Norbinaltorphimine dihydrochloride

SKU: orb1709016

Description

Norbinaltorphimine dihydrochloride is a selective, potent κ-opioid receptor (KOR) antagonist. It is widely used in neuroscience research to study KOR function, notably for inducing and investigating itch-related behaviors in murine models, as well as in vitro receptor binding assays.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 113158-34-2
• MW: 734.71
• Purity: ≥98% (May vary between batches)
• Formula: C₄₀H₄₅Cl₂N₃O₆
• SMILES: Cl.Cl.[H][C@@]12Oc3c4c(C[C@@]5([H])N(CC6CC6)CC[C@@]14[C@@]5(O)Cc1c4C[C@@]5(O)[C@@]6([H])Cc7ccc(O)c8O[C@@]([H])(c4[nH]c21)[C@]5(CCN6CC1CC1)c78)ccc3O
• Target: Opioid Receptor
• Solubility: H2O:20 mg/mL (27.22 mM);DMSO:80 mg/mL (108.89 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (4.49 mM)

Bioactivity

• In Vivo:
  In adolescent rats, Norbinaltorphimine dihydrochloride exhibits weak and inconsistent effects on THC-induced taste avoidance. Notably, the impact of Norbinaltorphimine dihydrochloride varies based on dose and trial, as it both attenuates and strengthens taste avoidance. However, these effects are limited, with no significant influence on the final one-bottle avoidance and no observable effects on the two-bottle preference test. Interestingly, Norbinaltorphimine dihydrochloride demonstrates no effect on THC-induced taste avoidance in adult rats as well.Furthermore, when administered as a pretreatment,Norbinaltorphimine dihydrochloride significantly attenuates stress-induced reinstatement of nicotine-conditioned place preference (CPP). However, it is important to note that Norbinaltorphimine dihydrochloride has no discernible effect on nicotine-primed reinstatement.
• In Vitro:
  Norbinaltorphimine dihydrochloride reversibly antagonizes the effects of κ agonists with pA2 values ranging from 10.2 to 10.4. However, it is important to note that Norbinaltorphimine dihydrochloride is much less potent as an antagonist at μ and δ receptors, where the pA2 values are 7.4-7.6 and 7.6-7.8, respectively.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Norbinaltorphimine, nor-Binaltorphimine, Norbinaltorphimine dihydrochloride, Norbinaltorphimine Dihydrochloride, nor-Binaltorphimine Dihydrochloride, nor-Binaltorphimine dihydrochloride, Nor-Binaltorphimine dihydrochloride, nor-BNI, nor-BNI Dihydrochloride, nor-BNI dihydrochloride, Nor-BNI dihydrochloride, Opioid Receptor, OpioidReceptor, κ opioid receptor

Compound Identifiers

PubChem CID

11957626