Name | 1-cyano-3-[2-[[2-(diaminomethylideneamino)-1,3-thiazol-4-yl]methylsulfanyl]ethyl]-2-methylguanidine |
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Synonyms |
ICI 125,211
TIOTIDINE Tiotidinum Tiotidina |
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]. |
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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 |
Density | 1.5g/cm3 |
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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 |