nor-Binaltorphimine dihydrochloride
Chemical Name: 17,17'-(Dicyclopropylmethyl)-6,6',7,7'-6,6'-imino- 7,7'-binorphinan-3,4',14,14'-tetrol dihydrochloride
Purity: ≥98%
Biological Activity
A selective κ-opioid receptor antagonist.Technical Data
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.
Additional Information
Background References
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Differential agonist regulation of the human κ-opioid receptor.
Blake et al.
J.Neurochem., 1997;68:1846 -
Nor-binaltorphimine precipitates withdrawal and excitatory amino acid release in the locus ceruleus of butorphanol- but not morphine-dependent rats.
Feng et al.
J.Pharmacol.Exp.Ther., 1997;283:932 -
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.
Portoghese et al.
J.Med.Chem., 1994;37:1495
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Citations for nor-Binaltorphimine dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for nor-Binaltorphimine dihydrochloride include:
30 Citations: Showing 1 - 10
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The kappa opioid receptor modulates GABA neuron excitability and synaptic transmission in midbrain-projections from the insular cortex.
Authors: Pina Et al.
Neuropharmacology 2020;165:107831
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Discovery of small molecules that normalize the transcriptome and enhance cysteine cathepsin activity in progranulin-deficient microglia.
Authors: Telpoukhovskaia Et al.
Sci Rep 2020;10
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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.
Authors: Norris Et al.
Sci Rep 2019;9:9760
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Selective blockade of spinal D2DR by levo-corydalmine attenuates MOR tolerance via suppressing PI3K/Akt-MAPK signaling in a MOR-dependent manner.
Authors: Dai Et al.
Exp Mol Med 2018;50:148
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Constitutive activation of kappa opioid receptors at ventral tegmental area inhibitory synapsesfollowing acute stress.
Authors: Polter
Elife 2017;6:e23785
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Endogenous central amygdala mu-opioid receptor signaling promotes sodium appetite in mice.
Authors: Smith Et al.
Proc Natl Acad Sci U S A 2016;113:13893
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Effect of adenoviral delivery of prodynorphin gene on experimental inflammatory pain induced by formalin in rats.
Authors: Chen Et al.
PLoS One 2015;7:4877
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Distinct functions of opioid-related peptides and gastrin-releasing peptide in regulating itch and pain in the spinal cord of primates.
Authors: Lee and Ko
Neuropsychopharmacology 2015;5:11676
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Low-frequency electroacupuncture suppresses focal epilepsy and improves epilepsy-induced sleep disruptions.
Authors: Yi Et al.
Appl Environ Microbiol 2015;22:49
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Effects and interactions of tachykinins and dynorphin on FSH and LH secretion in developing and adult rats.
Authors: Ruiz-Pino Et al.
Endocrinology 2015;156:576
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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.
Authors: Chen Et al.
Sci Rep 2015;10:e0145556
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Methamphetamine induces autophagy as a pro-survival response against apoptotic endothelial cell death through the Kappa opioid receptor.
Authors: Ma Et al.
Cell Death Dis 2014;5:e1099
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Upregulated dynorphin opioid peptides mediate alcohol-induced learning and memory impairment.
Authors: Kuzmin Et al.
Transl Psychiatry 2013;3:e310
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Prefrontal cortical kappa-opioid receptor modulation of local neurotransmission and conditioned place aversion.
Authors: Tejeda Et al.
Neuropsychopharmacology 2013;38:1770
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Hypothalamic κ-opioid receptor modulates the orexigenic effect of ghrelin.
Authors: Romero-Picó Et al.
Br J Cancer 2013;38:1296
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Functional selectivity of 6'-guanidinonaltrindole (6'-GNTI) at κ-opioid receptors in striatal neurons.
Authors: Schmid Et al.
J Biol Chem 2013;288:22387
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Label-free integrative pharmacology on-target of opioid ligands at the opioid receptor family.
Authors: Morse Et al.
BMC Pharmacol Toxicol 2013;14:17
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Salvinorin A reduces mechanical allodynia and spinal neuronal hyperexcitability induced by peripheral formalin injection.
Authors: Guida Et al.
Mol Pain 2012;8:60
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Effects of a post-shock injection of the kappa opioid receptor antagonist norbinaltorphimine (norBNI) on fear and anxiety in rats.
Authors: Rogala Et al.
PLoS One 2012;7:e49669
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GPR54-dependent stimulation of luteinizing hormone secretion by neurokinin B in prepubertal rats.
Authors: Grachev Et al.
Neuropsychopharmacology 2012;7:e44344
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Effect of κ-opioid receptor agonist on the growth of non-small cell lung cancer (NSCLC) cells.
Authors: Kuzumaki Et al.
Neuropsychopharmacology 2012;106:1148
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Ligand-directed functional selectivity at the mu opioid receptor revealed by label-free integrative pharmacology on-target.
Authors: Morse Et al.
PLoS One 2011;6:e25643
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κ opioid receptor localization and coupling to nitric oxide production in cells of the anterior chamber.
Authors: Russell-Randall and Dortch-Carnes
J Biomed Sci 2011;52:5233
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Identification of a κ-opioid agonist as a potent and selective lead for drug development against human African trypanosomiasis.
Authors: Jones Et al.
Biochem Pharmacol 2010;80:1478
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Antidepressant-like effects of κ-opioid receptor antagonists in Wistar Kyoto rats.
Authors: Carr Et al.
Invest Ophthalmol Vis Sci 2010;35:752
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Evidence for a role of opioids in epoxyeicosatrienoic acid-induced cardioprotection in rat hearts.
Authors: Gross Et al.
Am J Physiol Heart Circ Physiol 2010;298:H2201
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Endogenous opiates in the nucleus tractus solitarius mediate electroacupuncture-induced sleep activities in rats.
Authors: Cheng Et al.
PLoS One 2009;2011:159209
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Potential anxiolytic- and antidepressant-like effects of salvinorin A, the main active ingredient of Salvia divinorum, in rodents.
Authors: Braida Et al.
Br J Pharmacol 2009;157:844
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The dysphoric component of stress is encoded by activation of the dynorphin kappa-opioid system.
Authors: Land Et al.
J Neurosci 2008;28:407
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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.
Authors: García-Fuster Et al.
Int J Clin Exp Med 2007;32:399
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Successfully stopped selective agonist-induced ERK phosphorylation in CHO cells. It’s a very reliable compound.
Effectively blocked agonist-induced reductions in neuronal firing in slice. Works as advertised & would recommend.