| 产品描述: | Zaltidine(CP-57361) is a H2-receptor antagonist, which has the antisecretory action. IC50 Value: Target: H2 receptor in vitro: in vivo: In eight healthy male volunteers single oral doses of 5 mg, 25 mg and 100 mg produced dose-related inhibition of basal and pentagastrin-stimulated acid output (M.A.O.) with an estimated ID50 of 40 mg for the latter. In eight subjects with duodenal ulceration single 100 mg and 200 mg doses produced 85% and 97% inhibition of M.A.O. at peak (3 h post-dose) and 20% and 23% inhibition at 24 h, respectively; inhibition of basal acid output was 97% at 3 h and 50% at 24 h with both doses. One hundred and thirty-five patients were randomly allocated to 4 weeks' treatment with either 150 mg zaltidine once daily or placebo. Fifty-nine were treated for a full 4 weeks with zaltidine before the trial was stopped. Healing rates after 4 weeks of zaltidine and placebo were 86% and 19%, respectively (p less than 0.001) |
| 靶点: |
Histamine Receptor |
| 参考文献: |
1. Laferla G, Buchanan N, Hearns J, The antisecretory effects of zaltidine, a novel long-acting H2-receptor antagonist, in healthy volunteers and in subjects with a past history of duodenal ulcer. Br J Clin Pharmacol. 1986 Oct;22(4):395-9. 2. Farup PG. Zaltidine: an effective but hepatotoxic H2-receptor antagonist. Scand J Gastroenterol. 1988 Aug;23(6):655-8. |
| 溶解性: |
Soluble in H2O |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
4.499 ml |
22.495 ml |
44.99 ml |
| 5 mM |
0.9 ml |
4.499 ml |
8.998 ml |
| 10 mM |
0.45 ml |
2.25 ml |
4.499 ml |
| 50 mM |
0.09 ml |
0.45 ml |
0.9 ml |
|
| 注意: |
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