BTM-1086 is a potent gastric secretory inhibitor and an anti-ulcer agent.

BTM-1086 has a high affinity (pKi: 8.31-9.15) for the three muscarinic receptor subtypes in the guinea-pig cortex (M1), heart (M2), and salivary glands (M3) [1].

BTM-1086 (0.1 to 1 mg/kg, p.o.) prevents the development of ulcers, but only weakly inhibits the histamine-induced gastric ulcer. The inhibitory activities of BTM-1086 are 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., x14) shows a significant healing effect, which is higher than that of propantheline bromide. BTM-1086 (0.2 mg/kg, i.d.) remarkably inhibit 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 are prevented dose-dependently by pretreatment with BTM-1086. The LD50 value by oral, s.c., and i.v. administration with BTM-1086 is 880, 630, and 113 mg/kg, respectively, for male rats and 830, 650, and 119 mg/kg, respectively, for female rats [2].