diltiazem hydrochloride
| Price | $10 |
| Package | 1kg |
| Min. Order: | 1kg |
| Supply Ability: | Ex 20 tons |
| Update Time: | 2022-10-10 |
Product Details
| Product Name: diltiazem hydrochloride | CAS No.: 33286-22-5 |
| EC-No.: 251-443-3 | Min. Order: 1kg |
| Purity: 99% | Supply Ability: Ex 20 tons |
| Release date: 2022/10/10 |
Use of diltiazem hydrochloride
Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist).
| Name | diltiazem hydrochloride |
|---|---|
| Synonym | More Synonyms |
| Description | Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist). |
|---|---|
| Related Catalog | Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel Research Areas >> Cardiovascular Disease |
| In Vitro | 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]. |
| 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[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]. |
| Solvent | In Vitro: H2O : 33.33 mg/mL (73.91 mM; Need ultrasonic) |
| Solubility | 1 mM2.2174 mL11.0870 mL22.1739 mL5 mM0.4435 mL2.2174 mL4.4348 mL10 mM0.2217 mL1.1087 mL2.2174 mL |
| Storage | Powder-20°C3 years 4°C2 yearsIn solvent-80°C6 months -20°C1 month |
| Shipping | Room temperature in continental US; may vary elsewhere |
| SMILES | CN(C)CCN1C2=CC=CC=C2S[C@@H](C3=CC=C(OC)C=C3)[C@@H](OC(C)=O)C1=O.Cl |
| References | [1]. Kraus RL, et al. Molecular mechanism of diltiazem interaction with L-type Ca2+ channels. J Biol Chem. 1998 Oct 16;273(42):27205-12. [2]. van Breemen C, et al. The mechanism of inhibitory action of diltiazem on vascular smooth muscle contractility. J Pharmacol Exp Ther. 1981 Aug;218(2):459-63. [3]. Chiesi M, et al. Stereospecific action of diltiazem on the mitochondrial Na-Ca exchange system and on sarcolemmal Ca-channels. Biochem Pharmacol. 1987 Sep 1;36(17):2735-40. [4]. Freitas F, et al. Cardiac microvascular rarefaction in hyperthyroid rats is reversed by losartan, diltiazem, and propranolol. Fundam Clin Pharmacol. 2015 Feb;29(1):31-40. [5]. Sato M, et al. Hypotensive effects of diltiazem hydrochloride in the normotensive, spontaneously hypertensive and renal hypertensive rats (author's transl). Nihon Yakurigaku Zasshi. 1979 Mar;75(2):99-106. |
| Related Molecules | Neomycin sulfate | Nifedipine | Acetylcholine chloride | Ionomycin | (S)-(-)-Bay K 8644 | Nimodipine | Mibefradil dihydrochloride | Levetiracetam | CDN 1163 | Dantrolene sodium | Thapsigargin | Flufenamic Acid | ABT 639 | Ranolazine dihydrochloride | Cromolyn (sodium) |
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