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: 98.91%
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Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain.

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Norbinaltorphimine dihydrochloride

Norbinaltorphimine dihydrochloride Chemical Structure

CAS No. : 113158-34-2

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Based on 7 publication(s) in Google Scholar

Other Forms of Norbinaltorphimine dihydrochloride:

Norbinaltorphimine dihydrochloride Related Antibodies

Top Publications Citing Use of Products

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

  • Biological Activity

  • Purity & Documentation

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Description

Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain[1][2][3].

IC50 & Target

κ Opioid Receptor/KOR

 

In Vitro

Norbinaltorphimine (0.01 nM-0.1 μM; 120 min) dihydrochloride displaces the binding of [3H]U-69,593 to κ-opioid receptors in rat cortical cell membranes. Its Ki value is 4.8 nM in saline-infused rats, while its potency increases 12-fold (Ki = 0.4 nM) in butorphanol-infused rats, indicating that κ-opioid receptors are hypersensitive to this antagonist[2].
Norbinaltorphimine (20-200 nM; 30 min) dihydrochloride potently antagonizes κ-selective agonists in the longitudinal muscle of guinea pig ileum, while it exhibits extremely weak antagonistic effects on the μ-selective agonist morphine, with a κ/μ selectivity ratio of 19.2[3].
Norbinaltorphimine (20 nM; 30 min) dihydrochloride potently antagonizes κ-selective agonists in rabbit vas deferens preparations[3].

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

Norbinaltorphimine dihydrochloride Related Antibodies
In Vivo

Norbinaltorphimine (30 μg; intracerebroventricular injection; single administration / twice daily; consecutive 10 days) dihydrochloride acts as a selective, long-acting κ-opioid receptor antagonist in rats[1].
Norbinaltorphimine (12-100 nM/5 μl; intracerebroventricular injection; administered twice, at 3 hours before and 48 hours after the initiation of butorphanol infusion) dihydrochloride blocks most naloxone-precipitated withdrawal symptoms in butorphanol-dependent rats, exerts a significant blocking effect on diarrhea, alleviates forepaw tremor, and prevents butorphanol-induced desensitization of κ-opioid receptors in the cortex and striatum, as well as receptor downregulation in the cortex[2].

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

Animal Model: Sprague-Dawley (male, 250-270 g)[1]
Dosage: 30 μg (single treatment); 30 μg (repeated treatment)
Administration: i.c.v.; single injection (single treatment); i.c.v.; twice daily; 10 days (repeated treatment)
Result: Abolished U69593-induced antinociception (significant reduction in % MPE vs vehicle) when tested 1, 11, and 30 days post-single 30 μg i.c.v. injection.
Did not alter DAMGO- or DPDPE-induced antinociception when tested 1 and 11 days post-single 30 μg i.c.v. injection.
Abolished U69593-induced antinociception (significant reduction in % MPE vs vehicle) when tested 1, 2, 5, and 20 days post-last repeated 30 μg i.c.v. twice-daily injection.
Abolished DAMGO- and DPDPE-induced antinociception (significant reduction in % MPE vs vehicle) when tested 1 and 2 days post-last repeated 30 μg i.c.v. twice-daily injection.
Showed no effect on DAMGO- or DPDPE-induced antinociception at 5 and 20 days post-last repeated 30 μg i.c.v. twice-daily injection.
Exhibited magnitude of DAMGO and DPDPE antagonism on day 1 post-last repeated dose equivalent to that of selective μ-antagonist CTOP and δ-antagonist ICI 174,864, respectively.
Animal Model: Sprague-Dawley (7- to 8-week-old male, 250-300 g, butorphanol dependence model via intracerebroventricular osmotic minipump infusion of butorphanol tartrate at 26 nmol/h for 3 days)[2]
Dosage: 12 nM/5 μl per rat; 24 nM/5 μl per rat; 48 nM/5 μl per rat; 100 nM/5 μl per rat
Administration: i.c.v.; 2 doses (3 h before and 48 h after butorphanol infusion start)
Result: Completely blocked naloxone-precipitated withdrawal signs of escape behavior, teeth-chattering, wet shakes, ptosis, body weight loss (>3%), and reversed hypothermia to increased rectal temperatures.
Significantly blocked diarrhea at 12 nM dose.
Significantly blocked diarrhea and attenuated forepaw tremors at 24 nM dose.
Had no effect on withdrawal signs of yawning, ejaculation, or urination.
Prevented butorphanol-induced increases in [3H]U-69,593 K_D values in the cortex (4.33 nM, 96% of saline control) and striatum (5.49 nM, 105% of saline control) at 12 nmol dose.
Prevented butorphanol-induced decreases in [3H]U-69,593 B_max values in the cortex (59.46 fM/mg protein, 97% of saline control) at 12 nmol dose.
Prevented butorphanol-induced supersensitivity of cortical κ-opioid receptors to Norbinaltorphimine itself, blocking the significant reduction in K_i values seen with butorphanol alone.
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.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (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:

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(per animal)

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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
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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    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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