Pimobendan (Vetmedin)

Information	Pimobendan (Vetmedin) is a selective inhibitor of phosphodiesterase III (PDE III) with an IC50 of 0.32 μM.
Targets	Phosphodiesterase III
IC50	0.32 μM ^[1]
In vitro	Pimobendan exhibits selective inhibition of PDE III isolated from guinea pig cardiac muscle with an IC50 of 0.32 uM compared to the inhibition of PDE I and PDE II (IC50s >30 μM). ^[1] Pimobendan inhibits the activity of cAMP-PDE III with an IC50 of 2.4 μM, and exerts concentration-dependent positive inotropic effects in isolated guinea-pig papillary muscles with potency (EC50) of 6.0 μM in part due to selective cardiac PDE III inhibition. ^[2] In human atrial cells, 100 μM pimobendan significantly increases the L-type calcium current (I_Ca(L)) (evoked by depolarization to +10 mV from a holding potential of -40 mV) by 250.4% with the half-maximal stimulation (EC50) of 1.13 μM. In rabbit atrial cells, Pimobendan increases I_Ca(L) at +10 mV by 67.4.%, which is significantly lower than that obtained in human atrial cells ^[3]
In vivo	Pimobendan exerts beneficial effects on survival in the murine model of EMC virus-induced myocarditis. Administration of Pimobendan significantly increases the final survival rate from 33.6% (control) to 53.3% (0.1 mg/kg) or 66.7% (1 mg/kg). Pimobendan (1 mg/kg) significantly reduces the myocardial cellular infiltration, the level of intracardiac tumor necrosis factor (TNF)-α and interleukin (IL)-1β compared with control group, which has no effect on the myocardial nerosis, heart weight and body weight. Pimobendan suppresses the intracardiac iNOS gene expression, causing to the reduction of intracardiac NO production. ^[4]
Clinical Trials
Features

Information

Pimobendan (Vetmedin) is a selective inhibitor of phosphodiesterase III (PDE III) with an IC50 of 0.32 μM.

Targets

Phosphodiesterase III

IC50

0.32 μM ^[1]

In vitro

Pimobendan exhibits selective inhibition of PDE III isolated from guinea pig cardiac muscle with an IC50 of 0.32 uM compared to the inhibition of PDE I and PDE II (IC50s >30 μM). ^[1] Pimobendan inhibits the activity of cAMP-PDE III with an IC50 of 2.4 μM, and exerts concentration-dependent positive inotropic effects in isolated guinea-pig papillary muscles with potency (EC50) of 6.0 μM in part due to selective cardiac PDE III inhibition. ^[2] In human atrial cells, 100 μM pimobendan significantly increases the L-type calcium current (I_Ca(L)) (evoked by depolarization to +10 mV from a holding potential of -40 mV) by 250.4% with the half-maximal stimulation (EC50) of 1.13 μM. In rabbit atrial cells, Pimobendan increases I_Ca(L) at +10 mV by 67.4.%, which is significantly lower than that obtained in human atrial cells ^[3]

In vivo

Pimobendan exerts beneficial effects on survival in the murine model of EMC virus-induced myocarditis. Administration of Pimobendan significantly increases the final survival rate from 33.6% (control) to 53.3% (0.1 mg/kg) or 66.7% (1 mg/kg). Pimobendan (1 mg/kg) significantly reduces the myocardial cellular infiltration, the level of intracardiac tumor necrosis factor (TNF)-α and interleukin (IL)-1β compared with control group, which has no effect on the myocardial nerosis, heart weight and body weight. Pimobendan suppresses the intracardiac iNOS gene expression, causing to the reduction of intracardiac NO production. ^[4]

Clinical Trials

Features

Phosphodiesterase isoenzyme inhibition	The isoenzymes PDE I, PDE II and PDE III are isolated from left ventricular guinea pig muscle. For determination of enzyme inhibition, Pimobendan is preincubated for 5 minutes with the PDE in a buffer containing 40 mM Tris HCl, 50 mM MgCl₂, and 10 mM EGTA (PH 8.0). The reaction is initiated at 37 ℃ by adding 0.3 μM [³H]cAMP (or 2.5 μM [³H]cGMP in the case of PDE II). The concentration of PDE is such that maximally 10% of the substrate is hydrolyzed during the reaction, which is stopped after 20 minutes by briefly heating to 90 ℃. The reaction product [³H]AMP is split to [³H]adenosine by a phosphatase of the venom of the king cobra. [³H]adenosine is separated from unhydrolyzed [³H]cAMP by chromatography and quantified in a scintillation couter. The concentration that produces 50% inhibition of hydrolysis (IC50) is determined from concentration-response curves.

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

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 (WM):	334.37
Formula:	C₁₉H₁₈N₄O₂
CAS No.:	74150-27-9
Synonyms:	Acardi, pimobendane

Molecular Weight (WM):

334.37

Formula:

C₁₉H₁₈N₄O₂

CAS No.:

74150-27-9

Synonyms:

Acardi, pimobendane

Dissolve in (25°C):	DMSO ≥67mg/mL
	Water <1mg/mL
	Ethanol ≥5mg/mL
Storage:	2 years-20°CPowder
	1 week-4°Cin DMSO
	1 month-80°in DMSO

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Biological Activity

Protocol (Only for Reference)

Kinase Assay: [1]

Animal Study:[4]

References

Chemical Information

Quality Control & MSDS

Research Area

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Kinase Assay: ^[1]

Animal Study:^[4]

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