Cat. No.: HY-117040

nor-Binaltorphimine

(Synonyms: Norbinaltorphimine; NorBNI)

8 Cited Publications

Customer Review

Based on 8 publication(s) in Google Scholar

nor-Binaltorphimine (Norbinaltorphimine; NorBNI) is a selective, long-acting competitive antagonist of the κ-opioid receptor. nor-Binaltorphimine blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. nor-Binaltorphimine 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. nor-Binaltorphimine is applicable to research related to neurological disorders such as pain.

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

Purity: 99.27%
CAS No.: 105618-26-6
Formula: C₄₀H₄₃N₃O₆
Molecular Weight:661.79

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

nor-Binaltorphimine Chemical Structure

CAS No.: 105618-26-6

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

κ Opioid Receptor/KOR

All Opioid Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.039 K_e/nM Compound: nor BNI	Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells. Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells.	[PMID: 12672258]
CHO	EC₅₀	120 nM Compound: 1, norBNI	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 20568781]
CHO	EC₅₀	18.9 K_e/nM Compound: nor BNI	Stimulation of DAMGO binding in recombinant human Opioid receptor mu 1 transfected into CHO cells Stimulation of DAMGO binding in recombinant human Opioid receptor mu 1 transfected into CHO cells	[PMID: 12672258]
CHO	EC₅₀	380 nM Compound: 1, norBNI	Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 20568781]
CHO	EC₅₀	4.42 K_e/nM Compound: nor BNI	Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells. Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.	[PMID: 12672258]
CHO	EC₅₀	6 nM Compound: 1, norBNI	Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 20568781]
CHO	IC₅₀	0.28 nM Compound: norBNI	Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	[PMID: 25593096]
CHO	IC₅₀	2.9 nM Compound: norBNI	Antagonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of U50,488H-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis Antagonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of U50,488H-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis	[PMID: 27556704]
CHO	IC₅₀	4.6 nM Compound: norBNI	Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cells assessed as inhibition of U69,593-induced ERK phosphorylation pre-incubated with compound before U69,593 stimulation for 10 mins Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cells assessed as inhibition of U69,593-induced ERK phosphorylation pre-incubated with compound before U69,593 stimulation for 10 mins	[PMID: 25593096]
HEK293	EC₅₀	158 nM Compound: NorBNI	Increase of JNK phosphorylation in U50488 treated HEK293 cells expressing GFP tagged kappa opioid receptor Increase of JNK phosphorylation in U50488 treated HEK293 cells expressing GFP tagged kappa opioid receptor	[PMID: 17702750]
HEK293	IC₅₀	2.1 nM Compound: nor-BNI 1	Antagonist activity at human kappa opioid receptor expressed in HEK cells assessed as inhibition of dynorphin A-induced [35S]GTPgammaS binding Antagonist activity at human kappa opioid receptor expressed in HEK cells assessed as inhibition of dynorphin A-induced [35S]GTPgammaS binding	[PMID: 20719509]
HEK293	IC₅₀	212 nM Compound: nor-BNI 1	Antagonist activity at human mu opioid receptor expressed in HEK cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding Antagonist activity at human mu opioid receptor expressed in HEK cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding	[PMID: 20719509]
HEK293	IC₅₀	24 nM Compound: nor-BNI 1	Antagonist activity at human delta opioid receptor expressed in HEK cells assessed as inhibition of SNC-80-induced [35S]GTPgammaS binding Antagonist activity at human delta opioid receptor expressed in HEK cells assessed as inhibition of SNC-80-induced [35S]GTPgammaS binding	[PMID: 20719509]
U2OS	IC₅₀	2.5 nM Compound: norBNI	Antagonist activity against human kappa opioid receptor expressed in human U2OS cells co-expressing beta-arrestin2 pre-treated for 15 mins before U69,593 stimulation for 90 mins by DiscoveRx beta-arrestin2 recruitment based PathHunter assay Antagonist activity against human kappa opioid receptor expressed in human U2OS cells co-expressing beta-arrestin2 pre-treated for 15 mins before U69,593 stimulation for 90 mins by DiscoveRx beta-arrestin2 recruitment based PathHunter assay	[PMID: 25593096]

In Vitro

Nor-binaltorphimine (0.01 nM-0.1 μM; 120 min) displaces the binding of [³H]U-69,593 to κ-opioid receptors in rat cortical cell membranes. Its K_i value is 4.8 nM in saline-infused rats, while its potency increases 12-fold (K_i = 0.4 nM) in butorphanol-infused rats, indicating that κ-opioid receptors are hypersensitive to this antagonist^[2].
nor-Binaltorphimine (20-200 nM; 30 min) 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].
nor-Binaltorphimine (20 nM; 30 min) 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.

In Vivo

Nor-binaltorphimine (30 μg; intracerebroventricular injection; single administration / twice daily; consecutive 10 days) acts as a selective, long-acting κ-opioid receptor antagonist in rats^[1].
Nor-binaltorphimine (12-100 nM/5 μl; intracerebroventricular injection; administered twice, at 3 hours before and 48 hours after the initiation of butorphanol infusion) 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 nor-binaltorphimine itself, blocking the significant reduction in K_i values seen with butorphanol alone.

