Potent and specific blockade by AH 22216 of histamine-H2-receptor-mediated acid secretion in isolated rabbit gastric cells. Issue 9 (September 1983)

• Record Type: Journal Article
• Authors: Gespach, Christian; Menez, Isabelle; Emami, Shahin
• Is Part Of: Bioscience reports. Volume 3:Issue 9(1983)
• Page Start: 871
• Page End: 878
• Publication Date: 1983-09
• Subjects: Molecular biology -- Periodicals; Cytology -- Periodicals; 572.8
• DOI: 10.1007/BF01133786
• Languages: English
• ISSNs: 0144-8463

Abstract

Abstract : AH 22216 is a new histamine-H2 -receptor antagonist which possesses a triazole ring. When compared to cimetidine, AH 22216 is about 100 times more potent (Ki = 0.21×10 −8 M) in inhibiting histamine-stimulated acid secretion in isolated rabbit gastric cells. These two antihistamines have no effect on carbachol-stimulated acid secretion in the system. The data indicate that AH 22216 interacts directly and specifically on the gastric H2 -receptor of the parietal cell and are consistent with the reported pharmacological potencies of AH 22216 and cimetidine on histamine-induced gastric-acid secretion in vivo. AH 22216 could thus be a useful therapeutic agent in patients with peptic ulcers.