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

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

Cat. No.: HY-100903 Purity: 98.60%
Handling Instructions

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

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Description

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

IC50 & Target

κ opioid receptor[1]

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].

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].

Molecular Weight

734.71

Formula

C₄₀H₄₅Cl₂N₃O₆

CAS No.

113158-34-2

SMILES

O[[email protected]]12[[email protected]]34[[email protected]](OC5=C(O)C=CC(C[[email protected]@]2([H])N(CC6CC6)CC4)=C35)([H])C7=C(C8=C([[email protected]@](O9)([H])[[email protected]]%10%11[[email protected]](O)([[email protected]](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
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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

Purity: 98.60%

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Keywords:

Norbinaltorphiminenor-Binaltorphiminenor-BNIOpioid ReceptorInhibitorinhibitorinhibit

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