Potent and specific blockade by AH 22216 of histamine-H2-receptor-mediated acid secretion in isolated rabbit gastric cells.
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 x 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.
D000632:Aminopyrine / Q000378:metabolism; D000818:Animals; D002927:Cimetidine / Q000494:pharmacology; D005744:Gastric Acid / Q000378:metabolism*; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism; D006632:Histamine / Q000494:pharmacology; D008297:Male; D010880:Piperidines / Q000494:pharmacology*; D011817:Rabbits; D011968:Receptors, Histamine / Q000187:drug effects*; D011970:Receptors, Histamine H2 / Q000187:drug effects* / Q000502:physiology; D014230:Triazoles
D010880:Piperidines; D011968:Receptors, Histamine; D011970:Receptors, Histamine H2; D014230:Triazoles; D000632:Aminopyrine; D002927:Cimetidine; D006632:Histamine; C038304:lamtidine