1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Levonordefrin

Levonordefrin  (Synonyms: (-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin)

Cat. No.: HY-107915 Purity: 98.38%
Handling Instructions Technical Support

Levonordefrin ((-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin) is an α-adrenergic receptor agonist with blood pressure regulatory properties. Levonordefrin is a key metabolite responsible for the hypotensive effect of α-methyldopa. By stimulating central α-adrenergic receptors in the nucleus tractus solitarius region of the medulla oblongata, Levonordefrin induces centrally mediated hypotension and bradycardia. When administered intravenously, Levonordefrin increases mean arterial blood pressure in a dose-dependent manner. Levonordefrin is applicable for research on the pathophysiology of hypertension and drug metabolism.

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Levonordefrin

Levonordefrin Chemical Structure

CAS No. : 829-74-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
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100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Levonordefrin ((-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin) is an α-adrenergic receptor agonist with blood pressure regulatory properties. Levonordefrin is a key metabolite responsible for the hypotensive effect of α-methyldopa. By stimulating central α-adrenergic receptors in the nucleus tractus solitarius region of the medulla oblongata, Levonordefrin induces centrally mediated hypotension and bradycardia. When administered intravenously, Levonordefrin increases mean arterial blood pressure in a dose-dependent manner. Levonordefrin is applicable for research on the pathophysiology of hypertension and drug metabolism[1][2].

IC50 & Target

α1-adrenergic receptor

 

In Vivo

Microinjection of Levonordefrin into the bilateral nucleus tractus solitarius (NTS; 0.6 μL infused over 30 seconds, 5.8-92.0 nmol) induces a dose-dependent, sustained decrease in mean arterial blood pressure and heart rate in rat NTS, and these effects are blocked by prior local administration of Phentolamine (HY-12717)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar rats (male, 200-250 g, anesthetized with urethane)[2]
Dosage: 5.8 nmol; 23.0 nmol; 92.0 nmol; 23.0 nmol (post-Phentolamine pre-treatment)
Administration: bilateral microinjection into nucleus tractus solitarii; 0.6 μL over 30 seconds; 23.0 nmol (10 minutes after phentolamine microinjection)
Result: Caused a maximum mean blood pressure decrease of -16 ± 2 mm Hg and heart rate decrease of -27 ± 11 bpm at 5 minutes, with effects resolved by 30 minutes (blood pressure +1 ± 26 mm Hg, heart rate +42 ± 26 bpm) at 5.8 nmol.
Caused sustained, statistically significant (p < 0.01) decreases in mean blood pressure and heart rate through 30 minutes: -33 ± 6 mm Hg/-56 ± 14 bpm at 5 minutes, -33 ± 6 mm Hg/-66 ± 7 bpm at 10 minutes, -23 ± 5 mm Hg/-43 ± 7 bpm at 20 minutes, -15 ± 4 mm Hg/-28 ± 9 bpm at 30 minutes at 23.0 nmol.
Caused sustained, statistically significant (p < 0.01) decreases in mean blood pressure and heart rate through 30 minutes: -39 ± 5 mm Hg/-38 ± 7 bpm at 5 minutes, -43 ± 4 mm Hg/-75 ± 11 bpm at 10 minutes, -32 ± 3 mm Hg/-86 ± 11 bpm at 20 minutes, -20 ± 3 mm Hg/-74 ± 14 bpm at 30 minutes at 92.0 nmol.
Produced maximum changes of +31 ± 6 mm Hg (blood pressure) and +27 ± 9 bpm (heart rate) within 2 minutes when 23.0 nmol was administered 10 minutes after prior phentolamine microinjection, completely preventing and reversing hypotensive and bradycardic effects.
Clinical Trial
Molecular Weight

183.21

Formula

C9H13NO3

CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

OC1=CC=C([C@@H](O)[C@@H](N)C)C=C1O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (272.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 5 mg/mL (27.29 mM; ultrasonic and warming and adjust pH to 1 with HCl and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.4582 mL 27.2911 mL 54.5822 mL
5 mM 1.0916 mL 5.4582 mL 10.9164 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (13.65 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (13.65 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.62%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 5.4582 mL 27.2911 mL 54.5822 mL 136.4554 mL
5 mM 1.0916 mL 5.4582 mL 10.9164 mL 27.2911 mL
10 mM 0.5458 mL 2.7291 mL 5.4582 mL 13.6455 mL
15 mM 0.3639 mL 1.8194 mL 3.6388 mL 9.0970 mL
20 mM 0.2729 mL 1.3646 mL 2.7291 mL 6.8228 mL
25 mM 0.2183 mL 1.0916 mL 2.1833 mL 5.4582 mL
DMSO 30 mM 0.1819 mL 0.9097 mL 1.8194 mL 4.5485 mL
40 mM 0.1365 mL 0.6823 mL 1.3646 mL 3.4114 mL
50 mM 0.1092 mL 0.5458 mL 1.0916 mL 2.7291 mL
60 mM 0.0910 mL 0.4549 mL 0.9097 mL 2.2743 mL
80 mM 0.0682 mL 0.3411 mL 0.6823 mL 1.7057 mL
100 mM 0.0546 mL 0.2729 mL 0.5458 mL 1.3646 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Levonordefrin
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