ZALTIDINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C8H10N6S
Molecular Weight	222.27
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=NC=C(N1)C2=CSC(NC(N)=N)=N2

InChI

InChIKey=GIMNAEMRNXUAQP-UHFFFAOYSA-N

InChI=1S/C8H10N6S/c1-4-11-2-5(12-4)6-3-15-8(13-6)14-7(9)10/h2-3H,1H3,(H,11,12)(H4,9,10,13,14)

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Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2878075 | https://www.ncbi.nlm.nih.gov/pubmed/2902681 | https://www.ncbi.nlm.nih.gov/pubmed/2876724

Zaltidine (CP-57,361) is a guanidinothiazolylimidazole compound which is a highly specific H2-receptor antagonist. It potently inhibits gastric acid secretion. Zaltidine appears to be an effective treatment of duodenal ulcer in human studies. However, the incidence of hepatic damage (8%) seems higher than with commonly used H2-receptor antagonists.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Histamine H2 receptor 46 Target ID: CHEMBL1941 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2878075	Antagonist 2849

Conditions

Condition	Modality	Targets	Highest Phase	Product
Duodenal ulcer 49 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2902681 https://www.ncbi.nlm.nih.gov/pubmed/2876724	Primary		Not Provided 511	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Plasma analysis and pharmacokinetics of zaltidine, an H2-antagonist, in cattle after intravenous, intramuscular, subcutaneous, and oral administration.	1996-08	8866466
Zaltidine: an effective but hepatotoxic H2-receptor antagonist.	1988-08	2902681
Bioisosteric prototype design of biaryl imidazolyl and triazolyl competitive histamine H2-receptor antagonists.	1986-11	2878075
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.	1986-10	2876724

Patents

Sample Use Guides

In Vivo Use Guide

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.

Route of Administration: Oral

In Vitro Use Guide

Unknown

Name

Type

Language

(4-(2-METHYLIMIDAZOL-5-YL)-2-THIAZOLYL)QUANIDINE

Preferred Name

English

ZALTIDINE

Official Name

English

zaltidine [INN]

Common Name

English

GUANIDINE, (4-(2-METHYL-1H-IMIDAZOL-5-YL)-2-THIAZOLYL)-

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29702