Diltiazem Hydrochloride 是一种苯并硫氮卓类钙通道阻滞剂，由于其拮抗钙离子对膜功能的作用而具有血管舒张作用。

Diltiazem Hydrochloride is a benzothiazepine calcium channel blocking agent with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.

Benzothiazepine Ca2+ antagonist diltiazem hydrochloride interacts with transmembrane segments IIIS6 and IVS6 in the α1 subunit of L-type Ca2+ channels[1]. Diltiazem causes a dose-dependent inhibiton of contractions as well as Ca2+ influx stimulated by alpha adrenoceptor activation and high-K+ depolarization. Diltiazem is roughly equally potent in inhibiting contractions induced by high-K+ and a low concentration of norepinephrine (NE)[2]. Diltiazem also inhibits the Na-dependent Ca-efflux from heart mitochondria. Both the (+)-optical isomers of the cis- and trans-forms of diltiazem inhibit Na-Ca exchange activity with comparable potency (IC50 of 10-20 μM)[3].

Diltiazem produces a noncompetitive inhibition of Ca2+-induced contractions of depolarized rabbit aorta. Furthermore, there is a lack of parallelism between the smooth muscle effects of removal of [Ca2+]ex and of addition of diltiazem[2]. Diltiazem improves the cardiac microcirculation and function in an experimental model of hyperthyroidism in rats. The treatment of hyperthyroid rats with losartan diltiazem (4.7±0.7%; P< 0.001) significantly reduces the percentage of fibrosis areas in the left ventricle [4]. In conscious spontaneously hypertensive rats (SHR), diltiazem dose-dependently decreases the blood pressure and increases the heart rate after intravenous administration (0.03--1 mg/kg). Oral administration of diltiazem (100 mg/kg) also reduces the blood pressure of SHR[5].

33286-22-5

C22H27ClN2O4S

450.98

Diltiazem HCl;CRD-401;盐酸地尔硫卓;RG 83606 HCl

H2O:100 mg/mL (221.74 mM)
DMSO:12.4 mg/mL (27.5 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years