BTM-1086
| 中文名称 | BTM-1086 |
|---|---|
| 中文同义词 | 化合物 T10008 |
| 英文名称 | 1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-3-[(4-methyl-1-piperazinyl)methyl]-2-phenyl-, (2R,3S)-rel- |
| 英文同义词 | 1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-3-[(4-methyl-1-piperazinyl)methyl]-2-phenyl-, (2R,3S)-rel-;BTM1086,BTM 1086 |
| CAS号 | 72293-17-5 |
| 分子式 | C21H25N3OS |
| 分子量 | 367.51 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 72293-17-5.mol |
| 结构式 |  |
BTM-1086 性质
| 熔点 | 257-260 °C |
|---|---|
| 沸点 | 558.2±50.0 °C(Predicted) |
| 密度 | 1.176±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 14.11±0.60(Predicted) |
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.