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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.
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| 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 |
| Related PDE Products |
|---|
| MR-L2
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 μM. |
| MMPX
MMPX is a potent PDE1 inhibitor. |
| T-0156
T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. |
| TPN171
TPN171 is a potent, selective and oral bioavailable inhibitor of phosphodiesterase type 5 (PDE5) with an IC50 of 0.62 nM, being developed for the treatment of pulmonary arterial hypertension (PAH). |
| Mesopram
Mesopram (Daxalipram) is an orally active phosphodiesterase (PDE) 4 inhibitor. |
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