| Description | BTM-1086 is a potent gastric secretory inhibitor and an anti-ulcer agent. |
| In vitro | 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]. |
| In vivo | 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]. |
| molecular weight | 367.51 |
| Molecular formula | C21H25N3OS |
| CAS | 72293-17-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Eltze M, et al. Affinity profiles of BTM-1086 and BTM-1041 at muscarinic receptor subtypes and at H1- and alpha 1-receptors. Eur J Pharmacol. 1989 Nov 7;170(3):225-34. 2. Hajimu Y, et al. Antiulcer Effect of (-)-cis-2, 3-Dihydro-3-(4-Methylpiperazinylmethyl)-2-Phenyl-1, 5-Benzothiazepin-4-(5H)-One Hydrochloride (BTM-1086) in Experimental Animals. Japan J Pharmacol. 41, 283-292 (1986). |