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Tiotidine

Catalog No. T13163   CAS 69014-14-8
Synonyms: ICI 125211

Tiotidine is a selective histamine H2-receptor antagonist (pA2=7.3-7.8 for guinea-pig right atrium).

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Tiotidine Chemical Structure
Tiotidine, CAS 69014-14-8
Pack Size Availability Price/USD Quantity
1 mg 5 days $ 39.00
5 mg 5 days $ 119.00
1 mL * 10 mM (in DMSO) 5 days $ 112.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tiotidine is a selective histamine H2-receptor antagonist (pA2=7.3-7.8 for guinea-pig right atrium).
Targets&IC50 H3 receptor:4.8(pA2), H2 receptor:7.3-7.8 (pA2), H1 receptor:4.5(pA2)
In vitro 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 competitively antagonizes the positive chronotropic action of histamine with an apparent dissociation constant of 30 μM (23-38 μM). . Tiotidine actually behaves as an inverse agonist in U-937 cells, diminishing basal cAMP levels[3].
Synonyms ICI 125211
Molecular Weight 312.42
Formula C10H16N8S2
CAS No. 69014-14-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

TargetMolReferences and Literature

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.

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Keywords

Tiotidine 69014-14-8 Others ICI 125211 ICI-125211 ICI125211 inhibitor inhibit

 

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