nor-Binaltorphimine dihydrochloride

Cat. No. 0347

nor-Binaltorphimine dihydrochloride C40H43N3O6.2HCl [113158-34-2]

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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

Biological Activity

A selective κ-opioid receptor antagonist.

Licensing Information

Sold with the permission of the University of Minnesota

Technical Data

Soluble to 25 mM in water with gentle warming and to 25 mM in DMSO
>98 %
Store at RT

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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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.

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

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

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.

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.

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.

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

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.

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

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

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.

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

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

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

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.

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.

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.

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

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.

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.

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.

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Keywords: nor-Binaltorphimine dihydrochloride, supplier, selective, antagonists, κ-opioid, kappa-opioid, KOP, Receptors, OP2, Tocris Bioscience, κ Opioid Receptor Antagonist products

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