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NALOXONE Drug Record

  • Summary
  • Interactions
  • Claims
  • NALOXONE chembl:CHEMBL80 Approved

    Alternate Names:

    NARCANTI
    NARCAN
    NSC-70413
    NALONE
    SUBOXONE
    NALOXONE
    17-ALLYL-3,14-DIHYDROXY-4,5ALPHA-EPOXYMORPHINAN-6-ONE
    NALOXONA
    (−)-NALOXONE
    NARCAN®
    1-N-ALLYL-14-HYDROXYNORDIHYDROMORPHINONE
    (-)-NALOXONE
    NALOXONUM
    NALOSSONE
    17-ALLYL-3,14-DIHYDROXY-4,5Α-EPOXYMORPHINAN-6-ONE
    L-NALOXONE
    rxcui:7242
    drugbank:01183
    pubchem.compound:5284596
    chembl:CHEMBL80
    chemidplus:465-65-6

    Drug Info:

    Drug Class opiate antagonists
    Year of Approval 1971
    Drug Indications for treatment of opioid addiction
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications analgesic
    (3 More Sources)

    Publications:

    Nikolaev VO et al., 2007, Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors., J Biol Chem
    Hernandez-Avila CA et al., 2007, Population-specific effects of the Asn40Asp polymorphism at the mu-opioid receptor gene (OPRM1) on HPA-axis activation., Pharmacogenet Genomics
    Chong RY et al., 2006, The mu-opioid receptor polymorphism A118G predicts cortisol responses to naloxone and stress., Neuropsychopharmacology
    Hernandez-Avila CA et al., 2003, Association between the cortisol response to opioid blockade and the Asn40Asp polymorphism at the mu-opioid receptor locus (OPRM1)., Am J Med Genet B Neuropsychiatr Genet
    Wand GS et al., 2002, The mu-opioid receptor gene polymorphism (A118G) alters HPA axis activation induced by opioid receptor blockade., Neuropsychopharmacology
    Freye et al., 1998, [The opioid tramadol demonstrates excitatory properties of non-opioid character--a preclinical study using alfentanil as a comparison]., Schmerz
    Goodman et al., 2007, Mu opioid receptor antagonists: recent developments., ChemMedChem
    Helm et al., Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification., Pain Physician
    Narita et al., 2003, Up-regulation of mu-opioid receptor-mediated G-protein activation in protein kinase Cgamma knockout mice following repeated naloxone treatment., Neurosci. Lett.
    Spetea et al., 2003, Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist., Eur. J. Neurosci.
    Marek, 2003, Behavioral evidence for mu-opioid and 5-HT2A receptor interactions., Eur. J. Pharmacol.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Neal et al., 2003, Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors., J. Chem. Neuroanat.
    van Dorp et al., 2007, Naloxone treatment in opioid addiction: the risks and benefits., Expert Opin Drug Saf
    Vanvugt et al., 1989, Naloxone antagonism of corticotropin-releasing hormone stimulation of prolactin secretion in rhesus monkeys., J. Clin. Endocrinol. Metab.
    Malcangio et al., 1997, Nerve growth factor- and neurotrophin-3-induced changes in nociceptive threshold and the release of substance P from the rat isolated spinal cord., J. Neurosci.
    Cai J et al., 2014, Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity., Bioorg Med Chem
    Kakinohana et al., 2003, Neuraxial morphine may trigger transient motor dysfunction after a noninjurious interval of spinal cord ischemia: a clinical and experimental study., Anesthesiology
    Moncada et al., 2003, Effects of serine/threonine protein phosphatase inhibitors on morphine-induced antinociception in the tail flick test in mice., Eur. J. Pharmacol.
    Breljak et al., Oligopeptide fragments of the enkephalin molecule interfere with hematopoietic cell colony formation., Int J Immunopathol Pharmacol
    Osman et al., 2003, A possible role for an enkephalinergic system in the internal defense mechanism of Biomphalaria alexandrina exposed to Schistosoma mansoni., J Egypt Soc Parasitol
    Chudapongse et al., 2003, Nonspecific effects of the selective kappa-opioid receptor agonist U-50,488H on dopamine uptake and release in PC12 cells., J. Pharmacol. Sci.
    Mou et al., 2004, RXR-induced TNF-alpha suppression is reversed by morphine in activated U937 cells., J. Neuroimmunol.
    Peng et al., 2007, Kappa receptor bivalent ligands., Curr Top Med Chem
    Xie et al., 1989, New kelatorphan-related inhibitors of enkephalin metabolism: improved antinociceptive properties., J. Med. Chem.
    Pezet et al., 2002, BDNF modulates sensory neuron synaptic activity by a facilitation of GABA transmission in the dorsal horn., Mol. Cell. Neurosci.
    Martin et al., 2003, Morphine withdrawal is modified in pituitary adenylate cyclase-activating polypeptide type I-receptor-deficient mice., Brain Res. Mol. Brain Res.
    Nishi et al., 1987, Effects of naloxone on basal and vagus nerve-induced secretions of GRP, gastrin, and somatostatin from the isolated perfused rat stomach., Life Sci.
    Gilbeau et al., 1986, Dynorphin effects on plasma concentrations of anterior pituitary hormones in the nonhuman primate., J. Pharmacol. Exp. Ther.
  • NALOXONE   ADCYAP1R1

