产品
编 号:F355158
分子式:C22H26N2O4S
分子量:414.52
产品类型
结构图
CAS No: 42399-41-7
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生物活性:
Diltiazem is an orally active L-type Ca2+ channel blocker. Diltiazem shows antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.
体内研究:
Diltiazem (100 mg/kg; p.o.; for 4 weeks) prevents aortic aneurysm formation in a blood pressure-independent manner.Diltiazem limits aortic aneurysm formation in mice by a blood pressure-independent anti-inflammatory effect on monocytic cells.Diltiazem (2 mg/kg; i.v.) exhibits T1/2 of 61.2 min, CLel of 3.2 mL/min in rats.Animal Model:Male ApoE?/? mice, angiotensin II induced aneurysms
Dosage:100 mg/kg
Administration:Oral administration, in drinking water, for 4 weeks
Result:Srongly reduced the vascular remodeling but also lowered the blood pressure.
Animal Model:Rat (200-250 g)
Dosage:2 mg/kg (Pharmacokinetic Analysis)
Administration:Intravenous injection
Result:T1/2 (61.2 min), CLel (3.2 mL/min)
体外研究:
Diltiazem (200 μM) elicits a use-dependent blockade that proceeded within a relatively small number of pulses.Diltiazem reduces Ca2+ influx by accelerating inactivation during action potentials, and that the use-dependent blockade is due to increases in the number of channels in a sustained closed state.