Zaltidine
(Synonyms: 唑替丁,CP-57361) 目录号 : GC37959Zaltidine(CP-57361)是H2受体拮抗剂,有抗分泌活性。
Cas No.:85604-00-8
Sample solution is provided at 25 µL, 10mM.
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Zaltidine(CP-57361) is a H2-receptor antagonist, which has the antisecretory action.IC50 Value: Target: H2 receptorin 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 [1]. 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) [2].
[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.
Cas No. | 85604-00-8 | SDF | |
别名 | 唑替丁,CP-57361 | ||
Canonical SMILES | NC(NC1=NC(C2=CN=C(C)N2)=CS1)=N | ||
分子式 | C8H10N6S | 分子量 | 222.27 |
溶解度 | Water: 7.69 mg/mL (34.60 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 4.499 mL | 22.4952 mL | 44.9903 mL |
5 mM | 0.8998 mL | 4.499 mL | 8.9981 mL |
10 mM | 0.4499 mL | 2.2495 mL | 4.499 mL |
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Zaltidine: an effective but hepatotoxic H2-receptor antagonist
Scand J Gastroenterol 1988 Aug;23(6):655-8.PMID:2902681DOI:10.3109/00365528809093927.
Zaltidine is a new H2-receptor antagonist. This study compares the safety and efficacy of Zaltidine with those of placebo in the short-term treatment of duodenal ulcer. 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). Five patients in the Zaltidine group had increased serum aminotransferase levels at the final (4-week) visit. The values normalized when treatment was stopped. Liver biopsy specimens provide strong evidence of drug-induced injury. Hepatic damage was associated with plasma levels of Zaltidine in the upper half of the observed range. Zaltidine appears to be an effective treatment of duodenal ulcer. However, the incidence of hepatic damage (8%) seems higher than with commonly used H2-receptor antagonists.
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.PMID:2876724DOI:10.1111/j.1365-2125.1986.tb02908.x.
The potency and duration of the antisecretory action of Zaltidine, a novel H2-receptor antagonist, have been examined in healthy volunteers and in patients with previous duodenal ulceration. 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. The long duration of action of Zaltidine is ascribed to its relatively slow elimination from the plasma.