nor-Binaltorphimine dihydrochloride

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Cat.No. 0347 - nor-Binaltorphimine dihydrochloride | C40H43N3O6.2HCl | CAS No. 113158-34-2
Description: Standard κ selective antagonist
Alternative Names: nor-BNI, Norbinaltorphimine
Chemical Name: 17,17'-(Dicyclopropylmethyl)-6,6',7,7'-6,6'-imino- 7,7'-binorphinan-3,4',14,14'-tetrol dihydrochloride
Purity: ≥98% (HPLC)
Citations (21)

Biological Activity

A selective κ-opioid receptor antagonist.

Licensing Information

Sold with the permission of the University of Minnesota

Compound Libraries

nor-Binaltorphimine dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 734.72
Formula C40H43N3O6.2HCl
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 113158-34-2
PubChem ID 11957626
Smiles OC1=CC=C2C([C@]34CCN5CC6CC6)=C1O[C@H]4C%11=C(C7=C(N%11)[C@H]%10[C@@]8(CC%13)[C@@]([C@H](N%13CC%12CC%12)CC9=C8C(O%10)=C(O)C=C9)(O)C7)C[C@@]3(O)[C@H]5C2.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 18.37 25
water 18.37 25mM with gentle warming
phosphate buffered saline 36.74 50mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 734.72. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.36 mL 6.81 mL 13.61 mL
5 mM 0.27 mL 1.36 mL 2.72 mL
10 mM 0.14 mL 0.68 mL 1.36 mL
50 mM 0.03 mL 0.14 mL 0.27 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet


References are publications that support the products' biological activity.

Blake et al (1997) Differential agonist regulation of the human κ-opioid receptor. J.Neurochem. 68 1846 PMID: 9109509

Feng et al (1997) Nor-binaltorphimine precipitates withdrawal and excitatory amino acid release in the locus ceruleus of butorphanol- but not morphine-dependent rats. J.Pharmacol.Exp.Ther. 283 932 PMID: 9353416

Portoghese et al (1994) Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17'-basic group in the interaction with a putative address subsite on the κ opioid receptor. J.Med.Chem. 37 1495 PMID: 8182708

If you know of a relevant reference for nor-Binaltorphimine dihydrochloride, please let us know.

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View all κ Opioid Receptor Antagonists

Keywords: nor-Binaltorphimine dihydrochloride, supplier, selective, antagonists, κ-opioid, kappa-opioid, KOP, Receptors, OP2, nor-BNI, Norbinaltorphimine, Kappa, Opioid, Receptors, Kappa, Opioid, Receptors, Tocris Bioscience

21 Citations for nor-Binaltorphimine dihydrochloride

Citations are publications that use Tocris products. Selected citations for nor-Binaltorphimine dihydrochloride include:

Kuzumaki et al (2012) Effect of κ-opioid receptor agonist on the growth of non-small cell lung cancer (NSCLC) cells. Neuropsychopharmacology 106 1148 PMID: 22343623

Grachev et al (2012) GPR54-dependent stimulation of luteinizing hormone secretion by neurokinin B in prepubertal rats. Neuropsychopharmacology 7 e44344 PMID: 23028524

Russell-Randall and Dortch-Carnes (2011) κ opioid receptor localization and coupling to nitric oxide production in cells of the anterior chamber. J Biomed Sci 52 5233 PMID: 21666232

Jones et al (2010) Identification of a κ-opioid agonist as a potent and selective lead for drug development against human African trypanosomiasis. Biochem Pharmacol 80 1478 PMID: 20696141

Polter (2017) Constitutive activation of kappa opioid receptors at ventral tegmental area inhibitory synapsesfollowing acute stress. Elife 6 e23785 PMID: 28402252

Ruiz-Pino et al (2015) Effects and interactions of tachykinins and dynorphin on FSH and LH secretion in developing and adult rats. Endocrinology 156 576 PMID: 25490143

Lee and Ko (2015) Distinct functions of opioid-related peptides and gastrin-releasing peptide in regulating itch and pain in the spinal cord of primates. Neuropsychopharmacology 5 11676 PMID: 26119696

Chen et al (2015) Effect of adenoviral delivery of prodynorphin gene on experimental inflammatory pain induced by formalin in rats. PLoS One 7 4877 PMID: 25663984

Chen et al (2015) Berberine Improves Intestinal Motility and Visceral Pain in the Mouse Models Mimicking Diarrhea-Predominant Irritable Bowel Syndrome (IBS-D) Symptoms in an Opioid-Receptor Dependent Manner. Sci Rep 10 e0145556 PMID: 26700862

Yi et al (2015) Low-frequency electroacupuncture suppresses focal epilepsy and improves epilepsy-induced sleep disruptions. Appl Environ Microbiol 22 49 PMID: 26150021

García-Fuster et al (2007) Effects of opiate drugs on Fas-associated protein with death domain (FADD) and effector caspases in the rat brain: regulation by the ERK1/2 MAP kinase pathway. Int J Clin Exp Med 32 399 PMID: 16482086

Ma et al (2014) Methamphetamine induces autophagy as a pro-survival response against apoptotic endothelial cell death through the Kappa opioid receptor. Cell Death Dis 5 e1099 PMID: 24603327

Schmid et al (2013) Functional selectivity of 6'-guanidinonaltrindole (6'-GNTI) at κ-opioid receptors in striatal neurons. J Biol Chem 288 22387 PMID: 23775075

Kuzmin et al (2013) Upregulated dynorphin opioid peptides mediate alcohol-induced learning and memory impairment. Transl Psychiatry 3 e310 PMID: 24105441

Tejeda et al (2013) Prefrontal cortical kappa-opioid receptor modulation of local neurotransmission and conditioned place aversion. Neuropsychopharmacology 38 1770 PMID: 23542927

Romero-Picó et al (2013) Hypothalamic κ-opioid receptor modulates the orexigenic effect of ghrelin. Br J Cancer 38 1296 PMID: 23348063

Rogala et al (2012) Effects of a post-shock injection of the kappa opioid receptor antagonist norbinaltorphimine (norBNI) on fear and anxiety in rats. PLoS One 7 e49669 PMID: 23166745

Guida et al (2012) Salvinorin A reduces mechanical allodynia and spinal neuronal hyperexcitability induced by peripheral formalin injection. Mol Pain 8 60 PMID: 22913292

Carr et al (2010) Antidepressant-like effects of κ-opioid receptor antagonists in Wistar Kyoto rats. Invest Ophthalmol Vis Sci 35 752 PMID: 19924112

Cheng et al (2009) Endogenous opiates in the nucleus tractus solitarius mediate electroacupuncture-induced sleep activities in rats. PLoS One 2011 159209 PMID: 19729491

Land et al (2008) The dysphoric component of stress is encoded by activation of the dynorphin kappa-opioid system. J Neurosci 28 407 PMID: 18184783

Do you know of a great paper that uses nor-Binaltorphimine dihydrochloride from Tocris? If so please let us know.

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