Axomadol
(Synonyms: 阿索马多; EN3324) 目录号 : GC64853
Axomadol (EN3324) 具有阿片类激动特性，对单胺类的再摄取具有抑制作用，可用于缓解疼痛研究。
Cas No.:187219-99-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Axomadol (EN3324) is a centrally active analgesic agent with opioid agonistic properties and inhibitory effects on the reuptake of monoamines[1].
[1]. VÍctor Mangas-Sanjuan, et al. Population Pharmacokinetic/Pharmacodynamic Modelling of the Effects of Axomadol and Its O-demethyl Metabolite on Pupil Diameter and Nociception in Healthy Subjects. Br J Clin Pharmacol . 2016 Jul;82(1):92-107.
| Cas No. | 187219-99-4 | SDF | Download SDF |
| 别名 | 阿索马多; EN3324 | ||
| 分子式 | C16H25NO3 | 分子量 | 279.37 |
| 溶解度 | 储存条件 | 4°C, away from moisture and light | |
| 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 | 3.5795 mL | 17.8974 mL | 35.7948 mL |
| 5 mM | 0.7159 mL | 3.5795 mL | 7.159 mL |
| 10 mM | 0.3579 mL | 1.7897 mL | 3.5795 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。
Population pharmacokinetic/pharmacodynamic modelling of the effects of Axomadol and its O-demethyl metabolite on pupil diameter and nociception in healthy subjects
Br J Clin Pharmacol 2016 Jul;82(1):92-107.PMID:26924818DOI:PMC4917809
Aim: The aim of the present study was to characterize the pharmacokinetic/pharmacodynamic (PK/PD) properties of the active components of Axomadol and to quantify their contribution to observed the pupillometric and analgesic (measured through the cold pressor test) effects linking the PD engagement biomarker with clinical response. Methods: Healthy subjects (n = 74) received either placebo or Axomadol orally at doses ranging from 66 mg to 225 mg following multiple dosing regimens in two separate clinical trials. Plasma concentrations of the two enantiomers of Axomadol and their metabolites, and PD responses were measured at specific times. The population analysis was performed using NONMEM 7.2. Results: The kinetics of the parent drug and its metabolite could be described simultaneously using an extra compartment mimicking the liver, where the metabolite is formed. The SS parent compound elicited a plasma concentration-dependent increase in pupil diameter, with estimates (percentage relative standard errors) of maximal effect (Emax ) and plasma concentration exerting a half-maximal effect (C50 ) of 0.79 (17.4) mm, and 90.7 (27) ng ml(-1) , respectively. The predicted effect site concentrations of the RR O-demethyl metabolite decreased the pupil diameter linearly, with an estimate of the slope of 0.00967 (18.7) mm·ml ng(-1) . An additive model, integrating the net effect on pupil diameter, described adequately the reduction in pain with a linear function. The PK/PD model revealed that each 0.5 mm change in pupil diameter is associated with a 10% decrease in cold pressor area under the concentration-time curve effects. Conclusions: The PK/PD analysis performed enabled the individual contributions of the active compounds to the observed effects to be identified and quantified. These effects were in accordance with the known mechanisms of action - namely, opioid agonism and noradrenaline reuptake inhibition.