DGIdb - NALOXONE Drug Record

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

(4 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 CRH

Interaction Score: 5.8

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2542355

Sources:
NCI
NALOXONE ADCYAP1R1

Interaction Score: 2.9

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12573539

Sources:
NCI
NALOXONE GRP

Interaction Score: 1.66

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2889122

Sources:
NCI
NALOXONE OPRD1

Interaction Score: 1.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
24613457 12657847 18354714 12650833 12749773 14708857 14646257 17367258

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology
NALOXONE ANPEP

Interaction Score: 1.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2738884

Sources:
NCI
NALOXONE OPRM1

Interaction Score: 0.89

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 GuideToPharmacology PharmGKB
NALOXONE NTF3

Interaction Score: 0.72

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: 0.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2875176

Sources:
NCI
NALOXONE OPRK1

Interaction Score: 0.33

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
17367258 18354714 17305578

Sources:
TdgClinicalTrial GuideToPharmacology
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:
GuideToPharmacology: 135650684
- Version: 29-September-2020
Alternate Names:

Drug Info:

Publications:

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False
Direct Interaction?	True

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

NALOXONE Drug Record

NALOXONE chembl:CHEMBL80 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2542355

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12573539

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2889122

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

PMIDs: 24613457 12657847 18354714 12650833 12749773 14708857 14646257 17367258

Sources: DTC TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2738884

Sources: NCI

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 GuideToPharmacology PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9334418

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 14741437

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2875176

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

PMIDs: 17367258 18354714 17305578

Sources: TdgClinicalTrial GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12359151

Sources: NCI

TEND: NALOXONE

Alternate Names:

Drug Info: Year of Approval 1971 Drug Class opiate antagonists

Publications:

TdgClinicalTrial: NALOXONE

Alternate Names:

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

Publications:

NCI: NALOXONE

Alternate Names: C678 NCI drug code

Drug Info:

DTC: NALOXONE

Alternate Names: CHEMBL80 ChEMBL Drug ID

Drug Info:

PharmGKB: naloxone

Alternate Names:

Drug Info:

TTD: Naloxone

Alternate Names: D0X3FX TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL80

Alternate Names:

Drug Info:

Publications:

GuideToPharmacology: 135650684

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
2542355

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
12573539

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
2889122

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
24613457 12657847 18354714 12650833 12749773 14708857 14646257 17367258

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
2738884

Sources:
NCI

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 GuideToPharmacology PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
9334418

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
14741437

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
2875176

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
17367258 18354714 17305578

Sources:
TdgClinicalTrial GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
12359151

Sources:
NCI

Drug Info:

Year of Approval 1971

Drug Class opiate antagonists

Drug Info:

Drug Indications analgesic

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

C678 NCI drug code

Alternate Names:

CHEMBL80 ChEMBL Drug ID

Alternate Names:

D0X3FX TTD Drug ID