(Z)-10-Hydroxynortriptyline
(Synonyms: Z-10-羟基去甲替林) 目录号 : GC60427
An active metabolite of amitriptyline and nortriptyline
Cas No.:47132-19-4
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
cis-10-hydroxy Nortriptyline is an active metabolite of the tricyclic antidepressants amitriptyline and nortriptyline .1,2 It is formed from amitriptyline and nortriptyline by the cytochrome P450 (CYP) isoform CYP2D6.1 cis-10-hydroxy Nortriptyline inhibits norepinephrine reuptake in rat cortical slices (EC50 = 160 nM).2
1.Coutts, R.T., Bach, M.V., and Baker, G.B.Metabolism of amitriptyline with CYP2D6 expressed in a human cell lineXenobiotica27(1)33-47(1997) 2.Bertilsson, l., Mellstr?m, B., and Sj?qvist, F.Pronounced inhibition of noradrenaline uptake by 10-hydroxymetabolites of nortriptylineLife Sci.25(15)1285-1292(1979)
| Cas No. | 47132-19-4 | SDF | |
| 别名 | Z-10-羟基去甲替林 | ||
| Canonical SMILES | OC1C2=CC=CC=C2/C(C3=CC=CC=C3C1)=C\CCNC.[(Z)] | ||
| 分子式 | C19H21NO | 分子量 | 279.38 |
| 溶解度 | 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 | 3.5794 mL | 17.8968 mL | 35.7935 mL |
| 5 mM | 0.7159 mL | 3.5794 mL | 7.1587 mL |
| 10 mM | 0.3579 mL | 1.7897 mL | 3.5794 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。
Amitriptyline metabolism in relation to antidepressive effect
Clin Pharmacol Ther 1984 Apr;35(4):467-73.PMID:6705444DOI:10.1038/clpt.1984.61.
The relationship between amitriptyline (AT) metabolism and clinical response was studied in 14 outpatients treated with a daily dose of 150 mg AT. Riboflavin was added to the medication to check compliance. On days 0, 2, and 7 and at 3, 6, 9, and 13 wk after onset of therapy, blood samples were drawn from the patients 3 (+/- 0.5) hr after the first morning dose and a sample of the first morning urine was taken to check riboflavin. Serum levels of AT and its metabolites, nortriptyline (NT), E- and Z-10-hydroxynortriptyline (E- and Z-10-OH-NT), total (E + Z) 10-hydroxyamitriptyline (tot-10-OH-AT), and desmethylnortriptyline (DNT), were measured by means of HPLC while minimizing adsorption onto glass. On day 0 and after 6 and 13 wk the severity of the depressive disorder was scored by means of the self-rating depression scale of Zung.28 Mean steady-state concentrations of AT, NT, and E-10-OH-NT were in the order of 100 micrograms/l and tot-10-OH-AT and Z-10-OH-NT approximated 20 micrograms/l. DNT concentrations were under 15 micrograms/l. There was great variation in metabolic pattern between patients. After 6 wk concentrations of all compounds were approximately 15% lower than at 3 wk, indicating a weak autoinducible effect of AT or its metabolites. Steady-state concentrations of AT correlated well with that of NT (r = 0.64; P less than 0.05) but not with that of E-10-OH-NT.(ABSTRACT TRUNCATED AT 250 WORDS)
Comparison of amitriptyline metabolism in hepatocytes from streptozocin-induced diabetic rats and from non-diabetic rats
Cell Biol Toxicol 1997 Feb;13(2):131-7.PMID:9049103DOI:10.1023/b:cbto.0000010398.63757.4c.
Biotransformation of amitriptyline (AMI) was studied at different intervals in freshly isolated hepatocytes from healthy or streptozocin-induced diabetic rats in order to investigate the influence of the diabetic state. Levels of free and conjugated AMI, demethylated and hydroxylated metabolites, were assessed by HPLC analysis. In hepatocytes isolated from diabetic rats, AMI was less completely metabolized and the demethylation reaction became more important than in non-diabetic rat hepatocytes. Although the proportions of hydroxylated metabolites decreased in diabetic rats, it always remained predominant. Furthermore, glucuronidation of metabolites was greater, especially for (Z)-10-Hydroxynortriptyline in diabetic animals.