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
Drug Categories	alimentary tract and metabolism
Drug Categories	analgesics
Drug Categories	cytochrome p-450 cyp3a inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors (strong)
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	drugs for constipation
Drug Categories	drugs that are mainly renally excreted
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	narcotics
Drug Categories	natural opium alkaloids
Drug Categories	nervous system
Drug Categories	opiate antagonists
Drug Categories	opioid antagonists
Drug Categories	p-glycoprotein substrates
Drug Categories	peripheral opioid receptor antagonists
Drug Categories	ugt1a1 substrates

(5 More Sources)

Publications:

Wand GS et al., 2002, The mu-opioid receptor gene polymorphism (A118G) alters HPA axis activation induced by opioid receptor blockade., Neuropsychopharmacology
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., 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
Neal et al., 2003, Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors., J. Chem. Neuroanat.
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.
Marek, 2003, Behavioral evidence for mu-opioid and 5-HT2A receptor interactions., Eur. J. Pharmacol.
Spetea et al., 2003, Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist., Eur. J. Neurosci.
van Dorp et al., 2007, Naloxone treatment in opioid addiction: the risks and benefits., Expert Opin Drug Saf
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
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
Goodman et al., 2007, Mu opioid receptor antagonists: recent developments., ChemMedChem
Freye et al., 1998, [The opioid tramadol demonstrates excitatory properties of non-opioid character--a preclinical study using alfentanil as a comparison]., Schmerz
Chong RY et al., 2006, The mu-opioid receptor polymorphism A118G predicts cortisol responses to naloxone and stress., Neuropsychopharmacology
Chartoff et al., 2003, Dopamine-dependent increases in phosphorylation of cAMP response element binding protein (CREB) during precipitated morphine withdrawal in primary cultures of rat striatum., J. Neurochem.
Walters et al., 2005, Mu-opioid receptor and CREB activation are required for nicotine reward., Neuron
Li et al., 2003, Changes of phosphorylation of cAMP response element binding protein in rat nucleus accumbens after chronic ethanol intake: naloxone reversal., Acta Pharmacol. Sin.
Gao et al., 2003, Effects of ohmefentanyl stereoisomers on phosphorylation of cAMP- response element binding protein in cultured rat hippocampal neurons., Acta Pharmacol. Sin.
Hawes et al., 2006, Galanin attenuates cyclic AMP regulatory element-binding protein (CREB) phosphorylation induced by chronic morphine and naloxone challenge in Cath.a cells and primary striatal cultures., J. Neurochem.
Farooqui et al., 2006, Naloxone acts as an antagonist of estrogen receptor activity in MCF-7 cells., Mol. Cancer Ther.
Vanvugt et al., 1989, Naloxone antagonism of corticotropin-releasing hormone stimulation of prolactin secretion in rhesus monkeys., J. Clin. Endocrinol. Metab.
Lewis et al., 2012, (+)-naloxone, an opioid-inactive toll-like receptor 4 signaling inhibitor, reverses multiple models of chronic neuropathic pain in rats., J Pain
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.
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.
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
Breljak et al., Oligopeptide fragments of the enkephalin molecule interfere with hematopoietic cell colony formation., Int J Immunopathol Pharmacol
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
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.
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.
Bencharit S et al., 2003, Structural basis of heroin and cocaine metabolism by a promiscuous human drug-processing enzyme., Nat Struct Biol

NALOXONE CREB1

Interaction Score: 3.79

Interaction Types & Directionality:

other/unknown

Interaction Info:

PMIDs:
12969258 15953421 12956944 14653953 16417577

Sources:
DrugBank
NALOXONE ADCYAP1R1

Interaction Score: 1.89

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12573539

Sources:
NCI
NALOXONE CRH

Interaction Score: 1.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2542355

Sources:
NCI
NALOXONE GRP

Interaction Score: 1.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2889122

Sources:
NCI
NALOXONE OPRD1

Interaction Score: 0.59

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
18354714 14708857 14646257 12657847 12749773 17367258 24613457 12650833

