Quetiapine-d8 (fumarate)
(Synonyms: 富马酸喹硫平 d8 (富马酸盐)) 目录号 : GC48462
An internal standard for the quantification of quetiapine
Cas No.:1185247-12-4
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
Quetiapine-d8 is intended for use as an internal standard for the quantification of quetiapine by GC- or LC-MS. Quetiapine is an atypical, second generation antipsychotic compound.1,2,3 It has effects at multiple receptors, antagonizing dopamine D1, D2, and D3 receptors (Kis = 994, 379, and 340 nM, respectively), serotonin 5-HT1A, 5-HT2A, and 5-HT7 receptors (Kis = 394, 118, and 307 nM, respectively), and α1A, α1B, and α2C adrenergic receptors (Kis = 22, 15, and 29 nM, respectively).4,5 Quetiapine also potently antagonizes the histamine H1 receptor (Ki = 11 nM).5
1.Seeman, P.Atypical antipsychotics: Mechanism of actionCan. J. Psychiatry47(1)27-38(2002) 2.Rummel-Kluge, C., Komossa, K., Schwarz, S., et al.Second-generation antipsychotic drugs and extrapyramidal side effects: A systematic review and meta-analysis of head-to-head comparisonsSchizophr. Bull.38(1)167-177(2012) 3.Cerejeira, J., and Mukaetova-Ladinska, E.B.A clinical update on delirium: From early recognition to effective managementNurs. Res. Pract.875196(2011) 4.Richelson, E., and Souder, T.Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compoundsLife Sci.68(1)29-39(2000) 5.Kroeze, W.K., Hufeisen, S.J., Popadak, B.A., et al.H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugsNeuropsychopharmacology28(3)519-526(2003)
| Cas No. | 1185247-12-4 | SDF | |
| 别名 | 富马酸喹硫平 d8 (富马酸盐) | ||
| Canonical SMILES | OC(/C=C/C(O)=O)=O.OCCOCCN(C([2H])([2H])C1([2H])[2H])C([2H])([2H])C([2H])([2H])N1C2=NC(C=CC=C3)=C3SC4=C2C=CC=C4 | ||
| 分子式 | C21H17D8N3O2S•C4H4O4 | 分子量 | 507.6 |
| 溶解度 | DMF: soluble,DMSO: soluble,Methanol: soluble | 储存条件 | -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 | 1.9701 mL | 9.8503 mL | 19.7006 mL |
| 5 mM | 0.394 mL | 1.9701 mL | 3.9401 mL |
| 10 mM | 0.197 mL | 0.985 mL | 1.9701 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。
Measurement of quetiapine and four quetiapine metabolites in human plasma by LC-MS/MS
Biomed Chromatogr 2012 Sep;26(9):1125-32.PMID:22241669DOI:10.1002/bmc.2672
There is interest in monitoring plasma concentrations of N-desalkylquetiapine in relation to antidepressant effect. A simple LC-MS/MS method for quetiapine and four metabolites in human plasma (50 μL) has been developed to measure concentrations of these compounds attained during therapy. Analytes and internal standard (Quetiapine-d8) were extracted into butyl acetate-butanol (10:1, v/v) and a portion of the extract analysed by LC-MS/MS (100 × 2.1 mm i.d. Waters Spherisorb S5SCX; eluent: 50 mmol/L methanolic ammonium acetate, pH* 6.0; flow-rate 0.5 mL/min; positive ion APCI-SRM, two transitions per analyte). Assay calibration (human plasma calibrators) was linear across the ranges studied (quetiapine and N-desalkylquetiapine 5-800, quetiapine sulfoxide 100-15,000, others 2-100 µg/L). Assay validation was as per FDA guidelines. Quetiapine sulfone was found to be unstable and to degrade to quetiapine sulfoxide. In 47 plasma samples from patients prescribed quetiapine (prescribed dose 200-950 mg/day), the (median, range) concentrations found (µg/L) were: quetiapine 83 (7-748), N-desalkylquetiapine, 127 (7-329), O-desalkylquetiapine 12 (2-37), 7-hydroxyquetiapine 3 (<1-48), and quetiapine sulfoxide 3,379 (343-21,704). The analyte concentrations found were comparable to those reported by others except that the concentrations of the sulfoxide were markedly higher. The reason for this discrepancy in unclear.