Diltiazem hydrochloride is a calcium channel blocker that inhibits the transmembrane influx of extracellular calcium ions. Diltiazem hydrochloride is used in studies related to tumor and cardiovascular diseases. Diltiazem causes a dose-dependent inhibiton of contractions as well as Ca2+ influx stimulated by alpha adrenoceptor activation and high-K+ depolarization. Diltiazem also inhibits the Na-dependent Ca-efflux from heart mitochondria.
Diltiazem improves the cardiac microcirculation and function in an experimental model of hyperthyroidism in rats. Oral administration of diltiazem (100 mg/kg) reduces the blood pressure of SHR.
| Molecular Weight | 450.98 |
| Formula | C22H26N2O4S.HCl |
| CAS Number | 33286-22-5 |
| Solubility (25°C) | DMSO 60 mg/mL Water 30 mg/mL |
| Storage | 4°C, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] D Harrington, et al. Diltiazem hydrochloride
[3] B F McGraw. Diltiazem hydrochloride
[4] B J McAuley, et al. The use of diltiazem hydrochloride in cardiovascular disorders
[5] K Abe, et al. Diltiazem hydrochloride: synthetic and pharmacological studies and development
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