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Tiotidine is a selective histamine H2-receptor antagonist (pA2=7.3-7.8 for guinea-pig right atrium).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | 50 € | 5 days | |
5 mg | 113 € | 5 days | |
1 mL x 10 mM (in DMSO) | 106 € | 5 days |
Description | Tiotidine is a selective histamine H2-receptor antagonist (pA2=7.3-7.8 for guinea-pig right atrium). |
Targets&IC50 | H2 receptor:7.3-7.8 (pA2), H3 receptor:4.8(pA2), H1 receptor:4.5(pA2) |
In vitro | Tiotidine effectively neutralizes the increase in contractile force facilitated by H2, leaving the negative inotropic responses by H2 unchallenged. It also mitigates the effects of histamine on the A-V node, which include lengthening of the P-R interval and A-V block, at a concentration of 2.5 x 10(-7) M. Furthermore, tiotidine acts as a competitive antagonist against the positive chronotropic effects of histamine, presenting an apparent dissociation constant of 30 μM (23-38 μM). Additionally, tiotidine displays inverse agonist activity in U-937 cells by reducing basal cAMP levels. |
Alias | ICI 125211 |
Molecular Weight | 312.42 |
Formula | C10H16N8S2 |
Cas No. | 69014-14-8 |
Relative Density. | 1.50 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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