Amisulpride-d5
(Synonyms: 氨磺必利 d5) 目录号 : GC46843
An internal standard for the quantification of amisulpride
Cas No.:1216626-17-3
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
Amisulpride-d5 is intended for use as an internal standard for the quantification of amisulpride by GC- or LC-MS. Amisulpride is a dopamine D2 and D3 receptor antagonist (Kis = 3 and 3.5 nM, respectively).1 It is also an antagonist of the serotonin (5-HT) receptor subtypes 5-HT2B, 5-HT7, and 5-HT7A (Kis = 13, 11.5, and 135.5 nM, respectively). It is selective for these receptors over a panel of 39 additional receptors, ion channels, and transporters (Kis = >1,000 nM for all). Amisulpride increases 7-OH-DPAT-induced decreases in dopamine and acetylcholine release in electrically stimulated rat striatal slices (EC50s = 2.2 and 1.2 nM, respectively).2 It increases the levels of dopamine and the dopamine metabolite 3,4-dihydroxyphenylacetic acid (DOPAC) in rat striatum and nucleus accumbens when administered intraperitoneally at a dose of 10 mg/kg. Amisulpride decreases immobility time in the forced swim test in rats, as well as reduces stress-induced decreases in sucrose consumption in a rat model of depression induced by chronic mild stress.3
1.Abbas, A.I., Hedlund, P.B., Huang, X.P., et al.Amisulpride is a potent 5-HT7 antagonist: Relevance for antidepressant actions in vivoPsychopharmacology (Berl.)205(1)119-128(2009) 2.Schoemaker, H., Claustre, Y., Fage, D., et al.Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivityJ. Pharmacol. Exp. Ther.280(1)83-97(1997) 3.Papp, M., and Wieronska, J.Antidepressant-like activity of amisulpride in two animal models of depressionJ. Psychopharmacol.14(1)46-52(2000)
| Cas No. | 1216626-17-3 | SDF | |
| 别名 | 氨磺必利 d5 | ||
| Canonical SMILES | O=S(C1=CC(C(NCC2N(C([2H])([2H])C([2H])([2H])[2H])CCC2)=O)=C(OC)C=C1N)(CC)=O | ||
| 分子式 | C17H22D5N3O4S | 分子量 | 374.5 |
| 溶解度 | DMSO : 200 mg/mL (534.03 mM; Need ultrasonic); DMSO : 50 mg/mL (133.51 mM; Need ultrasonic); H2O : 0.2 mg/mL (0.53 mM; Need ultrasonic) | 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 | 2.6702 mL | 13.3511 mL | 26.7023 mL |
| 5 mM | 0.534 mL | 2.6702 mL | 5.3405 mL |
| 10 mM | 0.267 mL | 1.3351 mL | 2.6702 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。
A Liquid Chromatography-Tandem Mass Spectrometry Method for Quantifying Amisulpride in Human Plasma and Breast Milk, Applied to Measuring Drug Transfer to a Fully Breast-Fed Neonate
Ther Drug Monit 2016 Aug;38(4):493-8.PMID:27027463DOI:10.1097/FTD.0000000000000300
Background: Amisulpride is a second generation atypical antipsychotic drug. The management of psychosis exacerbation in late pregnancy or during lactation is often hampered by inadequate knowledge of risk to the baby from placental transfer or breast milk transfer of drugs. There is no specific information on adverse effects from amisulpride. To gather guiding information from one mother-baby pair, we conducted a drug concentration study on the fourth post-natal day and developed a novel liquid chromatography-tandem mass spectrometry method with application to the very small plasma volumes obtainable from a neonate, requiring 15 μL of plasma, and with application to human breast milk. Methods: Plasma and breast milk extracts, spiked with deuterated internal standard (Amisulpride-d5) were separated isocratically with a buffered water-methanol-acetonitrile mobile phase. A tandem mass spectrometer in positive electrospray ionisation mode with multiple reaction monitoring was used for detection. Results: Method linearity, sensitivity, imprecision, matrix effects, recovery, and overall process efficiency were satisfactory for milk and plasma. No interferences were found from a broad range of psychotropic and general drugs. The breast milk area under the concentration-time curve for the interval 0-12 hours was 10,726 mcg·h·L, corresponding to a mean breast milk concentration of 894 mcg/L. Breast milk amisulpride was 12-fold higher than the simultaneous plasma concentration. The baby's plasma amisulpride concentration was 10.5% of the maternal plasma concentration. Conclusions: An assay was developed that is suitable for therapeutic drug monitoring of amisulpride. Its application to breast milk and neonate plasma showed that amisulpride partitioned strongly into breast milk and that the neonate reached plasma levels that were more than desirable for a psychotropic drug.