匹莫苯丹鹽酸鹽
| 中文名稱 | 匹莫苯丹鹽酸鹽 |
|---|---|
| 中文同義詞 | 匹莫苯丹鹽酸鹽;鹽酸匹莫苯丹;化合物 T23159 |
| 英文名稱 | PiMobendan (hydrochloride) |
| 英文同義詞 | PiMobendan (hydrochloride);4,5-Dihydro-6-[2-(4-methoxyphenyl)-1H-benzimidazol-5-yl]-5-methyl-3(2H)-pyridazinone monohydrochloride;6-[2-(4-Methoxyphenyl)-1H-1,3-benzodiazol-6-yl]-5-methyl-2,3,4,5-tetrahydropyridazin-3-one hydrochloride |
| CAS號(hào) | 77469-98-8 |
| 分子式 | C19H19ClN4O2 |
| 分子量 | 370.83276 |
| EINECS號(hào) | |
| 相關(guān)類別 | |
| Mol文件 | 77469-98-8.mol |
| 結(jié)構(gòu)式 |  |
匹莫苯丹鹽酸鹽 性質(zhì)
| 熔點(diǎn) | 311°(dec) |
|---|---|
| 儲(chǔ)存條件 | Store at -20°C |
| 溶解度 | 溶于二甲基亞砜 |
| 形態(tài) | 粉末 |
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.
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.
安全信息
| 毒性 | LD50 orally in mice: ~600 mg/kg (Austel, 1982) |
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