Pimobendan (hydrochloride)
Names
[ CAS No. ]:
77469-98-8
[ Name ]:
Pimobendan (hydrochloride)
[Synonym ]:
PIMOBENDAN HYDROCHLORIDE
PiMobendan (hydrochloride)
Biological Activity
[Description]:
Pimobendan hydrochloride is a selective inhibitor of PDE3 with IC50 of 0.32 μM.Target: PDE3Pimobendan exhibits selective inhibition of PDE III isolated from guinea pig cardiac muscle with IC50 of 0.32 uM compared to the inhibition of PDE I and PDE II (IC50s >30 μM). In human atrial cells, 100 μM pimobendan significantly increases the L-type calcium current (ICa(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 ICa(L) at +10 mV by 67.4.%, which is significantly lower than that obtained in human atrial cells Pimobendan shows a beneficial effect 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) also significantly reduces myocardial cellular infiltration, the level of intracardiac tumor necrosis factor (TNF)-α and interleukin (IL)-1β compared with the control group, which shows no effect on myocardial necrosis, heart weight and body weight. Pimobendan suppresses expression of the intracardiac iNOS gene , causing reduction of intracardiac NO production.
[Related Catalog]:
[References]
[Related Small Molecules]
3-Isobutyl-1-methylxanthine
|
rolipram
|
PF-04957325
|
AN-2728
|
GLPG1690
|
BAY-60-7550
|
Icariin
|
Ibudilast
|
PF-8380
|
TAK-063
|
Dipyridamole
|
Cilostazol
|
GSK256066
|
Cialis
|
Pentoxifylline
Chemical & Physical Properties
[ Molecular Formula ]:
C19H19ClN4O2
[ Molecular Weight ]:
370.83300
[ Exact Mass ]:
370.12000
[ PSA ]:
79.37000
[ LogP ]:
3.66500
[ Storage condition ]:
2-8℃