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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, CAS 69014-14-8

Pack Size	Availability	Price/USD
2 mg	5 days	$ 53.00
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 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.

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

References 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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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

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