ZONIPORIDE DIHYDROCHLORIDE
| 中文名稱 | ZONIPORIDE DIHYDROCHLORIDE |
|---|---|
| 中文同義詞 | 化合物ZONIPORIDE |
| 英文名稱 | ZONIPORIDE DIHYDROCHLORIDE |
| 英文同義詞 | [1-(QUINOLIN-5-YL)-5-CYCLOPROPYL-1H-PYRAZOLE-4-CARBONYL]GUANIDINE DIHYDROCHLORIDE;ZONIPORIDE DIHYDROCHLORIDE;[1-(quinolin-5-yl)-5-cyclopropyl-1H-pyrazole-4-carbonyl]guanidine hydrochloride;5-cyclopropyl-N-(diaminomethylidene)-1-quinolin-5-ylpyrazole-4-carboxamide:hydrochloride;Zoniporide dihydroch |
| CAS號(hào) | 241800-97-5 |
| 分子式 | C17H17ClN6O |
| 分子量 | 356.81 |
| EINECS號(hào) | |
| 相關(guān)類別 | |
| Mol文件 | 241800-97-5.mol |
| 結(jié)構(gòu)式 |  |
ZONIPORIDE DIHYDROCHLORIDE 性質(zhì)
| 儲(chǔ)存條件 | Desiccate at -20°C |
|---|---|
| 溶解度 | 乙醇中≤1mg/ml；DMSO中10mg/ml；二甲基甲酰胺中10mg/ml |
| 形態(tài) | 結(jié)晶固體 |
| 穩(wěn)定性 | 吸濕性 |
Zoniporide (CP-597396) hydrochloride 是 1 型鈉氫交換劑 (NHE-1) 的有效和選擇性抑制劑。Zoniporide hydrochloride 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)。
IC50: 14 nM (NHE-1)
Zoniporide (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 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. |