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77469-98-8

中文名稱 匹莫苯丹鹽酸鹽
英文名稱 PiMobendan (hydrochloride)
CAS 77469-98-8
分子式 C19H19ClN4O2
分子量 370.833
MOL 文件 77469-98-8.mol
77469-98-8 結(jié)構(gòu)式 77469-98-8 結(jié)構(gòu)式

基本信息

中文別名
鹽酸匹莫苯丹
匹莫苯丹鹽酸鹽
英文別名
PiMobendan (hydrochloride)
4,5-Dihydro-6-[2-(4-methoxyphenyl)-1H-benzimidazol-5-yl]-5-methyl-3(2H)-pyridazinone monohydrochloride

物理化學(xué)性質(zhì)

熔點(diǎn)311°(dec)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)粉末

安全數(shù)據(jù)

毒性LD50 orally in mice: ~600 mg/kg (Austel, 1982)

常見問題列表

生物活性
Pimobendan hydrochloride (UD-CG115 hydrochloride) 是 PDE3 選擇性抑制劑,IC50為 320 nM。
體外研究

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.

體內(nèi)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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