Sources:
TEND DTC TdgClinicalTrial DrugBank GuideToPharmacology
NALOXONE ANPEP

Interaction Score: 0.58

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2738884

Sources:
NCI
NALOXONE OPRM1

Interaction Score: 0.52

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name REN-213

Trial Name buprenorphine + naloxone,Suboxone

Novel drug target Established target

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

Sources:
TEND DTC PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology
NALOXONE NTF3

Interaction Score: 0.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9334418

Sources:
NCI
NALOXONE TLR4

Interaction Score: 0.4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
22520687

Sources:
DrugBank
NALOXONE CES1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12679808

Sources:
DrugBank
NALOXONE RARA

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14741437

Sources:
NCI
NALOXONE PRL

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2875176

Sources:
NCI
NALOXONE OPRK1

Interaction Score: 0.2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
18354714 17367258 17305578

Sources:
TdgClinicalTrial DrugBank GuideToPharmacology
NALOXONE BDNF

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12359151

Sources:
NCI
NALOXONE ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

other/unknown

antagonist (inhibitory)

Interaction Info:

PMIDs:
16546975

Sources:
DrugBank

DrugBank: DB01183

Version: 5.1.7

Alternate Names:

465-65-6 CAS Number

Act Buprenorphine/naloxone Drug Brand

Bunavail Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups vet_approved

Publications:

Lewis et al., 2012, (+)-naloxone, an opioid-inactive toll-like receptor 4 signaling inhibitor, reverses multiple models of chronic neuropathic pain in rats., J Pain

Helm et al., Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification., Pain Physician

van Dorp et al., 2007, Naloxone treatment in opioid addiction: the risks and benefits., Expert Opin Drug Saf

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

465-65-6	CAS Number
Act Buprenorphine/naloxone	Drug Brand
Bunavail	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	vet_approved

other/unknown
antagonist (inhibitory)

NALOXONE Drug Record

NALOXONE chembl:CHEMBL80 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: other/unknown

Interaction Info:

PMIDs: 12969258 15953421 12956944 14653953 16417577

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12573539

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2542355

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: 18354714 14708857 14646257 12657847 12749773 17367258 24613457 12650833

Sources: TEND DTC TdgClinicalTrial DrugBank 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: 11751037 17616524 12627468 12842269 18354714 12566163 12909198 12887410 17367258 11752352 18004207 17918759 12799988 16123758

Sources: TEND DTC PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9334418

Sources: NCI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 22520687

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12679808

Sources: DrugBank

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: 18354714 17367258 17305578

Sources: TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12359151

Sources: NCI

Interaction Types & Directionality: other/unknown antagonist (inhibitory)

Interaction Info:

PMIDs: 16546975

Sources: DrugBank

DrugBank: DB01183

Alternate Names: 465-65-6 CAS Number Act Buprenorphine/naloxone Drug Brand Bunavail Drug Brand

Drug Info: Drug Type small molecule Drug Groups approved Drug Groups vet_approved

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

Interaction Types & Directionality:

other/unknown

PMIDs:
12969258 15953421 12956944 14653953 16417577

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
12573539

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
2542355

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:
18354714 14708857 14646257 12657847 12749773 17367258 24613457 12650833

Sources:
TEND DTC TdgClinicalTrial DrugBank 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:
11751037 17616524 12627468 12842269 18354714 12566163 12909198 12887410 17367258 11752352 18004207 17918759 12799988 16123758

Sources:
TEND DTC PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
9334418

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
22520687

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
12679808

Sources:
DrugBank

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:
18354714 17367258 17305578

Sources:
TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
12359151

Sources:
NCI

Interaction Types & Directionality:

other/unknown

antagonist (inhibitory)

PMIDs:
16546975

Sources:
DrugBank

Alternate Names:

465-65-6 CAS Number

Act Buprenorphine/naloxone Drug Brand

Bunavail Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups vet_approved

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