• Search
      • Search Interactions Search Categories
    • Browse
      • Browse Categories Browse Sources
    • Information
      • About Publications Interaction Types & Directionalities Interaction Score & Query Score API Documentation FAQ Known Data Clients News Contact
    • Downloads
      • Data Source Code

DEXTROMETHORPHAN Drug Record

  • Summary
  • Interactions
  • Claims
  • DEXTROMETHORPHAN chembl:CHEMBL52440 Approved

    Alternate Names:

    DEXTROMETHORPHAN
    DIMETANE-DX
    DEXTROMÉTHORPHANE
    (9S,13S,14S)-3-METHOXY-17-METHYLMORPHINAN
    D-METHORPHAN
    DM
    DEXTROMETHORPHANUM
    DEXTROMETHORFAN
    (+)-DEXTROMETHORPHAN
    DELTA-METHORPHAN
    DEXTROMETORFANO
    DEX
    chembl:CHEMBL52440
    rxcui:3289
    rxcui:236146
    chemidplus:125-71-3
    pubchem.compound:5360696
    drugbank:00514

    Drug Info:

    Drug Categories antitussive agents
    Drug Class antitussive agents
    Year of Approval approved before 1982
    FDA Approval Approved before 1982
    Drug Class small molecule
    Drug Indications Antitussive Agents
    Drug Indications analgesic
    FDA Approval approved
    Drug Class Small molecule
    Drug Indications antitussive agent
    Drug Categories anticholinergic agents
    Drug Categories antidepressive agents
    Drug Categories central nervous system depressants
    Drug Categories combined inhibitors of serotonin/norepinephrine reuptake
    Drug Categories cough and cold preparations
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a5 substrates
    Drug Categories cytochrome p-450 cyp3a7 substrates
    Drug Categories cytochrome p-450 substrates
    Drug Categories expectorants
    Drug Categories heterocyclic compounds, fused-ring
    Drug Categories narcotics
    Drug Categories nicotinic antagonists
    Drug Categories opium alkaloids and derivatives
    Drug Categories serotonergic drugs shown to increase risk of serotonin syndrome
    Drug Categories serotonin agents
    Drug Categories sigma-1 agonist
    Drug Categories sigma-1 receptor agonists
    Drug Categories uncompetitive n-methyl-d-aspartate receptor antagonist
    Drug Categories uncompetitive nmda receptor antagonists
    (6 More Sources)

    Publications:

    Uhr et al., 2004, P-glycoprotein is a factor in the uptake of dextromethorphan, but not of melperone, into the mouse brain: evidence for an overlap in substrate specificity between P-gp and CYP2D6., J. Psychopharmacol. (Oxford)
    Damaj et al., 2005, Effect of dextrometorphan and dextrorphan on nicotine and neuronal nicotinic receptors: in vitro and in vivo selectivity., J. Pharmacol. Exp. Ther.
    Zhang et al., 2004, Neuroprotective effect of dextromethorphan in the MPTP Parkinson's disease model: role of NADPH oxidase., FASEB J.
    Chou et al., 1999, Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan., Brain Res.
    Shin et al., 2005, The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: comparison with the effects of dextromethorphan., Br. J. Pharmacol.
    Shin et al., 2007, Dextromethorphan attenuates trimethyltin-induced neurotoxicity via sigma1 receptor activation in rats., Neurochem. Int.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Church et al., 2005, Spreading depression expands traumatic injury in neocortical brain slices., J. Neurotrauma
    Nagy LD et al., 2011, Substituted imidazole of 5-fluoro-2-[4-[(2-phenyl-1H-imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine Inactivates cytochrome P450 2D6 by protein adduction., Drug Metab Dispos
    Kamel et al., 2008, N-methyl-D-aspartate (NMDA) antagonists--S(+)-ketamine, dextrorphan, and dextromethorphan--act as calcium antagonists on bovine cerebral arteries., J Neurosurg Anesthesiol
    Wong et al., 1988, Dextrorphan and dextromethorphan, common antitussives, are antiepileptic and antagonize N-methyl-D-aspartate in brain slices., Neurosci. Lett.
    Codd et al., 1995, Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception., J. Pharmacol. Exp. Ther.
    Lee et al., 2006, Effects of dextrorotatory morphinans on alpha3beta4 nicotinic acetylcholine receptors expressed in Xenopus oocytes., Eur. J. Pharmacol.
    Vengurlekar et al., 2002, A sensitive LC-MS/MS assay for the determination of dextromethorphan and metabolites in human urine--application for drug interaction studies assessing potential CYP3A and CYP2D6 inhibition., J Pharm Biomed Anal
    Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
    Henderson et al., 1992, Dextromethorphan antagonizes the acute depletion of brain serotonin by p-chloroamphetamine and H75/12 in rats., Brain Res.
    Yin et al., 1999, Effect of dextromethorphan, a NMDA antagonist, on DNA repair in rat photochemical thrombotic cerebral ischemia., Brain Res.
  • DEXTROMETHORPHAN   ERCC6

