156137-99-4
| 中文名称 | 156137-99-4 |
|---|---|
| 中文同义词 | 化合物 T12690 |
| 英文名称 | Rapacuronium |
| 英文同义词 | Rapacuronium;Org 9487;Raplon;[(2S,3S,5S,8R,9S,10S,13S,14S,16S,17R)-3-acetyloxy-10,13-dimethyl-2-piperidin-1-yl-16-(1-prop-2-enylpiperidin-1-ium-1-yl)-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl] propanoate |
| CAS号 | 156137-99-4 |
| 分子式 | C37H61BrN2O4 |
| 分子量 | 677.81 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 156137-99-4.mol |
| 结构式 |  |
156137-99-4 性质
| 熔点 | 184° |
|---|---|
| 比旋光度 | 20D -12.7° (c = 1.01 in CHCl3) |
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：≥125mg/mL（184.42mM） |
| 形态 | 固体 |
| 颜色 | 浅黄至黄色 |
Muscarinic receptor
Rapacuronium binds to all muscarinic receptor subtypes at physiologically relevant concentrations and displays micromolar affinity and slight selectivity towards M 2 receptor. Rapacuronium exhibits complex effects on the kinetics of ACh binding and subsequent receptor activation estimated from stimulation of [ 35 S]GTPγS binding. Rapacuronium alone concentration dependently lowers [ 35 S]GTPγS binding to membranes with a maximal effect of approximately 25% at odd-numbered subtypes and 15% at even-numbered subtypes, with EC 50 ranging from 28 μM at M 2 receptors to 76 μM at M 3 receptors. While the EC 50 values of Rapacuronium in inhibiting [ 35 S]GTPγS binding at individual subtypes correlated with affinities measured in binding experiments with [ 3 H]ACh (R 2 = 0.76) they are lower (4- to 12-fold) at all subtypes. Measurements of ACh-stimulated [ 35 S]GTPγS binding in the presence of 0.1, 1 and 10 μM Rapacuronium shows differential effects of Rapacuronium on receptor activation by an orthosteric agonist at individual receptor subtypes. At even-numbered subtypes 1 μM and 10 μM Rapacuronium significantly increases ACh EC 50 , with lowering of E MAX at 10 μM Rapacuronium. At this subtype 0.1 and 1 μM Rapacuronium causes a significant 2-fold decrease in ACh EC 50 and approximately 60% and 35% increase in E MAX , respectively. Rapacuronium at 10 μM increases ACh EC 50 by about 3-fold without a significant change in E MAX . Rapacuronium (0.1 - 10 μM) has no effect on ACh efficacy at the M 1 and M 5 subtypes but decreases the EC 50 of ACh in stimulating [ 35 S]GTPγS binding by 1.5- and 4-fold, respectively, at concentrations of 0.1 and 1 μM. However, this effect is not evident at 10 μM Rapacuronium.
Time course of the neuromuscular effects of Rapacuronium following the administration of the 2×ED 90 doses to rats and guinea-pigs with ED 90 of 5953±199 and 187±16 µg/kg in rat and guinea pig, respectively.