Chemical Information

CAS No. 105618-26-6
Appearance Solid
Molecular Weight 661.79
Formula C₄₀H₄₃N₃O₆
Color White to light yellow
SMILES

O[C@]12[C@]34[C@](OC5=C(O)C=CC(C[C@@]2([H])N(CC4)CC6CC6)=C53)([H])C7=C(C8=C([C@@]9([H])[C@]%10%11[C@@](C8)([C@](CC%12=C%11C(O9)=C(C=C%12)O)([H])N(CC%10)CC%13CC%13)O)N7)C1
Synonyms

Norbinaltorphimine; NorBNI
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (8)

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Journal Impact Factor

Br J Anaesth

Kappa opioid receptor internalisation-induced p38 nuclear translocation suppresses glioma progression. [Abstract]

2025 Mar;134(3):759-771. PMID: 39741108
J Med Chem

2026 Mar 5;69(6):6508-6527.
J Med Chem

Systematic Structure-Activity Relationship Study of Nalfurafine Analogues toward Development of Potentially Nonaddictive Pain Management Treatments. [Abstract]

2024 Jun 13;67(11):9552-9574. PMID: 38814086
Front Immunol

Butorphanol Promotes Macrophage Phenotypic Transition to Inhibit Inflammatory Lung Injury via κ Receptors. [Abstract]

2021 Jul 7:12:692286. PMID: 34305926
Front Cell Neurosci

The Basolateral Amygdala to Ventral Hippocampus Circuit Controls Anxiety-Like Behaviors Induced by Morphine Withdrawal. [Abstract]

2022 Jun 2;16:894886. PMID: 35726232
Prog Neuropsychopharmacol Biol Psychiatry

A dorsolateral BNST-parabrachial nucleus pathway regulates adolescent alcohol-induced negative affect in females. [Abstract]

2026 Jun 20:147:111760. PMID: 42214652
Pharmacol Biochem Behav

Dual activation of 5-HT1A and μ-opioid receptors mediates dezocine's antidepressant effects in mice with comorbid pain and depression. [Abstract]

2026 Feb:259:174136. PMID: 41365431
Aging (Albany NY)

κ-opioid receptor stimulation alleviates rat vascular smooth muscle cell calcification via PFKFB3-lactate signaling. [Abstract]

2021 May 20;13(10):14355-14371. PMID: 34016793

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (151.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 33.08 mg/mL (49.99 mM; Need ultrasonic and warming)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5111 mL

7.5553 mL

15.1105 mL

5 mM

0.3022 mL

1.5111 mL

3.0221 mL

10 mM

0.1511 mL

0.7555 mL

1.5111 mL

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.

Molarity Calculator

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

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Spanagel R, et al. Evidence that nor-binaltorphimine can function as an antagonist at multiple opioid receptor subtypes. Eur J Pharmacol. 1994;264(2):157-162. [Content Brief]

[2]. Jaw SP, et al. Effects of nor-binaltorphimine on butorphanol dependence. Eur J Pharmacol. 1993;239(1-3):133-140. [Content Brief]

[3]. Portoghese PS, et al. Binaltorphimine and nor-binaltorphimine, potent and selective kappa-opioid receptor antagonists. Life Sci. 1987 Mar 30;40(13):1287-92. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.5111 mL	7.5553 mL	15.1105 mL	37.7763 mL
	5 mM	0.3022 mL	1.5111 mL	3.0221 mL	7.5553 mL
	10 mM	0.1511 mL	0.7555 mL	1.5111 mL	3.7776 mL
	15 mM	0.1007 mL	0.5037 mL	1.0074 mL	2.5184 mL
	20 mM	0.0756 mL	0.3778 mL	0.7555 mL	1.8888 mL
	25 mM	0.0604 mL	0.3022 mL	0.6044 mL	1.5111 mL
	30 mM	0.0504 mL	0.2518 mL	0.5037 mL	1.2592 mL
	40 mM	0.0378 mL	0.1889 mL	0.3778 mL	0.9444 mL
DMSO	50 mM	0.0302 mL	0.1511 mL	0.3022 mL	0.7555 mL
	60 mM	0.0252 mL	0.1259 mL	0.2518 mL	0.6296 mL
	80 mM	0.0189 mL	0.0944 mL	0.1889 mL	0.4722 mL
	100 mM	0.0151 mL	0.0756 mL	0.1511 mL	0.3778 mL

Keywords

nor-Binaltorphimine

8 Cited Publications

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nor-Binaltorphimine

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Neurotransmitter Receptor Compound Library

Anti-Obesity Compound Library

Protein-protein Interaction Inhibitor Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

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MCE Bioactive Compound Library

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Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) nor-Binaltorphimine

All Opioid Receptor Isoforms

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

nor-Binaltorphimine

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Neurotransmitter Receptor Compound Library

Anti-Obesity Compound Library

Protein-protein Interaction Inhibitor Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) nor-Binaltorphimine

All Opioid Receptor Isoforms

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

nor-Binaltorphimine Related Classifications

HY-117040 Related Classifications