Naloxone hydrochloride

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Cat.No. 0599 - Naloxone hydrochloride | C19H21NO4.HCl | CAS No. 357-08-4
Description: Non-selective opioid antagonist
Chemical Name: (5α)-4,5-Epoxy-3,14-dihydro-17-(2-propenyl)morphinan-6-one hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (31)
Reviews
Literature

Biological Activity

Opioid antagonist.

Technical Data

M. Wt 363.84
Formula C19H21NO4.HCl
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 357-08-4
PubChem ID 5464092
InChI Key RGPDIGOSVORSAK-STHHAXOLSA-N
Smiles O=C3[C@H]4[C@]25C1=C(O4)C(O)=CC=C1C[C@@H](N(CC5)CC=C)[C@@](O)2CC3.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 36.38 100

Preparing Stock Solutions

The following data is based on the product molecular weight 363.84. Batch specific molecular weights may vary from batch to batch due to the degree 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 2.75 mL 13.74 mL 27.48 mL
5 mM 0.55 mL 2.75 mL 5.5 mL
10 mM 0.27 mL 1.37 mL 2.75 mL
50 mM 0.05 mL 0.27 mL 0.55 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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

Pinelli and Trivulzio (1997) Quantitative evaluation of opioid withdrawal signs in rats repeatedly treated with mor. and injected with naloxone, in the absence or presence of the antiabstinence agent clon. J.Pharmacol.Toxicol.Methods 38 117 PMID: 9523765

Spivak et al (1997) Naloxone activation of mu-opioid receptors mutated at a histidine residue lining the opioid cavity. Mol.Pharmacol. 52 983 PMID: 9415708

Olson et al (1996) Endogenous opiates: 1995. Peptides 17 1421

Merck Index 12 6449


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Keywords: Naloxone hydrochloride, Naloxone hydrochloride supplier, Broad, spectrum, opioid, antagonists, Receptors, Miscellaneous/Non-selective, Opioids, 0599, Tocris Bioscience

31 Citations for Naloxone hydrochloride

Citations are publications that use Tocris products. Selected citations for Naloxone hydrochloride include:

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

Ali (2011) CB1 modulation of temporally distinct synaptic facilitation among local circuit interneurons mediated by N-type calcium channels in CA1. J Neurophysiol 105 1051 PMID: 21123660

Cheng et al (2009) Endogenous opiates in the nucleus tractus solitarius mediate electroacupuncture-induced sleep activities in rats. Proc Natl Acad Sci U S A 2011 159209 PMID: 19729491

Melyan et al (2004) Metabotropic regulation of intrinsic excitability by synaptic activation of kainate receptors. J Neurosci 24 4530 PMID: 15140923

Navratilova et al (2012) Pain relief produces negative reinforcement through activation of mesolimbic reward-valuation circuitry. FASEB J 109 20709 PMID: 23184995

Moore et al (2003) Adenosine gates synaptic plasticity at hippocampal mossy fiber synapses. Neuropsychopharmacology 100 14397 PMID: 14608033

Francois et al (2017) A Brainstem-Spinal Cord Inhibitory Circuit for Mechanical Pain Modulation by GABA and Enkephalins. Neuron 93 822 PMID: 28162807

Largent-Milnes et al (2010) Spinal or systemic TY005, a peptidic opioid agonist/neurokinin 1 antagonist, attenuates pain with reduced tolerance. Br J Pharmacol 161 986 PMID: 20977451

Cruz et al (2008) Absence and rescue of mor. withdrawal in GIRK/Kir3 knock-out mice. J Neurosci 28 4069 PMID: 18400906

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

Liu et al (2015) Morphological and physiological evidence of a synaptic connection between the lateral parabrachial nucleus and neurons in the A7 catecholamine cell group in rats. J Biomed Sci 22 79 PMID: 26385355

Gerhold et al (2015) Pronociceptive and Antinociceptive Effects of Bupren. in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude. J Neurosci 35 9580 PMID: 26134641

Wang et al (2018) Functional Divergence of Delta and Mu Opioid Receptor Organization in CNS Pain Circuits. Neuron 98 90 PMID: 29576387

Jeong et al (2018) Activation of temperature-sensitive TRPV1-like receptors in ARC POMC neurons reduces food intake. PLoS Biol 16 e2004399 PMID: 29689050

Wang et al (2015) Bupren.-elicited alteration of adenylate cyclase activity in human embryonic kidney 293 cells coexpressing κ-, μ-opioid and nociceptin receptors. Nature 19 2587 PMID: 26153065

Koch et al (2015) Hypothalamic POMC neurons promote cannabinoid-induced feeding. J Neurosci 519 45 PMID: 25707796

Navratilova et al (2015) Endogenous opioid activity in the anterior cingulate cortex is required for relief of pain. Front Endocrinol (Lausanne) 35 7264 PMID: 25948274

Levoye et al (2015) A Broad G Protein-Coupled Receptor Internalization Assay that Combines SNAP-Tag Labeling, Diffusion-Enhanced Resonance Energy Transfer, and a Highly Emissive Terbium Cryptate. PLoS One 6 167 PMID: 26617570

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. Psychopharmacology (Berl) 10 e0145556 PMID: 26700862

Kelly et al (2015) The opioid receptor pharmacology of GSK1521498 compared to other ligands with differential effects on compulsive reward-related behaviours. World J Gastroenterol 232 305 PMID: 24973897

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

Pereira et al (2015) Endogenous Opioid-Masked Latent Pain Sensitization: Studies from Mouse to Human. Proc Natl Acad Sci U S A 10 e0134441 PMID: 26305798

Marti et al (2013) Acute and chronic antiparkinsonian effects of the novel nociceptin/orphanin FQ receptor antagonist NiK-21273 in comparison with SB-612111. Br J Pharmacol 168 863 PMID: 22994368

Largent-Milnes et al (2013) Building a better analgesic: multifunctional compounds that address injury-induced pathology to enhance analgesic efficacy while eliminating unwanted side effects. J Pharmacol Exp Ther 347 7 PMID: 23860305

Chen et al (2014) Antinociceptive effects of novel melatonin receptor agonists in mouse models of abdominal pain. Neuropsychopharmacology 20 1298 PMID: 24574803

Zhou et al (2013) Development of functionally selective, small molecule agonists at kappa opioid receptors. J Biol Chem 288 36703 PMID: 24187130

Moser and Giesler (2013) Itch and analgesia resulting from intrathecal application of morphine: contrasting effects on different populations of trigeminothalamic tract neurons. J Neurosci 33 6093 PMID: 23554490

Patel et al (2007) Mechanisms of cardiac protection from ischemia/reperfusion injury: a role for caveolae and caveolin-1. Nat Commun 21 1565 PMID: 17272740

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. J Cell Mol Med 32 399 PMID: 16482086

Proudfoot et al (2006) Analgesia mediated by the TRPM8 cold receptor in chronic neuropathic pain. Curr Biol 16 1591 PMID: 16920620

Hauser et al (2018) Pharmacogenomics of GPCR Drug Targets. Cell 172 41 PMID: 29249361


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