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.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Black J. W., Duncan W. A., Durant C. J., Ganellin C. R., Parsons E. M. Definition and antagonism of histamine H 2 -receptors. Nature. 1972 Apr 21;236(5347):385–390. doi: 10.1038/236385a0. [DOI] [PubMed] [Google Scholar]
- Bunce K. T., Parsons M. E. A quantitative study of metiamide, a histamine H2-antagonist, on the isolated whole rat stomach. J Physiol. 1976 Jun;258(2):453–465. doi: 10.1113/jphysiol.1976.sp011430. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Clark A. J. The antagonism of acetyl choline by atropine. J Physiol. 1926 Aug 6;61(4):547–556. doi: 10.1113/jphysiol.1926.sp002315. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Furchgott R. F. The pharmacological differentiation of adrenergic receptors. Ann N Y Acad Sci. 1967 Feb 10;139(3):553–570. doi: 10.1111/j.1749-6632.1967.tb41229.x. [DOI] [PubMed] [Google Scholar]
- Parsons M. E. Studies on gastric acid secretion using an isolated whole mammalian stomach in vitro. J Physiol. 1975 May;247(1):35P–36P. [PubMed] [Google Scholar]
- Scholes P., Cooper A., Jones D., Major J., Walters M., Wilde C. Characterization of an adenylate cyclase system sensitive to histamine H2-receptor excitation in cells from dog gastric mucosa. Agents Actions. 1976 Nov;6(6):677–682. doi: 10.1007/BF02026087. [DOI] [PubMed] [Google Scholar]
- Stone M., Angus J. A. Developments of computer-based estimation of pA2 values and associated analysis. J Pharmacol Exp Ther. 1978 Dec;207(3):705–718. [PubMed] [Google Scholar]
- Wan B. Y. Metiamide and stimulated acid secretion from the isolated non-distended and distended mouse stomach. J Physiol. 1977 Apr;266(2):327–346. doi: 10.1113/jphysiol.1977.sp011770. [DOI] [PMC free article] [PubMed] [Google Scholar]