Methoxamine hydrochloride
(Synonyms: 盐酸甲氧明) 目录号 : GC31215
Methoxaminehydrochloride是去甲肾上腺素能受体α1的激动剂。
Cas No.:61-16-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Methoxamine hydrochloride is a noradrenergic α1 agonistsup>[1].
Methoxamine produces a dose-related increase in force development of the cat papillary muscle that was selectively blocked by alpha-adrenergic antagonists. This is suggestive evidence of the presence of alpha-adrenergic receptors in ventricular myocardium[1].Methoxamine greatly enhances bistable behavior in the decerebrate. Methoxamine approximately doubles the amplitude of IPIC without changing its onset voltage, its offset voltage, or its persistence[2].
[1]. Rabinowitz B, et al. Positive inotropic effects of methoxamine: evidence for alpha-adrenergic receptors in ventricular myocardium. Am J Physiol. 1975 Sep;229(3):582-5. [2]. Lee RH, et al. Enhancement of bistability in spinal motoneurons in vivo by the noradrenergic alpha1 agonist methoxamine. J Neurophysiol. 1999 May;81(5):2164-74.
| Cas No. | 61-16-5 | SDF | |
| 别名 | 盐酸甲氧明 | ||
| Canonical SMILES | OC(C(N)C)C1=CC(OC)=CC=C1OC.[H]Cl | ||
| 分子式 | C11H18ClNO3 | 分子量 | 247.72 |
| 溶解度 | DMSO : 50mg/mL | 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 | 4.0368 mL | 20.1841 mL | 40.3682 mL |
| 5 mM | 0.8074 mL | 4.0368 mL | 8.0736 mL |
| 10 mM | 0.4037 mL | 2.0184 mL | 4.0368 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。
Methoxamine hydrochloride in the treatment of paroxysmal supraventricular tachycardia; report of three cases
Ventricular arrythmia induced by methoxamine hydrochloride
The anaesthetised methoxamine-sensitised rabbit model of torsades de pointes
Current guidelines describe strategies on how the potential of non-antiarrhythmic drugs to delay ventricular repolarisation should be assessed. However, the non-clinical guidelines recommend repolarisation assays only and do not advocate experimental models that express the proarrhythmia of concern, torsades de pointes (TdP). Although the repolarisation assays may predict QT interval prolongation in man they cannot alone sufficiently predict proarrhythmia risk. Furthermore, there is also a need for more robust surrogate markers of drug-induced proarrhythmia and such validated markers are on the horizon as a result of the availability of sensitive animal models of TdP. This review will describe the methoxamine-sensitised rabbit model of TdP, one of the most frequently used proarrhythmia models, and present some of it characteristics, its pros and cons and how it historically has been used for assessing proarrhythmia liability of drugs.
The effect of methoxamine hydrochloride (vasoxyl) on cardiac rhythm
A randomised, controlled, crossover study to investigate the safety and response of 1R,2S-methoxamine hydrochloride (NRL001) on anal function in healthy volunteers
Aims: This study aimed to assess the dose and volume effects of suppository preparations and safety of NRL001 (one of four possible stereoisomers of methoxamine hydrochloride) on anal sphincter tone using rectal suppositories in healthy adult volunteers.
Methods: This was a Phase I, single-centre, randomised, double-blind, three-way crossover study during which subjects received three single doses of 1 g rectal suppositories (containing 5 or 10 mg NRL001 or matching placebo) or 2 g rectal suppositories (containing 10 or 15 mg NRL001 or matching placebo) on three separate dosing days. The outcome measures were mean anal resting pressure (MARP) variables (monitored continuously for 20-30 min before and up to 6 h after dosing), pharmacokinetics (PK) and safety assessments.
Results: Twenty-six subjects were dosed with study medication. Two subjects were withdrawn prematurely and were not included in the main analysis. There was a dose-dependent increase in anal sphincter tone (MARP) when comparing the 5 and 10 mg doses of NRL001; however, the 15 mg dose did not have a significantly greater effect than the 10 mg dose. Suppository size (1 or 2 g) did not appear to have an effect on sphincter tone. There was no evidence against dose proportionality for the PK variables, but the mean maximum plasma concentration (Cmax ) for the 1 g suppository group was higher than for the 2 g group. Twenty-one adverse events were reported in 8 (30.8%) subjects. A dose dependent decrease in heart rate was noted; however, there were no adverse events reported that were related to this reduction in heart rate.
Conclusions: The increase in anal sphincter tone supports the potential therapeutic use of NRL001 in treating faecal incontinence, with further studies in patients required. NRL001 was well tolerated in single doses of up to 15 mg.