利喷西平
| 中文名称 | 利喷西平 |
|---|---|
| 中文同义词 | 利喷西平;化合物 T16758 |
| 英文名称 | Rispenzepine |
| 英文同义词 | Rispenzepine;Rispenzepine [inn];Unii-W99llm73R7;11-[(1-methyl-piperidine-3-yl)-carbonyl]-6,11-dihydro-5H-pyrido[2,3-b][1,5]-benzodiazepine-5-one;5H-Pyrido[2,3-b][1,5]benzodiazepin-5-one, 6,11-dihydro-11-[(1-methyl-3-piperidinyl)carbonyl]- |
| CAS号 | 96449-05-7 |
| 分子式 | C19H20N4O2 |
| 分子量 | 336.39 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 96449-05-7.mol |
| 结构式 |  |
利喷西平 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
M 1 , and M 3 receptor
The presence of muscarinic autoreceptors in human and guinea pig trachea is investigated by comparing the effects of the muscarinic receptor antagonists Pirenzepine (M 1 ), Methoctramine (M 2 ), 4-DAMP (M 3 ), and Rispenzepine (M 1 /M 3 ) on cholinergic neural contractile responses evoked by electrical field stimulation (EFS) and [ 3 H]ACh release. The M 1 , M 1 /M 3 , or M 3 antagonists inhibit the EFS-evoked cholinergic contractile response in a concentration-dependent manner (4-DAMP > Rispenzepine > Pirenzepine), whereas Methoctramine facilitates this response at low concentrations (<3 μM). In ACh release studies, the M 3 antagonist has no significant effect, whereas Pirenzepine, Methoctramine, and Rispenzepine significantly increase ACh release in guinea pig trachea. Rispenzepine almost completely inhibits cholinergic, contractile responses at 0.3 μM (92.7±6.2% inhibition, n=6, p<0.05; pD 2 value of 7.31±0.15) .