BTM-1086

Muscarinic receptor

Functional and binding experiments shows that the (-) enantiomer (BTM-1086) has a high affinity (pK _i =8.31-9.15) for the three muscarinic receptor subtypes in guinea-pig cortex (M1), heart (M2) and salivary glands (M3).

BTM-1086 prevents the development of ulcer at a dose of 0.1 to 1 mg/kg, p.o., 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 at a dose of 0.2 mg/kg , i.d., remarkably inhibits 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 LD ₅₀ value by oral, s.c., and i.v. administration with this compound is 880, 630 and 113 mg/kg, respectively, for male rats and 830, 650 and 119 mg/kg, respectively, for female rats.