Histamine H2-receptor antagonism by propantheline and derivatives.
Article Details
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Hough LB, Barker LA
Histamine H2-receptor antagonism by propantheline and derivatives.
J Pharmacol Exp Ther. 1981 Nov;219(2):453-8.
- PubMed ID
- 6116801 [ View in PubMed]
- Abstract
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.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Methantheline Histamine H2 receptor Protein Humans YesAntagonistDetails