nor-Binaltorphimine dihydrochloride

Discontinued Product

nor-Binaltorphimine dihydrochloride (Cat. No. 0347) has been withdrawn from sale for commercial reasons.
Description: Selective κ 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 (30)
Reviews (3)
Literature (2)

Biological Activity for nor-Binaltorphimine dihydrochloride

nor-Binaltorphimine dihydrochloride is a selective κ-opioid receptor antagonist.

Licensing Information

Sold with the permission of the University of Minnesota

Technical Data for nor-Binaltorphimine dihydrochloride

M. Wt 734.72
Formula C40H43N3O6.2HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 113158-34-2
PubChem ID 11957626
Smiles Cl.Cl.OC1=CC=C2C[C@H]3N(CC4CC4)CC[C@@]45[C@@H](OC1=C24)C1=C(C[C@@]35O)C2=C(N1)[C@@H]1OC3=C(O)C=CC4=C3[C@@]11CCN(CC3CC3)[C@H](C4)[C@]1(O)C2

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Product Datasheets for nor-Binaltorphimine dihydrochloride

Certificate of Analysis / Product Datasheet
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References for nor-Binaltorphimine dihydrochloride

References are publications that support the biological activity of the product.

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

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Keywords: nor-Binaltorphimine dihydrochloride, nor-Binaltorphimine dihydrochloride supplier, selective, antagonists, κ-opioid, kappa-opioid, KOP, Receptors, OP2, nor-BNI, Norbinaltorphimine, Kappa, Opioid, 0347, Tocris Bioscience

30 Citations for nor-Binaltorphimine dihydrochloride

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

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

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

Smith et al (2016) Endogenous central amygdala mu-opioid receptor signaling promotes sodium appetite in mice. Proc Natl Acad Sci U S A 113 13893 PMID: 27849613

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

Morse et al (2013) Label-free integrative pharmacology on-target of opioid ligands at the opioid receptor family. BMC Pharmacol Toxicol 14 17 PMID: 23497702

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

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

Braida et al (2009) Potential anxiolytic- and antidepressant-like effects of salvinorin A, the main active ingredient of Salvia divinorum, in rodents. Br J Pharmacol 157 844 PMID: 19422370

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

Gross et al (2010) Evidence for a role of opioids in epoxyeicosatrienoic acid-induced cardioprotection in rat hearts. Am J Physiol Heart Circ Physiol 298 H2201 PMID: 20400686

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

Norris et al (2019) The Bivalent Rewarding and Aversive properties of δ9-tetrahydrocannabinol are Mediated Through Dissociable Opioid Receptor Substrates and Neuronal Modulation Mechanisms in Distinct Striatal Sub-Regions. Sci Rep 9 9760 PMID: 31278333

Pina et al (2020) The kappa opioid receptor modulates GABA neuron excitability and synaptic transmission in midbrain-projections from the insular cortex. Neuropharmacology 165 107831 PMID: 31870854

Telpoukhovskaia et al (2020) Discovery of small molecules that normalize the transcriptome and enhance cysteine cathepsin activity in progranulin-deficient microglia. Sci Rep 10

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

Morse et al (2011) Ligand-directed functional selectivity at the mu opioid receptor revealed by label-free integrative pharmacology on-target. PLoS One 6 e25643 PMID: 22003401

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

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

Dai et al (2018) Selective blockade of spinal D2DR by levo-corydalmine attenuates MOR tolerance via suppressing PI3K/Akt-MAPK signaling in a MOR-dependent manner. Exp Mol Med 50 148 PMID: 30429454

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

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

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

Reviews for nor-Binaltorphimine dihydrochloride

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JNK-dependent rescue of LTPGABA by acute norBNI.
By Anonymous on 03/18/2020
Assay Type: In Vivo
Species: Rat
Cell Line/Tissue: brain


PMID: 28402252
review image

Reliable compound.
By Anonymous on 11/25/2019
Assay Type: In Vitro
Species: Human

Successfully stopped selective agonist-induced ERK phosphorylation in CHO cells. It’s a very reliable compound.

review image

Good product.
By Anonymous on 05/14/2019
Assay Type: Ex Vivo
Species: Mouse

Effectively blocked agonist-induced reductions in neuronal firing in slice. Works as advertised & would recommend.

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