替仑西平二盐酸盐
| 中文名称 | 替仑西平二盐酸盐 |
|---|---|
| 中文同义词 | 替仑西平二盐酸盐;化合物 T23452;3-甲基-4-(2-(4-甲基哌嗪-1-基)乙酰基)-4H-苯并[B]噻吩并[3,4-E][1,4]二氮杂-10(9H)-酮二盐酸盐 |
| 英文名称 | TELENZEPINE DIHYDROCHLORIDE |
| 英文同义词 | 4,9-DIHYDRO-3-METHYL-4-[(4-METHYL-1-PIPERAZINYL)ACETYL]-10H-THIENO[3,4-B][1,5] BENZODIAZEPIN-10-ONE DIHYDROCHLORIDE;TELENZEPINE DIHYDROCHLORIDE;TELENZEPINE DIHYDROCHLORIDE SELECTIVE M1 MUSCARIN;4,9-Dihydro-3-methyl-4-((4-methyl-1-piperazinyl)acetyl)-(10H)thieno[3,4-b][1,5]benzodiazepin-10-onedihydrochloride;Telenzepine dihydrochloide;Telenzepine hydrate dihydrochloride;4,9-Dihydro-3-methyl-4-((4-methyl-1-piperazinyl)acetyl)-(10H);JTQJFSQQHGPLOX-UHFFFAOYSA-N |
| CAS号 | 147416-96-4 |
| 分子式 | C19H22N4O2S |
| 分子量 | 370.47 |
| EINECS号 | |
| 相关类别 | Acetylcholine receptor |
| Mol文件 | 147416-96-4.mol |
| 结构式 |  |
替仑西平二盐酸盐 性质
| 储存条件 | Store at RT |
|---|---|
| 溶解度 | H2O: >10 mg/mL |
| 形态 | 固体 |
| 颜色 | 白色 |
| 水溶解性 | Soluble to 100 mM in water |
Ki: 0.94 nM (Muscarinic M1 receptor), 17.8 nM (Muscarinic M2 receptor)
At submicromolar concentrations (100 nM), Telenzepine abolishes responses to either muscarine or the muscarinic component of the acetylcholine response. The excitatory effect of muscarine at postsynaptic M1 receptors is dose dependently inhibited by Telenzepine (0.1-1000 nM) at concentrations.
The threshold dose of Telenzepine as an antagonist of the muscarinic depolarization in AH/type 2 neurons is in the range of 0.1-1 nM. The IC
50
of Telenzepine needed to abolish the response is 8.5 nM.
Intravenous Telenzepine potently inhibits gastric acid secretion in the Ghosh-Schild rat (carbachol-stimulated), the chronic fistula rat (basal secretion), or, both intravenously and orally, in the modified Shay rat.
Telenzepine (2.7 μmol/kg; orally) treatment shows significantly longer duration antiulcer effects in the modified Shay rat.
安全信息
| WGK Germany | 3 |
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| 提供商 | 语言 |
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英文
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