TUVATIDINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C10H17N9O2S3
Molecular Weight	391.496
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN1C(N)=NS(=O)(=O)N=C1NCCSCC2=CSC(NC(N)=N)=N2

InChI

InChIKey=FSWCCDQGXZITPD-UHFFFAOYSA-N

InChI=1S/C10H17N9O2S3/c1-19-8(13)17-24(20,21)18-9(19)14-2-3-22-4-6-5-23-10(15-6)16-7(11)12/h5H,2-4H2,1H3,(H2,13,17)(H,14,18)(H4,11,12,15,16)

HIDE SMILES / InChI

Description
Sources: https://apps.who.int/iris/bitstream/handle/10665/275695/WHO-EMP-RHT-TSN-2018.1-eng.pdf?sequence=1&isAllowed=y | https://www.ncbi.nlm.nih.gov/pubmed/3840559 | https://www.ncbi.nlm.nih.gov/pubmed/3840560

Tuvatidine (HUK 978) is a potent H2-antagonist. HUK 978 was shown to be devoid of activity at the histamine H1-receptor, the muscarinic receptor and the alpha and beta-adrenergic receptors. In both the guinea-pig gastric mucosa preparation and the rat perfused stomach model, HUK 978 was a powerful inhibitor of acid secretion. HUK 978 is a highly specific H2-antagonist and inhibits acid secretion for longer periods than other competitive compounds.

Approval Year

PubMed

Title	Date	PubMed
Anti-secretory activity of the novel H2-antagonist, HUK 978, in rat, guinea-pig and dog.	1985 Nov 4	3840560
In vitro histamine H2-antagonist activity of the novel compound HUK 978.	1985 Nov 4	3840559

Sample Use Guides

In Vivo Use Guide

Dogs: The effect of the continuous intravenous infusion of different doses of HUK 978 (0.02 to 0.06 uM/kg/h). At doses close to the ID50 values, HUK 978 (0.07 uM/kg) gave almost twice the inhibition at 120 min post dose compared to cimetidine.

Route of Administration: Intragastric

In Vitro Use Guide

Tuvatidine (HUK 978) inhibited histamine stimulated adenylate cyclase from guinea-pig gastric fundic mucosa in a dose dependent manner. HUK 978 had no effect on the unstimulated basal activity of adenylate cyclase. Analysis by the method of Schild from six separate experiments gave a mean KB value of 4.8 x 10(-8) M with a slope of 1.03 showing the antagonism to be competitive. Using membranes prepared from guinea-pig cerebral cortex, HUK 978 inhibited 3H-tiotidine binding with a Ki of 2.0 x 10(-8) M.

Name

Type

Language

TUVATIDINE

Official Name

English

tuvatidine [INN]

Common Name

English

(4-(((2-((5-AMINO-4-METHYL-4H-1,24,6-THRIATRIAZIN-3-YL)AMINO)ETHYL)THIO)METHYL)-2-THIAZOLYL)GUANIDINE S'',S''-DIOXIDE

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29702