中文名 | Pimobendan (hydrochloride) |
英文名 | Pimobendan (hydrochloride) |
别名 | 盐酸匹莫苯丹 匹莫苯丹盐酸盐 化合物 T23159 |
英文别名 | PiMobendan (hydrochloride) Pimobendan (hydrochloride) 4,5-Dihydro-6-[2-(4-methoxyphenyl)-1H-benzimidazol-5-yl]-5-methyl-3(2H)-pyridazinone monohydrochloride |
CAS | 77469-98-8 |
化学式 | C19H19ClN4O2 |
分子量 | 370.83276 |
熔点 | 311°(dec) |
溶解度 | 10毫米DMSO |
存储条件 | -20℃ |
体外研究 | Pimobendan hydrochloride (UD-CG115 hydrochloride) exhibits selective inhibition of PDE III isolated from guinea pig cardiac muscle with IC 50 of 0.32 uM compared to the inhibition of PDE I and PDE II (IC 50 >30 μM). In human atrial cells, 100 μM Pimobendan (UD-CG115) 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 (EC 50 ) of 1.13 μM. In rabbit atrial cells, Pimobendan (UD-CG115) increases ICa(L) at +10 mV by 67.4.%, which is significantly lower than that obtained in human atrial cells. |
体内研究 | Pimobendan (UD-CG115) shows a beneficial effect on survival in the murine model of EMC virus-induced myocarditis. Administration of Pimobendan (UD-CG115) significantly increases the final survival rate from 33.6% (control) to 53.3% (0.1 mg/kg) or 66.7% (1 mg/kg). Pimobendan (UD-CG115) (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 (UD-CG115) suppresses expression of the intracardiac iNOS gene , causing reduction of intracardiac NO production. |
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