Scopolamine N-oxide hydrobromide (Hyoscine N-oxide hydrobromide)
(Synonyms: 东莨菪碱N-氧化物氢溴酸盐一水合物) 目录号 : GC30901
Scopolamine N-Oxide (Hyoscine N-oxide, Genoscopolamine) is a muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors.
Cas No.:6106-81-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Scopolamine N-Oxide (Hyoscine N-oxide, Genoscopolamine) is a muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors.
| Cas No. | 6106-81-6 | SDF | |
| 别名 | 东莨菪碱N-氧化物氢溴酸盐一水合物 | ||
| Canonical SMILES | Br[H].C[N]1([O])[C@H]2[C@@H](O3)[C@@H]3[C@@H]1C[C@H](OC([C@@H](C4=CC=CC=C4)CO)=O)C2 | ||
| 分子式 | C17H22BrNO5 | 分子量 | 400.26 |
| 溶解度 | DMSO : 300 mg/mL (749.51 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4984 mL | 12.4919 mL | 24.9838 mL |
| 5 mM | 0.4997 mL | 2.4984 mL | 4.9968 mL |
| 10 mM | 0.2498 mL | 1.2492 mL | 2.4984 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Affinities of the protonated and non-protonated forms of hyoscine and hyoscine N-oxide for muscarinic receptors of the guinea-pig ileum and a comparison of their size in solution with that of atropine
1. At 37 degrees C in 0.1 M NaCl the pKa of hyoscine (10 mM) is 7.53; the non-protonated form has about one-tenth of the affinity (log K = 8.58) of the protonated form (log K = 9.58) for muscarine-sensitive receptors of the guinea-pig ileum at 37 degrees C. 2. In the same conditions the pKa of hyoscine N-oxide is 5.78 and the non-protonated form is inactive on the ileum whereas the protonated form is highly active with log K estimated to be 9.9, at least as active as hyoscine methobromide (log K = 9.85). 3. Hyoscine methobromide appears to occupy less space in water than atropine methobromide; hyoscine hydrochloride occupies less space than hyoscyamine hydrochloride: the non-protonated forms are slightly bigger. Hyoscine N-oxide hydrobromide is slightly smaller than hyoscine methobromide but the removal of the proton is accompanied by a reduction in volume, such as is seen with other zwitterions. 4. These differences in volume indicated a reduction in entropy on solution which may allow a greater increase in entropy on binding to receptors and hence greater affinity. The higher activity of hyoscine itself could also be due to the presence of the N-methyl group in the axial position, rather than equatorial as in hyoscyamine or atropine. 5. The different position of the N-methyl group may partly explain why the pKa of hyoscine is 2 units lower than that of hyoscyamine or atropine. It is also probable that the unionized form of hyoscine is stabilized by hydration. 6. Although hyoscine N-oxide is only weakly active at pH 7.6, it is present in a highly active form in the acid environment of the stomach and so might be expected to act selectively at this site.
'Death rattle' after withdrawal of mechanical ventilation: practical and ethical considerations
The noise produced by oscillatory movements of secretions in oropharynx, hypopharynx and trachea during inspiration and expiration in unconscious terminal patients is often described as 'the death rattle'. The reported incidence of death rattle in terminally ill patients varied between six and 92%. It is most commonly reported in patients dying from pulmonary malignancies, primary brain tumours or brain metastases, and predicts death within 48 hours in 75% of the patients. Clinical studies demonstrate that hyoscine hydrobromide is effective at improving symptoms. After withdrawal of artificial ventilation on the intensive care unit, excessive respiratory secretions resulting in rattling breathing, during the last hours of life, is not uncommon. Physicians and nurses experience considerable difficulties and frustrations in treating the death rattle. The distressing experience and negative influence in the bereavement process indicates an ethical demand to treat this symptom from the perspective of others merely than that of the patient. This article provides practical and ethical considerations in the management of this near-death symptom. The fact that relatives were relieved in almost all cases, in which a positive effect was obtained, makes treatment in anticipation of death rattle an ethical demand. In practice, injectable scopolamine is the reference drug for symptomatic treatment of death rattle.