N-Desmethylclomipramine (hydrochloride)
(Synonyms: 去甲氯丙咪嗪盐酸,Desmethylclomipramine hydrochloride) 目录号 : GC44352An Analytical Reference Material
Cas No.:29854-14-6
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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N-Desmethylclomipramine (hydrochloride) is an analytical reference material that is an active metabolite of clomipramine . This product is intended for research and forensic applications. This product is a qualified Reference Material (RM) that has been manufactured and tested to meet ISO/IEC 17025 and ISO Guide 34 guidelines. These materials are tested using validated analytical methods on qualified instrumentation to ensure traceability of measurements. All traceable RMs may be distinguished by their CofAs and can be downloaded below using the batch number located on the product label. For a representative CofA please contact our technical support.
Cas No. | 29854-14-6 | SDF | |
别名 | 去甲氯丙咪嗪盐酸,Desmethylclomipramine hydrochloride | ||
Canonical SMILES | ClC1=CC2=C(C=C1)CCC3=C(C=CC=C3)N2CCCNC.Cl | ||
分子式 | C18H21ClN2•HCl | 分子量 | 337.3 |
溶解度 | DMSO : 25 mg/mL (74.12 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.9647 mL | 14.8236 mL | 29.6472 mL |
5 mM | 0.5929 mL | 2.9647 mL | 5.9294 mL |
10 mM | 0.2965 mL | 1.4824 mL | 2.9647 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 | ||||||||||
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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。
Metabolism of clomipramine in a Japanese psychiatric population: hydroxylation, desmethylation, and glucuronidation
Neuropsychopharmacology 1995 Jul;12(4):323-33.PMID:7576009DOI:10.1016/0893-133X(94)00098-K.
We measured the concentrations of clomipramine and its metabolites, N-Desmethylclomipramine, 8-hydroxy-N-desmethylclomipramine, 8-hydroxyclomipramine by high-performance liquid chromatography in 108 Japanese psychiatric patients receiving clomipramine hydrochloride PO. The concentrations of the glucuronide conjugates of 8-hydroxyclomipramine and 8-hydroxy-N-desmethylclomipramine were assayed via enzymatic hydrolysis. Although there were large interindividual variations of concentrations of parent, intermediate metabolic compounds, and glucuronide conjugates, significant positive correlations were observed between these drug concentrations and daily doses of clomipramine hydrochloride (mg/kg body weight). Although the metabolic ratios for desmethylation, hydroxylation, and glucuronidation that were calculated from steady-state drug concentrations varied substantially with 36-, 14-, and 28-fold interindividual variations, respectively, apparent poor desmethylators, poor hydroxylators, or poor glucuronidators were not found.
Clinical significance of plasma levels of clomipramine, its hydroxylated and desmethylated metabolites: prediction of clinical outcome in mood disorders using discriminant analysis of therapeutic drug monitoring data
J Affect Disord 1993 Dec;29(4):267-79.PMID:8126313DOI:10.1016/0165-0327(93)90017-e.
We measured the plasma concentrations of clomipramine and its metabolites, N-desmethylclompiramine, 8-hydroxy-N-desmethylclomipramine, 8-hydroxyclomipramine in 65 depressed patients with subtypes of DSM-III-R mood disorders receiving clomipramine hydrochloride. There were large interindividual variations in the concentrations of the parent and each of the metabolic compounds, though the overall correlations between drug concentrations and daily doses of clomipramine were highly significant. Metabolic ratios for both desmethylation and hydroxylation varied by 15-35-fold interindividually. Discriminant analysis of the data from drug concentrations and scores of Global Assessment of Functioning revealed that it is useful to monitor the concentrations of both desmethylated and hydroxylated metabolites in order to predict the clinical effects of clomipramine.
Interindividual variations of desmethylation and hydroxylation of clomipramine in an Oriental psychiatric population
J Clin Psychopharmacol 1993 Jun;13(3):181-8.PMID:8354734doi
We measured the concentrations of clomipramine and its metabolites, N-Desmethylclomipramine, 8-hydroxy-N-desmethylclomipramine, and 8-hydroxyclomipramine in plasma in 92 Japanese psychiatric patients receiving clomipramine hydrochloride (Anafranil, Ciba-Geigy Japan Limited, Takarazuka, Japan) by high-performance liquid chromatography. Although there were large interindividual variations of total drug concentrations and concentrations of parent or intermediate metabolic compounds in plasma, significant positive correlations were observed between these drug concentrations and daily doses of clomipramine hydrochloride (milligrams per kilogram of body weight). The metabolic ratios for both desmethylation and hydroxylation varied substantially with 30- to 90-fold interindividual variations. Frequency distribution histograms and probit analyses of these parameters identified only one possible poor hydroxylator but no poor desmethylator of clomipramine. These results suggest that there are large interindividual variations of capacities for hydroxylation and desmethylation of clomipramine in the Oriental population and that therapeutic drug monitoring is essential in clinical practice to reduce the adverse effects of clomipramine and to prevent poor response to clomipramine.
[Clinical significance of plasma levels of clomipramine and its desmethylated and hydroxylated metabolites]
Yakubutsu Seishin Kodo 1993 Aug;13(4):239-49.PMID:8237141doi
Concentrations of clomipramine and its metabolites, N-Desmethylclomipramine (DC), 8-hydroxy-N-desmethylclomipramine (HDC) and 8-hydroxyclomipramine (HC), in plasma were determined in 99 patients treated with clomipramine hydrochloride. Doses patients received were not fixed but titrated according to their clinical severity and response to the treatment. Large interindividual variations were present in the concentrations of parent or each metabolic compounds in plasma, however, strong correlations existed between these drug concentrations and daily doses of clomipramine (0.40-5.10 mg/kg of body weight) (r = 0.62-0.80). Metabolic ratios for desmethylation and those for hydroxylation were calculated from these data, and revealed very large inter-individual variations of 30-36 fold and 10-96 fold, respectively. Pharmacological data from 65 of these patients with DSM-III-R mood disorders were analyzed by discriminant analysis using the scores of Global Assessment of Functioning. The overall prediction value for responder or nonresponder was calculated as 70% 2 wk after the initiation of pharmacotherapy. Concentrations of hydroxylated metabolites in plasma does contribute as much to the prediction of clinical response to clomipramine as desmethylated metabolites.