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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 of TUVATIDINE

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

Molecular Formula C10H17N9O2S3
Molecular Weight 391.496
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

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

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.
Substance Class Chemical
Record UNII
TWN203TLYT
Record Status Validated (UNII)
Record Version