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72293-17-5

中文名稱 BTM-1086
英文名稱 1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-3-[(4-methyl-1-piperazinyl)methyl]-2-phenyl-, (2R,3S)-rel-
CAS 72293-17-5
分子式 C21H25N3OS
分子量 367.51
MOL 文件 72293-17-5.mol
72293-17-5 結(jié)構(gòu)式 72293-17-5 結(jié)構(gòu)式

基本信息

中文別名
化合物 T10008
英文別名
1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-3-[(4-methyl-1-piperazinyl)methyl]-2-phenyl-, (2R,3S)-rel-

物理化學性質(zhì)

熔點257-260 °C
沸點558.2±50.0 °C(Predicted)
密度1.176±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)14.11±0.60(Predicted)

常見問題列表

生物活性
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靶點

Muscarinic receptor

體外研究

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).

體內(nèi)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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