156137-99-4
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- CAS号:
- 156137-99-4
- 英文名:
- Rapacuronium
- 英文别名:
- Raplon;Org 9487;Rapacuronium;[(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
- 中文名:
- 156137-99-4
- 中文别名:
- 化合物 T12690
- CBNumber:
- CB91179647
- 分子式:
- C37H61BrN2O4
- 分子量:
- 677.81
- MOL File:
- 156137-99-4.mol
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156137-99-4化学性质
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熔点:
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184°
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比旋光度:
-
20D -12.7° (c = 1.01 in CHCl3)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO : ≥ 125 mg/mL (184.42 mM)
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156137-99-4性质、用途与生产工艺
Rapacuronium bromide 是一种毒蕈碱性乙酰胆碱受体 (mAChR) 的变构调节剂。
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.
156137-99-4
上下游产品信息
上游原料
下游产品
156137-99-4, 156137-99-4 相关搜索:
5a-雄甾烷-3a,17b-二醇 2,16-双(哌啶-1-基)雄甾-3,17-二醇 烯丙基三甲基溴化铵 (2b,3a,16b,17b)-2,16-双(哌啶基)-3,17-二乙酰氧基-5-雄甾烷 维库溴铵 N,N,N-三甲基-1-十四烷基溴化铵 十六烷基三甲基溴化铵 溴化乙酰甲胆碱 十六烷基二甲基乙基溴化铵 烯丙基三乙胺溴化物
- C37H61BrN2O4
- C37H61N2O4Br
- 化合物 T12690
- 156137-99-4
- [(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
- Raplon
- Org 9487
- Rapacuronium