Up-regulation of H2 Receptor and Adenylate Cyclase in Rabbit Parietal Cells During Prolonged Treatment with H2-receptor Antagonists

Overview

Journal Dig Dis Sci

Specialty Gastroenterology

Date 1999 Sep 24

PMID 10492156

Citations 4

Authors

K Takeuchi

M Kajimura

M Kodaira

S Lin

H Hanai

E Kaneko

Affiliations

Soon will be listed here.

Abstract

Intragastric hyperacidity occurs after abrupt withdrawal of histamine H2-receptor antagonists, and the prolonged administration of these agents induces tachyphylaxis of the inhibitory effects on gastric acid secretion. We examined the effect of the prolonged administration of H2-receptor antagonists on the H2-receptor signaling system in parietal cells isolated from rabbits that had received H2-receptor antagonists for 14 days. [125I]aminopotentidine (APT) binding sites to H2 receptors in parietal cell membranes were increased without any significant change in the affinity for [125I]APT. The expression of Gs(alpha), guanosine triphosphate (GTP)-binding protein coupled to H2 receptor, was slightly increased. Basal as well as GTP- or histamine-stimulated cAMP production was increased, but no significant change was observed in the presence of an H2-receptor antagonist. The up-regulation of the H2 receptor and adenylate cyclase appeared to cause hypersecretion of acid after withdrawal of H2-receptor blockade.

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