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编 号:F165876
分子式:C26H32N2O9S
分子量:548.61
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生物活性:
Diltiazem malate is a potent and orally active L-type calcium channel inhibitor. Diltiazem malate shows antihypertensive and antiarrhythmic effects. Diltiazem malate can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.

体内研究:
Diltiazem malate (100 mg/kg; p.o.; daily for 4 weeks) prevents aortic aneurysm formation in a blood pressure-independent manner.Diltiazem malate (100 mg/kg; p.o.; daily for 6 days) with ATII (1.44 mg/kg; p.o.; daily for 6 days) reduces the ATII-induced vascular inflammation and macrophage accumulation in ApoE?/? mice.Diltiazem malate (2 mg/kg; i.v.) exhibits T1/2 of 61.2 min, CLel of 3.2 mL/min in rats.

体外研究:
Diltiazem malate (200 μM) elicits a use-dependent blockade that proceeded within a relatively small number of pulses.Diltiazem malate 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.
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