Antiulcer effect of (-)-cis-2,3-dihydro-3-(4-methylpiperazinylmethyl) -2-phenyl-1,5-benzothiazepin-4-(5H)-one hydrochloride (BTM-1086) in experimental animals.

Abstract

Effects of (-) cis-2,3-dihydro-3-(4-methylpiperazinylmethyl)-2-phenyl-1,5-benz othiazepin-4-(5H ) -one hydrochloride (BTM-1086) on various experimental gastric and duodenal ulcers were studied in rats. In the pylorus-ligated ulcer, restraint and water immersion stress ulcer, and drug-induced ulcer (indomethacin, aspirin, reserpine, serotonin, cysteamine), BTM-1086 prevented the development of ulcer at a dose of 0.1 to 1 mg/kg, p.o., but only weakly inhibited the histamine-induced gastric ulcer. The inhibitory activities of BTM-1086 were significantly higher than those of atropine sulfate. In the healing experiment with the acetic acid-induced stomach ulcer, BTM-1086 (1 mg/kg/day, p.o., X 14) showed a significant healing effect, which was higher than that of propantheline bromide. BTM-1086 at a dose of 0.2 mg/kg, i.d., remarkably inhibited the gastric secretion 6 hr after pylorus ligation. The aspirin-induced reductions of the total acid and K+ as well as the increments of the volume and Na+ in the gastric secretion were prevented dose-dependently by pretreatment with BTM-1086.

• Authors: H Yamamoto, Y Nakamura, Y Kunoh, K Ichihara, M Nagasaka, H Asai
• Journal: Japanese journal of pharmacology (Jpn J Pharmacol) Vol. 41 Issue 3 Pg. 283-92 (Jul 1986) ISSN: 0021-5198 [Print] Japan
• PMID: 3761747 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Anti-Ulcer Agents
• Thiazepines
• BTM 1042

Topics

• Animals
• Anti-Ulcer Agents
• Duodenal Ulcer (drug therapy, etiology)
• Male
• Rats
• Rats, Inbred Strains
• Stomach Ulcer (drug therapy, etiology)
• Thiazepines (pharmacology, therapeutic use)