Identification | Back Directory | [Name]
1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-3-[(4-methyl-1-piperazinyl)methyl]-2-phenyl-, (2R,3S)-rel- | [CAS]
72293-17-5 | [Synonyms]
1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-3-[(4-methyl-1-piperazinyl)methyl]-2-phenyl-, (2R,3S)-rel- | [Molecular Formula]
C21H25N3OS | [MDL Number]
MFCD31628722 | [MOL File]
72293-17-5.mol | [Molecular Weight]
367.51 |
Chemical Properties | Back Directory | [Melting point ]
257-260 °C | [Boiling point ]
558.2±50.0 °C(Predicted) | [density ]
1.176±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [pka]
14.11±0.60(Predicted) |
Hazard Information | Back Directory | [Uses]
BTM-1086 is a potent anti-ulcer and gastric secretory inhibiting agent. | [in vivo]
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 LD50 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[2]. | [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. DOI:10.1016/0014-2999(89)90543-8 [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). |
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