nor-Binaltorphimine dihydrochloride (Synonyms: nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) |
| رقم الكتالوجGC13645 |
نور-بينالتورفيمين ثنائي هيدروكلوريد هو مضاد قوي وانتقائي لمستقبلات الأفيون.
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Cas No.: 113158-34-2
Sample solution is provided at 25 µL, 10mM.
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nor-Binaltorphimine dihydrochloride is a potent and selective κ opioid receptor (KOR) antagonist[1]. nor-Binaltorphimine dihydrochloride can block the binding of endogenous ligands to KOR, thereby regulating pain perception, emotions and addictive behaviors[2, 3]. nor-Binaltorphimine dihydrochloride can reduce morphine withdrawal symptoms and the resulting conditioned place aversion in rats[4].
In vitro, treatment of rat pheochromocytoma cell line PC12 cells with nor-Binaltorphimine dihydrochloride (100nM) for 10min reversed the inhibitory effect of U-69593 (κ-opioid receptor agonist) on nicotine-induced increase in tyrosine hydroxylase (TH) enzyme activity and TH mRNA level[5].
In vivo, nor-Binaltorphimine dihydrochloride (2mg/kg) was intraperitoneally injected into hyperlipidemia model mice, blocking the normalizing effect of U50488H on mouse endothelial ultrastructure and function, inhibiting U50488H-induced increase in Akt/eNOS phosphorylation, increase in serum/medium NO levels and enhancement of eNOS activity, and also blocking the inhibitory effect of U50488H on iNOS activity[6].
References:
[1] Schmidhammer H, Erli F, Guerrieri E, et al. Development of diphenethylamines as selective kappa opioid receptor ligands and their pharmacological activities[J]. Molecules, 2020, 25(21): 5092.
[2] Ji M J, Yang J, Gao Z Q, et al. The role of the kappa opioid system in comorbid pain and psychiatric disorders: function and implications[J]. Frontiers in Neuroscience, 2021, 15: 642493.
[3] Kishioka S, Kiguchi N, Kobayashi Y, et al. Pharmacokinetic evidence for the long-lasting effect of nor-binaltorphimine, a potent kappa opioid receptor antagonist, in mice[J]. Neuroscience letters, 2013, 552: 98-102.
[4] Kaski S W, White A N, Gross J D, et al. Potential for kappa-opioid receptor agonists to engineer nonaddictive analgesics: a narrative review[J]. Anesthesia & Analgesia, 2021, 132(2): 406-419.
[5] Takekoshi K, Ishii K, Kawakami Y, et al. κ-Opioid inhibits catecholamine biosynthesis in PC12 rat pheochromocytoma cell[J]. FEBS letters, 2000, 477(3): 273-277.
[6] Tian F, Zheng X Y, Li J, et al. κ-Opioid receptor stimulation improves endothelial function via Akt-stimulated NO production in hyperlipidemic rats[J]. Scientific reports, 2016, 6(1): 26807.
| Cell experiment [1]: | |
Cell lines | PC12 cells |
Preparation Method | Experiments were initiated by replacing the medium with HEPES-buffered Krebs buffer containing various concentrations (10nM–1μM) of U-69593 or U-69593 (1μM) in the presence of nor-Binaltorphimine dihydrochloride (100nM), and the cells were incubated at 37°C for 10min. Then, cells were homogenized in 0.25M sucrose (50 volumes) using a glass tissue grinder, measurement of tyrosine hydroxylase (TH, a rate-limiting enzyme in biosynthesis of catecholamine) enzyme activity. |
Reaction Conditions | 100nM; 10min |
Applications | Nor-Binaltorphimine dihydrochloride reverses the inhibitory effect of U-69593 (a κ-opioid receptor agonist) on nicotine-induced increases in tyrosine hydroxylase (TH) enzyme activity. |
| Animal experiment [2]: | |
Animal models | Sprague Dawley rats |
Preparation Method | Sixty male 8-weekold Sprague Dawley rats were randomly divided into six groups: normal diet group (ND), high-fat diet group (HFD), high-fat diet+saline group (HFD+V) (0.3mL saline was intraperitoneally (i.p.) injected every 2 days), high-fat diet+U50488H group (HFD+U) (1.25mg/kg U50488H was i.p. injected every other day), high-fat diet+nor-Binaltorphimine dihydrochloride group (HFD+N) (2.0mg/kg nor-Binaltorphimine dihydrochloride, was i.p. injected every other day), high-fat diet+U50488H+nor-BNI group (HFD+U+N) (2.0mg/kg nor-Binaltorphimine dihydrochloride was i.p. injected and 1.25mg/kg U50488H was i.p. injected 10min later every other day). ND group received a regular chow diet and all other groups received a high-fat (5% cholesterol supplemented) diet. |
Dosage form | 2mg/kg; i.p. |
Applications | Nor-Binaltorphimine dihydrochloride blocked the normalizing effects of U50488H on endothelial ultrastructure and function under hyperlipidemic conditions. nor-Binaltorphimine dihydrochloride inhibited the U50488H-induced increase in Akt/eNOS phosphorylation, serum/medium NO levels, and enhanced eNOS activity. In addition, nor-Binaltorphimine dihydrochloride blocked the inhibitory effect of U50488H on iNOS activity. |
References: | |
| Cas No. | 113158-34-2 | SDF | |
| المرادفات | nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride | ||
| Chemical Name | (4bS,8R,8aS,10aS,11R,14aS,19aR,20bR)-7,12-bis(cyclopropylmethyl)-6,7,8,8a,9,10,10a,11,12,13,14,19a,20,20b-tetradecahydro-5H-4,8:11,15-dimethanodibenzofuro[2,3-a:3',2'-i]dipyrido[4,3-b:3',4'-h]carbazole-1,8a,10a,18-tetraol dihydrochloride | ||
| Canonical SMILES | OC1=C(O2)C3=C(C[C@]4([H])[C@]5(O)CC(C(C[C@@]6(O)[C@@]7([H])CC8=C9C(O%10)=C(O)C=C8)=C%11[C@@]%10([H])[C@@]69CCN7CC%12CC%12)=C(N%11)[C@@]2([H])[C@]35CCN4CC%13CC%13)C=C1.Cl.Cl | ||
| Formula | C40H43N3O6.2HCl | M.Wt | 734.72 |
| الذوبان | <18.37mg/ml in Water; <18.37mg/ml in DMSO | Storage | 4°C, sealed storage, away from moisture |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.3611 mL | 6.8053 mL | 13.6106 mL |
| 5 mM | 0.2722 mL | 1.3611 mL | 2.7221 mL |
| 10 mM | 0.1361 mL | 0.6805 mL | 1.3611 mL |
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- Purity: >98.00%
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