    Interaction Score: 5.62

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12573539


    Sources:
    NCI

  • NALOXONE   CRH

    Interaction Score: 5.62

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    2542355


    Sources:
    NCI

  • NALOXONE   GRP

    Interaction Score: 1.61

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    2889122


    Sources:
    NCI

  • NALOXONE   OPRD1

    Interaction Score: 1.51

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name REN-213
    Novel drug target Established target

    PMIDs:
    24613457 12657847 18354714 12650833 12749773 14708857 14646257 17367258


    Sources:
    DTC TdgClinicalTrial TEND

  • NALOXONE   ANPEP

    Interaction Score: 1.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    2738884


    Sources:
    NCI

  • NALOXONE   OPRM1

    Interaction Score: 0.97

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name REN-213
    Trial Name buprenorphine + naloxone,Suboxone
    Novel drug target Established target

    PMIDs:
    17616524 18004207 16123758 12627468 11751037 12799988 17918759 18354714 12566163 12887410 12909198 11752352 12842269 17367258


    Sources:
    DTC TdgClinicalTrial TEND PharmGKB

  • NALOXONE   NTF3

    Interaction Score: 0.7

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9334418


    Sources:
    NCI

  • NALOXONE   RARA

    Interaction Score: 0.37

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14741437


    Sources:
    NCI

  • NALOXONE   PRL

    Interaction Score: 0.34

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    2875176


    Sources:
    NCI

  • NALOXONE   OPRK1

    Interaction Score: 0.33

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name buprenorphine + naloxone capsule,NanoBUP
    Novel drug target Established target
    Trial Name buprenorphine + naloxone,Suboxone

    PMIDs:
    17367258 18354714 17305578


    Sources:
    TdgClinicalTrial

  • NALOXONE   BDNF

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12359151


    Sources:
    NCI

  • TEND: NALOXONE

    • Version: 01-August-2011

    Alternate Names:

    Drug Info:
    Year of Approval 1971
    Drug Class opiate antagonists

    Publications:

  • TdgClinicalTrial: NALOXONE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications analgesic
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • NCI: NALOXONE

    • Version: 14-September-2017

    Alternate Names:
    C678 NCI drug code

    Drug Info:

    Publications:
    Martin et al., 2003, Morphine withdrawal is modified in pituitary adenylate cyclase-activating polypeptide type I-receptor-deficient mice., Brain Res. Mol. Brain Res.
    Vanvugt et al., 1989, Naloxone antagonism of corticotropin-releasing hormone stimulation of prolactin secretion in rhesus monkeys., J. Clin. Endocrinol. Metab.
    Xie et al., 1989, New kelatorphan-related inhibitors of enkephalin metabolism: improved antinociceptive properties., J. Med. Chem.

  • DTC: NALOXONE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL80 ChEMBL Drug ID

    Drug Info:

    Publications:
    Nikolaev VO et al., 2007, Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors., J Biol Chem
    Cai J et al., 2014, Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity., Bioorg Med Chem

  • PharmGKB: naloxone

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Wand GS et al., 2002, The mu-opioid receptor gene polymorphism (A118G) alters HPA axis activation induced by opioid receptor blockade., Neuropsychopharmacology
    Hernandez-Avila CA et al., 2003, Association between the cortisol response to opioid blockade and the Asn40Asp polymorphism at the mu-opioid receptor locus (OPRM1)., Am J Med Genet B Neuropsychiatr Genet
    Hernandez-Avila CA et al., 2007, Population-specific effects of the Asn40Asp polymorphism at the mu-opioid receptor gene (OPRM1) on HPA-axis activation., Pharmacogenet Genomics

  • TTD: Naloxone

    • Version: 2020.06.01

    Alternate Names:
    D0X3FX TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL80

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21