863406-85-3
中文名稱
ZONIPORIDE HYDROCHLORIDE HYDRATE
英文名稱
Zoniporide hydrochloride hydrate
CAS
863406-85-3
分子式
C17H19ClN6O2
分子量
374.83
MOL 文件
863406-85-3.mol
863406-85-3 結(jié)構(gòu)式
常見問題列表
生物活性
Zoniporide (CP-597396) hydrochloride hydrate 是 1 型鈉氫交換劑 (NHE-1) 的有效和選擇性抑制劑。Zoniporide hydrochloride hydrate 抑制人 NHE-1 (IC50=14 nM)，與其他 NHE 亞型相比具有大于 150 倍的選擇性，并有效抑制離體 NHE-1 依賴性的人血小板溶脹 (IC50=59 nM)。靶點(diǎn)
IC50: 14 nM (NHE-1)
體內(nèi)研究
Zoniporide hydrochloride hydrate (0.25-4 mg/kg; i.v.; every hour for 2 hours) elicits a dose-dependent reduction in infarct size (ED
50
=0.45 mg/kg/h) in open chest anesthetized rabbits.
Zoniporide exhibits moderate plasma protein binding, has a t
1/2
of 1.5 hours in monkeys, and has one major active metabolite.
Zoniporide hydrochloride hydrate treatment shows the AUC
0-∞
and t
1/2
are 0.07 μg h/mL and 0.5 hours, respectively.
| Animal Model: | Rabbit |
| Dosage: | 0.25, 1, 4 mg/kg |
| Administration: | Every hour for 2 hours; intravenous injection |
| Result: | Elicited a significant dose-dependent reduction in infarct size in the anesthetized rabbit. The ED 50 was 0.45 mg/kg/h. |
| Animal Model: | Rat |
| Dosage: | 1 mg/kg |
| Administration: | Intravenous injection(Pharmacokinetic Analysis) |
| Result: | The AUC 0-∞ and t 1/2 were 0.07 μg h/mL and 0.5 hours, respectively. |