4-Methoxyphenyl 4-(3,4,5-trimethoxybenzyl)-1-piperazineacetate monofumarate monohydrate (KB-5492), a new anti-ulcer agent with a selective affinity for the sigma receptor, prevents cysteamine-induced duodenal ulcers in rats by a mechanism different from that of cimetidine

Jpn J Pharmacol. 1994 Mar;64(3):221-4. doi: 10.1254/jjp.64.221.

Abstract

Both KB-5492, a new anti-ulcer agent, and cimetidine, administered orally at 25-200 mg/kg, dose-dependently prevented cysteamine (400 mg/kg, s.c.)-induced duodenal ulcers in rats with ED50 values of 63 and 40 mg/kg, respectively. Anti-ulcer doses of cimetidine, but not KB-5492, inhibited gastric acid hypersecretion induced by cysteamine (400 mg/kg, s.c.). In contrast, anti-ulcer doses of KB-5492, but not cimetidine, increased duodenal HCO3- secretion in normal anesthetized rats. These findings suggest that KB-5492 prevents cysteamine-induced duodenal ulcers by stimulating duodenal HCO3- secretion, whereas cimetidine does so by inhibiting cysteamine-induced gastric acid hypersecretion.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Anti-Ulcer Agents / metabolism
  • Anti-Ulcer Agents / therapeutic use*
  • Bicarbonates / metabolism
  • Cimetidine / therapeutic use*
  • Cysteamine
  • Duodenal Ulcer / chemically induced
  • Duodenal Ulcer / prevention & control*
  • Duodenum / drug effects
  • Duodenum / metabolism
  • Gastric Acid / metabolism
  • Intestinal Secretions / drug effects
  • Male
  • Piperazines / metabolism
  • Piperazines / therapeutic use*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, sigma / drug effects
  • Receptors, sigma / metabolism*

Substances

  • Anti-Ulcer Agents
  • Bicarbonates
  • Piperazines
  • Receptors, sigma
  • KB 5492
  • Cysteamine
  • Cimetidine