CAS 69014-14-8|Tiotidine
Introduction：Basic information about CAS 69014-14-8|Tiotidine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| 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 | / |
| MSDS | / | Flash Point | 282.5ºC |
Names
| Name | 1-cyano-3-[2-[[2-(diaminomethylideneamino)-1,3-thiazol-4-yl]methylsulfanyl]ethyl]-2-methylguanidine |
|---|---|
| Synonym | More Synonyms |
Tiotidine BiologicalActivity
| 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 | Research Areas >>Cardiovascular DiseaseSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorSignaling Pathways >>GPCR/G Protein >>Histamine Receptor |
| 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 |
| InChIKey | YDDXVAXDYKBWDX-UHFFFAOYSA-N |
| SMILES | CN=C(NC#N)NCCSCc1csc(N=C(N)N)n1 |
Synonyms
| ICI 125,211 |
| TIOTIDINE |
| Tiotidinum |
| Tiotidina |
