Zaltidine

Modify Date: 2024-01-02 17:35:31

Zaltidine Structure
Zaltidine structure
Common Name Zaltidine
CAS Number 85604-00-8 Molecular Weight 222.27000
Density 1.7g/cm3 Boiling Point 622.9ºC at 760 mmHg
Molecular Formula C8H10N6S Melting Point N/A
MSDS N/A Flash Point 330.5ºC

 Use of Zaltidine


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].

 Names

Name 2-[4-(2-methyl-1H-imidazol-5-yl)-1,3-thiazol-2-yl]guanidine
Synonym More Synonyms

 Zaltidine Biological Activity

Description 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].
Related Catalog
References

[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.

 Chemical & Physical Properties

Density 1.7g/cm3
Boiling Point 622.9ºC at 760 mmHg
Molecular Formula C8H10N6S
Molecular Weight 222.27000
Flash Point 330.5ºC
Exact Mass 222.06900
PSA 134.21000
LogP 2.14710
Index of Refraction 1.844
Storage condition 2-8℃

 Synonyms

Zaltidine hydrochloride [USAN]
Zaltidinum
Zaltidina
Zaltidine
Zaltidine HCl
Zaltidinum [Latin]
Zaltidina [Spanish]
ZALTIDINE HYDROCHLORIDE