| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
alpha1-adrenoceptor; beta1-adrenoceptor
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|---|---|
| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
No specific in vitro assays for the deuterated form are provided. The non-deuterated DL-Norepinephrine hydrochloride is a neurotransmitter that targets alpha1 and beta1 adrenoceptors. It has an increasing effect on subendocardial oxygen tension. Deuterium labeling provides a distinct mass signature for analytical quantification without altering receptor binding properties. |
| ln Vivo |
Cellular activity data for the deuterated form are not specifically reported. The non-deuterated norepinephrine acts on adrenergic receptors in various cell types, activating Gq-coupled alpha1 receptors leading to phospholipase C activation and calcium mobilization, and Gs-coupled beta1 receptors leading to cAMP accumulation, resulting in vasoconstriction and increased cardiac contractility.
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| Enzyme Assay |
Radioligand binding assays for adrenergic receptors are performed using membrane preparations from rat brain cortex or transfected cells expressing human alpha1 or beta1 receptors. [3H]-prazosin is used for alpha1 binding and [3H]-CGP12177 for beta1 binding. Test compound is incubated with membranes at varying concentrations. Bound radioligand is separated by filtration and counted by scintillation. Ki values are calculated from competition curves.
|
| Cell Assay |
Cell-based functional assays for adrenergic receptor activation use HEK-293 cells expressing alpha1 or beta1 receptors. For alpha1 activity, cells are loaded with calcium-sensitive dye and treated with serial dilutions of DL-Norepinephrine-d6 (or non-deuterated reference). Receptor activation induces calcium increase measured by fluorescence. For beta1 activity, cAMP accumulation is measured via HTRF or ELISA.
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| Animal Protocol |
In vivo animal studies with DL-Norepinephrine-d6 are not typically performed as it is primarily an analytical internal standard. Pharmacokinetic studies using the deuterated compound as a tracer involve intravenous infusion to rodents or other animals, followed by blood collection at multiple time points. LC-MS/MS analysis quantifies the labeled compound to determine endogenous catecholamine levels.
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| ADME/Pharmacokinetics |
The deuterated form is designed as an analytical internal standard for LC-MS/MS quantification of norepinephrine in biological matrices such as plasma, urine, or brain tissue. It exhibits identical chromatographic retention time as the non-deuterated compound but a distinct mass due to six deuterium atoms. This allows precise and accurate quantification of endogenous norepinephrine levels without isotopic interference.
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| Toxicity/Toxicokinetics |
As an analytical standard, DL-Norepinephrine-d6 hydrochloride is not intended for therapeutic use and thus toxicology studies are not performed on the labeled compound. The non-deuterated norepinephrine is an endogenous catecholamine neurotransmitter with well-characterized physiological actions and is used clinically as a vasopressor agent.
|
| References | |
| Additional Infomation |
DL-Norepinephrine-d6 hydrochloride is a stable isotope-labeled internal standard used exclusively for research and bioanalytical applications. It is particularly valuable for studying neurotransmitter activity, adrenergic receptor function, and cardiovascular health. The compound enables accurate quantification of norepinephrine levels in biological samples for basic neuroscience and clinical research.
|
| Molecular Formula |
C8H6D6CLNO3
|
|---|---|
| Molecular Weight |
211.68
|
| Exact Mass |
205.05
|
| CAS # |
1219803-04-9
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| Related CAS # |
DL-Norepinephrine hydrochloride;55-27-6
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| PubChem CID |
71751187
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| Appearance |
White to off-white solid powder
|
| Melting Point |
40-42°C
|
| Flash Point |
9℃
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| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
13
|
| Complexity |
142
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
[2H]C1=C(C(=C(C(=C1C([2H])(C([2H])([2H])N)O)[2H])O)O)[2H].Cl
|
| InChi Key |
FQTFHMSZCSUVEU-GVFLBQLQSA-N
|
| InChi Code |
InChI=1S/C8H11NO3.ClH/c9-4-8(12)5-1-2-6(10)7(11)3-5;/h1-3,8,10-12H,4,9H2;1H/i1D,2D,3D,4D2,8D;
|
| Chemical Name |
4-(2-amino-1,2,2-trideuterio-1-hydroxyethyl)-3,5,6-trideuteriobenzene-1,2-diol;hydrochloride
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| 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 | 4.7241 mL | 23.6206 mL | 47.2411 mL | |
| 5 mM | 0.9448 mL | 4.7241 mL | 9.4482 mL | |
| 10 mM | 0.4724 mL | 2.3621 mL | 4.7241 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.
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