiazem (0.1 - 3 mg/kg) produced a dose-related decrease in blood pressure. Similarly, in conscious spontaneously hypertensive rats (SHR), diltiazem dose-dependently decreased the blood pressure and increased the heart rate after intravenous administration (0.03 - 1 mg/kg). Oral administration of diltiazem (100 mg/kg) also reduced the blood pressure of SHR. In addition, the progressive increase in blood pressure in young SHR was significantly suppressed by chronic oral administration of diltiazem (30 mg/kg)[4]. Diltiazem hydrochloride has beneficial effects on I/R (ischemia-reperfusion injury) injury, but this effect is weaker than cilostazol[5]. Diltiazem hydrochloride-loaded microsponges dispersed in rectal gels may be useful to overcome some limitations of conventional local chronic anal fissure therapy[6]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02203630 | Septic Shock ... 展开 >>Sepsis Shock Tachycardia Arrhythmia 收起 << | Phase 4 | Terminated(Slow enrollment; La... 展开 >>ck of support and equipoise) 收起 << | - | United States, Tennessee ... 展开 >> Vanderbilt University Medical Center Nashville, Tennessee, United States, 37232 收起 << |
| NCT02203630 | - | Terminated(Slow enrollment; La... 展开 >>ck of support and equipoise) 收起 << | - | - | |
| NCT00000620 | Atherosclerosis ... 展开 >> Cardiovascular Diseases Hypercholesterolemia Hypertension Diabetes Mellitus, Type 2 Diabetes Mellitus Coronary Disease 收起 << | Phase 3 | Completed | - | United States, Minnesota ... 展开 >> Minneapolis Medical Research Foundation Minneapolis, Minnesota, United States, 55404 United States, New York Columbia University New York, New York, United States, 10027 United States, North Carolina Wake Forest University Winston-Salem, North Carolina, United States, 27106 United States, Ohio Case Western Reserve University Cleveland, Ohio, United States, 44106 United States, Tennessee Veterans Affairs Memphis, Tennessee, United States, 38104 United States, Washington University of Washington Seattle, Washington, United States, 98195 Canada, Ontario McMaster University Hamilton, Ontario, Canada 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.22mL 0.44mL 0.22mL |
11.09mL 2.22mL 1.11mL |
22.17mL 4.43mL 2.22mL |
| 参考文献 |
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