2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. Norbinaltorphimine dihydrochloride

Norbinaltorphimine dihydrochloride  (Synonyms: nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride)

Cat. No.: HY-100903 Purity: 98.17%
SDS COA Handling Instructions

Molarity Calculator

Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.

For research use only. We do not sell to patients.

Norbinaltorphimine dihydrochloride Chemical Structure

Norbinaltorphimine dihydrochloride Chemical Structure

CAS No. : 113158-34-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 154 In-stock
Solution
10 mM * 1 mL in DMSO USD 154 In-stock
Solid
5 mg USD 95 In-stock
10 mg USD 150 In-stock
50 mg USD 520 In-stock
100 mg USD 830 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Norbinaltorphimine dihydrochloride:

Norbinaltorphimine dihydrochloride Related Antibodies

Top Publications Citing Use of Products

View All Opioid Receptor Isoform Specific Products:

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.

IC50 & Target

κ Opioid Receptor/KOR

 

In Vitro

Norbinaltorphimine reversibly antagonize the effects of κ agonists with pA2 values of 10.2-10.4. Norbinaltorphimine is much less potent as an antagonist at μ and δ receptors, pA2 values are 7.4-7.6 and 7.6-7.8, respectively[1].

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

Norbinaltorphimine dihydrochloride Related Antibodies
In Vivo

Norbinaltorphimine has weak and inconsistent effects on THC-induced taste avoidance in adolescent rats in that Norbinaltorphimine both attenuates and strengthens taste avoidance dependent on dose and trial. Norbinaltorphimine has limited impact on the final one-bottle avoidance and no effects on the two-bottle preference test. Interestingly, Norbinaltorphimine has no effect on THC-induced taste avoidance in adult rats as well[2]. Norbinaltorphimine pretreatment significantly attenuates stress-induced reinstatement of nicotine-CPP, but has no effect on nicotine-primed reinstatement[3].

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

734.71

Formula

C40H45Cl2N3O6
CAS No.
Appearance

Solid

Color

Light yellow to gray

SMILES

O[C@]12[C@]34[C@](OC5=C(O)C=CC(C[C@@]2([H])N(CC6CC6)CC4)=C35)([H])C7=C(C8=C([C@@](O9)([H])[C@]%10%11[C@](O)([C@](CC%12=C%11C9=C(C=C%12)O)([H])N(CC%13CC%13)CC%10)C8)N7)C1.Cl[H].Cl[H]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (136.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 33.33 mg/mL (45.36 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3611 mL 6.8054 mL 13.6108 mL
5 mM 0.2722 mL 1.3611 mL 2.7222 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 (sealed storage, away from moisture). 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
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (3.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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 (3.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 98.17%

SDS (252 KB)

COA (257 KB) HNMR (158 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[2][3]

Rats[2]

Norbinaltorphimine is dissolved in sterile H2O at a concentration of 15 mg/mL and administered subcutaneously (SC) at a dose of 15 mg/kg. Male Sprague Dawley rats are ranked according to average water consumption on all habituation cycles and assigned to one of two groups [Norbinaltorphimine (n=42) and Vehicle (n=42)], such that mean water intake is comparable among groups. On PND 34 (approximately 24 h prior to conditioning, see below), subjects assigned to the Norbinaltorphimine group are injected with Norbinaltorphimine (15 mg/kg) and subjects assigned to the Vehicle group are injected with the Norbinaltorphimine vehicle at an equal volume[2].

Mice[3]

Mice are conditioned with 0.5 mg/kg nicotine, injected subcutaneously (s.c.) for 3 days and tested in the nicotine-conditioned place preference (CPP) model. After 3 days extinction, Norbinaltorphimine (10 mg/kg, s.c.) is administered 16 h prior to a priming dose of nicotine (0.1 mg/kg, s.c.), and mice are tested in the CPP model for nicotine-induced reinstatement of CPP. A separate group of mice is subjected to a 2-day modified forced swim test (FST) paradigm to induce stress after 3 days extinction from CPP. Mice are given vehicle or Norbinaltorphimine (10 mg/kg, s.c.) 16 h prior to each FST session[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 (sealed storage, away from moisture). 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 1.3611 mL 6.8054 mL 13.6108 mL 34.0270 mL
5 mM 0.2722 mL 1.3611 mL 2.7222 mL 6.8054 mL
10 mM 0.1361 mL 0.6805 mL 1.3611 mL 3.4027 mL
15 mM 0.0907 mL 0.4537 mL 0.9074 mL 2.2685 mL
20 mM 0.0681 mL 0.3403 mL 0.6805 mL 1.7014 mL
25 mM 0.0544 mL 0.2722 mL 0.5444 mL 1.3611 mL
30 mM 0.0454 mL 0.2268 mL 0.4537 mL 1.1342 mL
40 mM 0.0340 mL 0.1701 mL 0.3403 mL 0.8507 mL
DMSO 50 mM 0.0272 mL 0.1361 mL 0.2722 mL 0.6805 mL
60 mM 0.0227 mL 0.1134 mL 0.2268 mL 0.5671 mL
80 mM 0.0170 mL 0.0851 mL 0.1701 mL 0.4253 mL
100 mM 0.0136 mL 0.0681 mL 0.1361 mL 0.3403 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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Norbinaltorphimine dihydrochloride Related Classifications

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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.

Keywords:

Norbinaltorphimine113158-34-2nor-Binaltorphiminenor-BNIOpioid ReceptorInhibitorinhibitorinhibit

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