Diltiazem is an orally active L-type Ca²⁺ channel blocker, with antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris^{[1] [2] [3]} .

L-type Ca²⁺ channel^[1]

Diltiazem (200 μM) in the superfusate, multichannel currents shows a use-dependent decline in amplitude reflecting reductions in the numbers of superpositions of channel openings in isolated guinea pig ventricular myocytes^[1] .
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^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Diltiazem (100 mg/kg; p.o.; for 4 weeks) prevents aortic aneurysm formation in a blood pressure-independent manner^[3] .
Diltiazem limits aortic aneurysm formation in mice by a blood pressure–independent anti-inflammatory effect on monocytic cells^[3] .
Diltiazem (2 mg/kg; i.v.) has t_1/2 of 61.2 min, CL_el of 3.2 mL/min^[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

414.52

C??H??N?O?S

42399-41-7

地尔硫卓

CN(C)CCN1C2=CC=CC=C2S[C@@H](C3=CC=C(OC)C=C3)[C@@H](OC(C)=O)C1=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Yoshinari Niimi, et al. Diltiazem facilitates inactivation of single L-type calcium channels in guinea pig ventricular myocytes. Jpn Heart J. 2003 Nov;44(6):1005-14.

  [2]. S Lin Tang, et l. Structural Basis for Diltiazem Block of a Voltage-Gated Ca2+ Channel. Mol Pharmacol. 2019 Oct; 96(4): 485–492.

  [3]. Anja Mieth , et al. L-type calcium channel inhibitor diltiazem prevents aneurysm formation by blood pressure-independent anti-inflammatory effects. Hypertension. 2013 Dec;62(6):1098-104.

  [4]. S. J. Downing, et al. Diltiazem pharmacokinetics in the rat and relationship between its serum concentration and uterine and cardiovascular effects. Br J Pharmacol. 1987 Aug; 91(4): 735–745.