Pimobendan (Vetmedin) is a Ca (2+) sensitizer with an IC50 of 26 uM and a selective phosphodiesterase III inhibitor with an IC50 of <1 uM. The inhibitory effects of pimobendan on catecholamine secretion and synthesis in cultured bovine adrenal medullary cells. Pimobendan decreased the catecholamine secretion (IC (50)=29.5 uM) elicited by carbachol, an agonist at nicotinic acetylcholine receptors, but not that elicited by veratridine, an activator of voltage-dependent Na (+) channels, or by high K (+), an activator of voltage-dependent Ca (2+) channels. Pimobendan also inhibited carbachol-induced influx of Na (+) (IC (50)=25.9 uM) and Ca (2+) (IC (50)=26.0 uM), but not veratridine-induced Na (+) influx or high K (+)-induced Ca (2+) influx.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male DBA/2 mice of viral myocarditis |
| Formulation | Prepared as an oral suspension in 0.25% methylcellulose solution, in concentrations of 120 μg/mL and 12 μg/mL |
| Dosages | 0.1 or 1 mg/kg |
| Administration | Orally once daily |
| Molecular Weight | 334.37 |
| Formula | C19H18N4O2 |
| CAS Number | 74150-27-9 |
| Solubility (25°C) | DMSO 55 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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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