BTM-1086
- CAS号:72293-17-5
- 英文名:1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-3-[(4-methyl-1-piperazinyl)methyl]-2-phenyl-, (2R,3S)-rel-
- 中文名:BTM-1086
- CBNumber:CB63339541
- 分子式:C21H25N3OS
- 分子量:367.51
- MOL File:72293-17-5.mol
- 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 :Soluble in DMSO
- 酸度系数(pKa) :14.11±0.60(Predicted)
BTM-1086性质、用途与生产工艺
- 生物活性 BTM-1086是一种有效的抗溃疡和胃分泌抑制剂。
-
靶点
Muscarinic receptor
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体外研究
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).
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体内研究
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.
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