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  • Title: Estimation of pKB values for histamine H2-receptor antagonists using an in vitro acid secretion assay.
    Author: Angus JA, Black JW, Stone M.
    Journal: Br J Pharmacol; 1980 Mar; 68(3):413-23. PubMed ID: 6132635.
    Abstract:
    1 Histamine H2-receptor antagonism by burimamide, metiamide and cimetidine was analysed under apparent equilibrium conditions in the lumen-perfused isolated stomach preparation of the mouse. 2 The behaviour of these compounds was not incompatible with simple competitive antagonism but the estimated pKB values (-log KB) were all significantly lower, by about 1 log unit, than reference values reported for guinea-pig atrium or rat uterus. 3 There seems no need to propose that the parietal cell receptors are somehow different from the others; metiamide continually appears in the gastric juice so that a steady-state but not equilibrium can presumably be reached with respect to the bath concentration and this could keep the antagonist concentration artificially low in the region of the receptors.
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