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.
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 55 mg/mL|
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