Bepridil hydrochloride (CERM 1978) is a calcium channel blocker, with antianginal activity. Bepridil hydrochloride also inhibits Na+/Ca2+ exchange (NCX), sodium channels and cardiac sarcolemmal KATP channels. Bepridil hydrochloride acts as a calcium sensitizer. Bepridil hydrochloride (21 mg/kg) reduces heart rate and mean arterial pressure, decreases the mean coronary vascular resistance and increases stroke volume in rats.
| Molecular Weight | 403 |
| Formula | C24H34N2O.HCl |
| CAS Number | 68099-86-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL Water 10 mg/mL |
| Storage | -20°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.
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SNX-482, a peptidyl toxin of the spider Hysterocrates gigas, is a potent, high affinity, selective and voltage-dependent R-type CaV2.3 channel blocker with an IC50 of 30 nM. |
| ω-Conotoxin MVIIC
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| ω-Conotoxin CnVIIA
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