| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
(E)-10-Hydroxynortriptyline retains affinity for norepinephrine and serotonin transporters, contributing to the therapeutic effects of its parent drug. It also has affinity for muscarinic acetylcholine receptors. In vitro, it is approximately 50% as effective as nortriptyline as a norepinephrine uptake inhibitor.
|
|---|---|
| ln Vitro |
In vitro, (E)-10-Hydroxynortriptyline acts as a norepinephrine reuptake inhibitor with approximately 50% of the effectiveness of nortriptyline. It exhibits weak anticholinergic effects in humans. It is used in clinical pharmacology to understand drug metabolism and receptor binding profiles.
|
| ln Vivo |
In vivo, (E)-10-Hydroxynortriptyline is an active metabolite of nortriptyline with anxiolytic activity. It influences the pharmacokinetics and receptor binding profile of its parent drug. It is studied to understand individualized treatment responses based on metabolic variations.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for (E)-10-Hydroxynortriptyline typically involve measuring its affinity for norepinephrine and serotonin transporters. Radioligand binding displacement assays are performed using membrane preparations expressing these transporters. The compound's ability to inhibit neurotransmitter uptake is measured in synaptosomal preparations.
|
| Cell Assay |
For in vitro cell assays, cells expressing neurotransmitter transporters are treated with (E)-10-Hydroxynortriptyline at various concentrations. Norepinephrine or serotonin uptake inhibition is measured using radiolabeled substrates. Cell viability is assessed to determine cytotoxicity. The compound's effects on receptor-mediated signaling pathways are evaluated.
|
| Animal Protocol |
For in vivo animal studies, (E)-10-Hydroxynortriptyline is typically administered to rodents to study its pharmacokinetics and pharmacodynamics. Blood and brain tissue samples are collected, and the compound is quantified by LC-MS. Behavioral studies may be conducted to evaluate anxiolytic effects.
|
| ADME/Pharmacokinetics |
(E)-10-Hydroxynortriptyline (MW 279.38) has the molecular formula C₁₉H₂₁NO. It is a white to off-white solid powder with a logP of 3.708. The compound is stable under recommended storage conditions (powder at -20°C). It has a density of 1.164 g/cm³ and a boiling point of 462.3°C.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are available for (E)-10-Hydroxynortriptyline. As an active metabolite of the approved antidepressant nortriptyline, its safety profile is expected to be consistent with that of tricyclic antidepressants. It may contribute to the side effect profile of the parent drug.
|
| References |
[1]. Shimoda K, et al. The impact of CYP2C19 and CYP2D6 genotypes on metabolism of amitriptyline in Japanese psychiatric patients. J Clin Psychopharmacol. 2002 Aug;22(4):371-8.
[2]. Shimoda K, et al. Dean L. Amitriptyline Therapy and CYP2D6 and CYP2C19 Genotype. Biotechnology Information (US); 2012-2017 Mar 23. [3]. Bertilsson L, Nordin C, Otani K, et al. Disposition of single oral doses of E-10-hydroxynortriptyline in healthy subjects, with some observations on pharmacodynamic effects. Clin Pharmacol Ther. 1986;40(3):261-267. [4]. Dumont E, von Bahr C, Perry TL Jr, Bertilsson L. Glucuronidation of the enantiomers of E-10-hydroxynortriptyline in human and rat liver microsomes. Pharmacol Toxicol. 1987;61(5):335-341. |
| Additional Infomation |
(E)-10-Hydroxynortriptyline (CAS# 47132-16-1) is an active metabolite of nortriptyline, a tricyclic antidepressant used to treat depression and chronic pain. It has not been approved as a standalone therapeutic agent. The compound is used in research to study drug metabolism, efficacy, and individualized treatment responses. It is also known as E-10-OH-NT.
|
| Molecular Formula |
C19H21NO
|
|---|---|
| Molecular Weight |
279.38
|
| Exact Mass |
279.162
|
| CAS # |
47132-16-1
|
| Related CAS # |
(Z)-10-Hydroxynortriptyline;47132-19-4;(E)-10-Hydroxynortriptyline maleate;74853-74-0;(E)-10-Hydroxynortriptyline-d3
|
| PubChem CID |
6440567
|
| Appearance |
White to off-white solid powder
|
| Density |
1.164g/cm3
|
| Boiling Point |
462.3ºC at 760mmHg
|
| Flash Point |
142.1ºC
|
| LogP |
3.708
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
21
|
| Complexity |
365
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CNCCC=C1C2=CC=CC=C2CC(C3=CC=CC=C31)O
|
| InChi Key |
VAGXZGJKNUNLHK-LFIBNONCSA-N
|
| InChi Code |
InChI=1S/C19H21NO/c1-20-12-6-11-16-15-8-3-2-7-14(15)13-19(21)18-10-5-4-9-17(16)18/h2-5,7-11,19-21H,6,12-13H2,1H3/b16-11+
|
| Chemical Name |
(2E)-2-[3-(methylamino)propylidene]tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,11,13-hexaen-9-ol
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O: 3.57 mg/mL (12.78 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
