Pharmacological studies on the new quinoline derivative 1-(2-methylphenyl)-4-[(3-hydroxypropyl) amino]-6-trifluoromethoxy-2,3-dihydropyrrolo[3,2-c] quinoline with potent anti-ulcer effect.

Abstract

The effects of the novel acylquinoline derivative, 1-(2-methylphenyl)-4-[(3-hydroxypropyl)amino]-6-trifluoromethoxy-2,3- dihydropyrrolo[3,2-c]quinoline (AU-006) on experimental ulcer models and on gastric secretion were examined. AU-006 prevented dose dependently gastric lesions induced by 95% ethanol when given orally (30-300 mg/kg). Similarly, gastric lesions caused by 0.3 N NaOH were inhibited by oral pretreatment with AU-006. To investigate the anti-ulcer mechanism of AU-006, the effect of AU-006 on gastric acid secretion was tested. Intraduodenal administration of AU-006 reduced in vivo gastric acid secretion. The protective effect of AU-006 against gastric lesions induced by ethanol was not affected by a nitric oxide synthase inhibitor, NG-nitro-L-arginine-methyl ester (l-NAME). In addition, the ethanol-induced mucus reduction was not recovered upon AU-006 administration. These results suggest that AU-006 is effective in the treatment of gastric ulcers by inhibiting gastric acid secretion, and that its activity is not related to either nitric oxide production or mucus secretion.

• Authors: H G Cheon, H J Kim, S S Kim, J K Choi, J Y Kong
• Journal: Arzneimittel-Forschung (Arzneimittelforschung) Vol. 48 Issue 12 Pg. 1168-71 (Dec 1998) ISSN: 0004-4172 [Print] Germany
• PMID: 9893932 (Publication Type: Journal Article)

Chemical References

• Anti-Ulcer Agents
• Enzyme Inhibitors
• Quinolines
• Nitric Oxide Synthase
• AU 006

Topics

• Animals
• Anti-Ulcer Agents (pharmacology)
• Enzyme Inhibitors (pharmacology)
• Gastric Acid (metabolism)
• Gastric Mucosa (drug effects, pathology)
• Male
• Nitric Oxide Synthase (antagonists & inhibitors)
• Pylorus (drug effects)
• Quinolines (pharmacology)
• Rats
• Rats, Sprague-Dawley
• Stomach Ulcer (chemically induced, prevention & control)