Histamine H2-receptor antagonism by propantheline and derivatives.

Article Details

Citation

Copy to clipboard

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	Yes	Antagonist	Details