Clozapine-d4
(Synonyms: 氯氮平-D4,HF 1854-d4) 目录号 : GC47110An internal standard for the quantification of clozapine
Cas No.:204395-52-8
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
Clozapine-d4 is intended for use as an internal standard for the quantification of clozapine by GC- or LC-MS. Clozapine is a partial agonist at the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 180 nM).1,2 It also binds to 5-HT2A, 5-HT2C, 5-HT3, 5-HT6 and 5-HT7 receptors (Kis = 3.3, 13, 110, 4, and 21 nM, respectively), as well as the histamine H1 and α1-adrenergic receptors (Kis = 2.1 and 23 nM, respectively). It does not bind to the 5-HT1B receptor and has a lower affinity for dopamine receptors (Kis = 540, 150, and 360 nM for D1-3, respectively). Clozapine induces the release of glutamate and D-serine, an agonist at the glycine site of the NMDA receptor, from astrocytes, and reduces the expression of astrocytic glutamate transporters.3 It reverses locomotor hyperactivity and deficits in prepulse inhibition of acoustic startle in a rat neonatal ventral hippocampal ibotenic lesion model of schizophrenia when administered at a dose of 2.5 mg/kg per day.4 Formulations containing clozapine have been used in the treatment of schizophrenia.
1.Millan, M.J.Improving the treatment of Schizophrenia: Focus on serotonin (5-HT)1A receptorsJ. Pharmacol. Exp. Ther.295(3)853-861(2000) 2.Schotte, A., Janssen, P.F., Gommeren, W., et al.Risperidone compared with new and reference antipsychotic drugs: In vitro and in vivo receptor bindingPsychopharmacology (Berl)124(1-2)57-73(1996) 3.Tanahashi, S., Yamamura, S., Nakagawa, M., et al.Clozapine, but not haloperidol, enhances glial D-serin and L-glutamate release in rat frontal cortex and primary cultured astrocytesBr. J. Pharmacol.1651543-1555(2012) 4.Rueter, L.E., Ballard, M.E., Gallagher, K.B., et al.Chronic low dose risperidone and clozapine alleviate positive but not negative symptoms in the rat neonatal ventral hippocampal lesion model of schizophreniaPsychopharmacology (Berl).176(3-4)312-319(2004)
| Cas No. | 204395-52-8 | SDF | |
| 别名 | 氯氮平-D4,HF 1854-d4 | ||
| Canonical SMILES | ClC(C=C1)=CC2=C1NC(C=CC=C3)=C3C(N4C([2H])([2H])CN(C)CC4([2H])[2H])=N2 | ||
| 分子式 | C18H15D4ClN4 | 分子量 | 330.9 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml,Ethanol: 5 mg/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 | 3.0221 mL | 15.1103 mL | 30.2206 mL |
| 5 mM | 0.6044 mL | 3.0221 mL | 6.0441 mL |
| 10 mM | 0.3022 mL | 1.511 mL | 3.0221 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 novel approach to quantitative LC-MS/MS: therapeutic drug monitoring of clozapine and norclozapine using isotopic internal calibration
Anal Bioanal Chem 2013 Nov;405(29):9455-66.PMID:24091736DOI:10.1007/s00216-013-7361-8
Therapeutic drug monitoring (TDM) requires timely results in order to be clinically helpful. Such assays, when carried out using mass spectrometry-based methods, typically involve a batched sample approach with multipoint calibration. Isotopic internal calibration offers the possibility of open-access mass spectrometric analysis with consequent shortening of turnaround times. We measured plasma clozapine and N-desmethylclozapine (norclozapine) concentrations in (1) external quality assessment (EQA) samples (N = 22) and (2) patient samples (N = 100) using liquid chromatography-tandem mass spectrometry with isotopic internal calibration (ICAL-LC-MS/MS). Analyte concentrations were calculated from graphs of the response of three internal calibrators (Clozapine-d4, norclozapine-D8, and clozapine-D8) against concentration. Precision (% RSD) and accuracy (% nominal concentrations) for the ICAL-LC-MS/MS method were <5 % and 104-112 %, respectively for both analytes. There was excellent agreement with consensus mean and with 'spiked' values on analysis of the EQA samples (R (2) = 0.98 and 0.97, respectively, inclusive of clozapine and norclozapine results). In the patient samples, comparison against traditionally calibrated HPLC-UV and LC-MS/MS methods showed excellent agreement (R (2) = 0.97 or better) with small albeit significant mean differences (<0.041 and <0.042 mg/L for clozapine and norclozapine, respectively). These differences probably reflect discrepancies in the in-house preparation of calibrators and/or interference in the UV method. Internal calibration offers a novel and attractive alternative to traditionally calibrated batch analysis in analytical toxicology. The method described has been validated for use in the high-throughput TDM of clozapine and norclozapine, and allows for (1) same-day reporting of results and (2) significant cost savings.