Original Articles
Copyright ©The Author(s) 2000. Published by Baishideng Publishing Group Inc. All rights reserved.
World J Gastroenterol. Oct 15, 2000; 6(5): 651-658
Published online Oct 15, 2000. doi: 10.3748/wjg.v6.i5.651
Stimulation by nizatidine, a histamine H2-receptor antagonist, of duodenal HCO3- secretion in rats: relation to anti-cholinesterase activity
Koji Takeuchi, Shoji Kawauchi, Hideo Araki, Shigeru Ueki, Osamu Furukawa
Koji Takeuchi, Shoji Kawauchi, Hideo Araki, Shigeru Ueki, Department of Pharmacology and Experimental Therapeutics, Kyoto Pharmaceutical University, Misasagi, Yamashina, Kyoto 607-8414, Japan
Osamu Furukawa, CURE, Bldg.114, Suite 217 West LA VAMC 11301 Wilshire Blvd. Los Angeles, CA 90073
Author contributions: All authors contributed equally to the work.
Correspondence to: Koji Takeuchi, Ph.D., Department of Pharmacology and Experimental Therapeutics Kyoto Pharmaceutical University, Misasagi, Yamashina, Kyoto 607-8414, Japan. takeuchi@mb.kyoto-phu.ac.jp
Received: August 8, 2000
Revised: August 18, 2000
Accepted: August 25, 2000
Published online: October 15, 2000
Abstract

AIM: To examine whether nizatidine stimulates duodenal HCO3- secretion in rats by inhibiting AChE activity.

METHODS: Under pentobarbital anesthesia, a proximal duodenal loop was perfused with saline, and the HCO3- secretion was measured at pH7.0 using a pH-stat method and by adding 10 mM HCl. Nizatidine, neostigmine, carbachol or famotidine was administered i.v. as a single injection.

RESULTS: Intravenous administration of nizatidine (3-30 mg/kg) dose-dependently increased duodenal HCO3- secretion, and the effect at 10 mg/kg was equivalent to that obtained by carbachol at 0.01 mg/kg. This nizatidine action was observed at the same dose range that inhibited acid secretion and enhanced gastric motility, mimicked by i.v. injection of neostigmine (0.03 mg/kg), and significantly attenuated by bilateral vagotomy and prior s.c. administration of atropine but not by indomethacin, a cyclooxygenase inhibitor, or NG-nitro-L-arginine methyl ester, a NO synthase inhibitor. The HCO3- secretory response to acetylcholine (0.001 mg/kg) was significantly potentiated by the concurrent administration of nizatidine (3 mg/kg, i.v.). The IC50 of nizatidine for AChE of rat erythrocytes was 1.4 × 10-6 M, about 12 times higher than that of neostigmine. Neither famotidine (> 10-3 M, 30 mg/kg, i.v.) nor cisapride (> 10-3 M, 3 mg/kg, i.v.) had any influence on AChE activity or duodenal HCO3- secretion. Duodenal damage induced by acid perfusion (100 mM HCl for 4 h) in the presence of indomethacin was significantly prevented by nizatidine and neostigmine, at the doses that increased the HCO3- secretion.

CONCLUSION: Nizatidine stimulates duodenal HCO3- secretion, in both vagal-dependent and atropine-sensitive manners, and the action is associated with the anti-AChE activity of this agent.

Keywords: nizatidine; histamine H2 receptor blockaders; duodenal HCO3- secretion; cholinesterase inhibitors; rats