Histamine H2-receptor antagonism by propantheline and derivatives.

The histamine H2-antagonist properties of propantheline and its tertiary amine derivatives were investigated. Propantheline and methantheline inhibited the histamine-activated cyclase of guinea-pig brain homogenates, a well characterized H2-receptor preparation; the inhibition was not competitive. Tertiary amine derivatives were competitive H2-antagonist in this system, one such derivative exhibiting greater potency than cimetidine. In concentrations blocking the brain H2-receptors, these derivatives had no effect on atrial histamine dose-response curves, but evidence for their antagonism on peripheral H2-receptors was obtained with papillary muscle preparations. The results suggest that the guinea-pig brain H2-linked cyclase of homogenates is a sensitive predictor of peripheral H2-antagonist activity. These drugs may also be effective inhibitors of gastric secretion.

Citation

L B Hough, L A Barker. Histamine H2-receptor antagonism by propantheline and derivatives. The Journal of pharmacology and experimental therapeutics. 1981 Nov;219(2):453-8

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PMID: 6116801

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