Tiotidine

Modify Date: 2024-01-13 18:28:06

Tiotidine Structure
Tiotidine structure
Common Name Tiotidine
CAS Number 69014-14-8 Molecular Weight 312.41800
Density 1.5g/cm3 Boiling Point 543.6ºC at 760 mmHg
Molecular Formula C10H16N8S2 Melting Point N/A
MSDS N/A Flash Point 282.5ºC

 Use of Tiotidine


Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors[1][2].

 Names

Name 1-cyano-3-[2-[[2-(diaminomethylideneamino)-1,3-thiazol-4-yl]methylsulfanyl]ethyl]-2-methylguanidine
Synonym More Synonyms

 Tiotidine Biological Activity

Description Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors[1][2].
Related Catalog
Target

H2 Receptor:7.3-7.8 (pA2)

H1 receptor:<4.5 (pA2)

H3 Receptor:4.8 (pA2)

In Vitro Tiotidine competitively antagonizes the positive chronotropic action of histamine with an apparent dissociation constant of 30 μM (23-38 μM). Tiotidine abolishes H2-mediated increases in contractile force leaving H2-mediated negative inotropic responses unopposed. The actions of histamine at the A-V node, manifested by lengthening of the P-R interval and A-V block, are attenuated by 2.5 x 10(-7) M Tiotidine[2]. Tiotidine actually behaves as an inverse agonist in U-937 cells, diminishing basal cAMP levels[3].
References

[1]. Barth H, et al. Structural requirements of imidazole compounds to be inhibitors or activators of histaminemethyltransferase: investigation of histamine analogues and H2-receptor antagonists.

[2]. Trzeciakowski JP, et al. The cardiac pharmacology of tiotidine (LCL 125, 211): a new histamine H2-receptor antagonist. J Pharmacol Exp Ther. 1980 Sep;214(3):629-34.

[3]. Monczor F, et al. Tiotidine, a histamine H2 receptor inverse agonist that binds with high affinity to an inactive G-protein-coupled form of the receptor. Experimental support for the cubic ternary complex model. Mol Pharmacol. 2003 Aug;64(2):512-20.

 Chemical & Physical Properties

Density 1.5g/cm3
Boiling Point 543.6ºC at 760 mmHg
Molecular Formula C10H16N8S2
Molecular Weight 312.41800
Flash Point 282.5ºC
Exact Mass 312.09400
PSA 188.54000
LogP 1.98258
Index of Refraction 1.728

 Synonyms

ICI 125,211
TIOTIDINE
Tiotidinum
Tiotidina