Diltiazem hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种突触后肌肉松弛剂，可抑制肌浆网储存的 Ca2+ 离子释放；拮抗兰尼碱受体。

A postsynaptic muscle relaxant that inhibits Ca2+ ions release from sarcoplasmic reticulum stores; antagonizes ryanodine receptors; can prevent cell death in neural progenitor cells derived from Wolfram syndrome iPS cells.Hypertension Approved(In Vitro):Benzothiazepine Ca2+ antagonist diltiazem hydrochloride interacts with transmembrane segments IIIS6 and IVS6 in the α1 subunit of L-type Ca2+ channels. 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). 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). (In Vivo):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. 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 . 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.

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CRD-401

GPCR/G Protein

Calcium Channel

CalciumChannel

Cardiovascular Disease

Hypertension

33286-22-5

450.9788

C22H27ClN2O4S

>98% (HPLC)

10 mM in DMSO

CC(=O)O[C@@H]1[C@@H](SC2=CC=CC=C2N(C1=O)CCN(C)C)C3=CC=C(C=C3)OC.Cl

1,5-Benzothiazepin-4(5H)-one, 3-(acetyloxy)-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-, hydrochloride (1:1), (2S,3S)-

(-20℃)

With Ice Pack

≥ 2 years