Tiotidine - CAS 69014-14-8
Category: Inhibitor
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Histamine Receptor
Tiotidine is a potent histamine H2 receptor antagonist with negligible activity against H1- and H3- receptors.
Brife Description:
histamine H2 receptor antagonist
≥99% by HPLC
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1.Mechanism of action of H2-antagonists on histamine- or dimaprit-stimulated H2-receptors of spontaneously beating guinea-pig atrium.
Krielaart MJ;Veenstra DM;van Buuren KJ Agents Actions. 1990 Aug;31(1-2):23-35.
Cimetidine, ranitidine and famotidine are antagonists of the histamine H2-receptors on the spontaneously beating right atrium of the guinea pig. When analyzed by the classical Schild method their pA2-values are respectively: 6.3, 6.8 and 7.7 with dimaprit as agonist and 5.8, 6.5 and 7.7 with histamine as agonist. Radioligand-displacement studies with [3H]-tiotidine as radioligand resulted in pKd values for cimetidine, ranitidine and famotidine of 6.3; 6.9 and 8.2 respectively. In dimaprit-stimulated atria all antagonists added at concentrations above their Kd values depressed the maximal increase in frequency. In the presence of histamine this effect was much less pronounced and only visible at concentrations of ranitidine and famotidine around 10.Kd. The rightward shift of the curves as well as the decrease in Emax are reversible but the dissociation constants of the antagonists are small (less than 10(-3) s-1). The spontaneously beating right atrium showed receptor reserve for histamine and virtually no receptor reserve for dimaprit. The results have been interpreted in a model in which H2-antagonists act mainly by competing with the agonist for the histamine receptor site but have in addition a distinct affinity for a secondary site on the receptor.
2.Is [3H]-tiotidine a specific ligand for the H2-receptor?
Batzri S;Harmon JW Pharmacology. 1986;32(5):241-7.
The H2-antagonist tiotidine inhibited the H2-receptor-mediated, histamine-induced increase in cyclic AMP in dispersed mucosal cells from guinea pig stomach (Ki, 4 X 10(-8) M). The radiolabeled [3H]-tiotidine bound specifically and reversibly to the same cells with a half-maximal binding occurring at 5 X 10(-7) M tiotidine. The dissociation of bound [3H]-tiotidine from gastric cells and the Scatchard analysis of the binding binding data suggest the existence of additional binding sites for tiotidine. Eight other antagonists which inhibited the H2-receptor-mediated increase in cyclic AMP also inhibited [3H]-tiotidine binding. However, the potencies of these agents for binding did not agree with their effects on cyclic AMP. The selective H2-agonists impromidine and dimaprit which increased cyclic AMP caused only partial inhibition of [3H]-tiotidine binding. These results demonstrate that [3H]-tiotidine has limited binding to the H2-receptors and as such [3H]-tiotidine is not a suitable ligand for labelling the H2-receptor on gastric mucosal cells.
3.Dose-response curve analysis of gastric secretory responses in the dog and man to impromidine: a new histamine-H2-receptor agonist.
McIsaac RL;Johnston BJ;Flannery MC J Pharmacol Exp Ther. 1983 Apr;225(1):186-90.
The new histamine-H2-receptor agonist, impromidine, was assessed for its effect on gastric acid secretion using a dose-response format. Maximal acid output and ED50 were calculated for infusions of impromidine in the Heidenhain pouch dog (0.05-1.6 x 10(-8) mol/kg/hr) and in man (0.39-6.22 x 10(-8) mol/kg/hr). Analysis of the responses was carried out by nonlinear regression using the logistic function. This allowed the data to be analyzed without making assumptions about the steepness of the curve which in man was almost twice that found in the dog (1.8:1). The ED50 in the dog was 0.26 +/- 0.029 x 10(-8) mol/kg/hr. The control dose-responses could be inhibited in a competitive manner by histamine-H2-receptor antagonists. Analysis of the control curve and three curves in the presence of increasing doses of antagonist was carried out by fitting all the curves simultaneously to calculate an in vivo ID50. In the dog, the antagonist was tiotidine (0.05, 0.1 and 0.2 x 10(-6) mol/kg/hr) and the ID50 was 0.012 +/- 0.002 x 10(-6) mol/kg/hr. In man, cimetidine (1.05, 2.10 and 4.2 x 10(-6) mol/kg/hr) was used to inhibit secretion. The calculated ID50 was 0.63 +/- 0.085 x 10(-6) mol/kg/hr. Comparison of the effect of cimetidine and tiotidine against both impromidine and histamine showed that the ID50 was the same for both stimulants.
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CAS 69014-14-8 Tiotidine

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