    Interaction Score: 1.89

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9974119


    Sources:
    NCI

  • DEXTROMETHORPHAN   PGRMC1

    Interaction Score: 1.89

    Interaction Types & Directionality:
    binder

    Interaction Info:

    PMIDs:
    10064839


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   SIGMAR1

    Interaction Score: 1.55

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Details of the Assay for Interaction Sigma receptor cloned from Jurkat cells, identified as SIGMAR1.
    Specific Action of the Ligand Agonist
    Endogenous Drug? False

    PMIDs:
    15723099 17386960 11752352 17139284 10064839 17016423 15716633


    Sources:
    TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • DEXTROMETHORPHAN   CYBB

    Interaction Score: 1.42

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    14734632


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   GRIN3A

    Interaction Score: 0.57

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name AVP-923
    Novel drug target Established target
    Trial Name morphine/dextromethorphan,MorphiDex

    PMIDs:
    18812887 2897648 17139284 10064839 17016423


    Sources:
    TEND TdgClinicalTrial DrugBank

  • DEXTROMETHORPHAN   CHRNA2

    Interaction Score: 0.53

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    16563374 15356218 17139284 17016423


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   CHRNB4

    Interaction Score: 0.32

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    15356218


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   CHRNB2

    Interaction Score: 0.21

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    15356218


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   CHRNA3

    Interaction Score: 0.19

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    15356218


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   SLC6A4

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    17139284 1280529 17016423 7562497


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   CHRNA4

    Interaction Score: 0.1

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    15356218


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   CHRNA7

    Interaction Score: 0.09

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    15356218


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   GRIN2C

    Interaction Score: 0.08

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Measured <i>vs.</i> exogenously expressed zeta1/epsilon3 (<i>GRIN1/GRIN2C</i>) subunits, at pH 6.9
    Specific Action of the Ligand None
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • DEXTROMETHORPHAN   SLC6A2

    Interaction Score: 0.07

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    7562497


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   OPRD1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    7562497


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   OPRK1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    7562497


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   OPRM1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    7562497


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   ABCB1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15582917


    Sources:
    NCI

  • DEXTROMETHORPHAN   CYP2D6

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Combination therapy Dextromethorphan,Quinidine

    PMIDs:
    21422192


    Sources:
    DTC FDA

  • DEXTROMETHORPHAN   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12151071 9187528


    Sources:
    NCI PharmGKB

  • DrugBank: DB00514

    • Version: 5.1.7

    Alternate Names:
    DEXTROMETHORPHAN DrugBank Drug Name
    125-71-3 CAS Number
    12 Hour Cough Relief Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Categories alkaloids

    Publications:
    Lee et al., 2006, Effects of dextrorotatory morphinans on alpha3beta4 nicotinic acetylcholine receptors expressed in Xenopus oocytes., Eur. J. Pharmacol.
    Damaj et al., 2005, Effect of dextrometorphan and dextrorphan on nicotine and neuronal nicotinic receptors: in vitro and in vivo selectivity., J. Pharmacol. Exp. Ther.
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

  • TEND: DEXTROMETHORPHAN

    • Version: 01-August-2011

    Alternate Names:
    DEXTROMETHORPHAN Primary Drug Name

    Drug Info:
    Year of Approval approved before 1982
    Drug Class antitussive agents

    Publications:

  • TdgClinicalTrial: DEXTROMETHORPHAN

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antitussive agent
    Drug Class Small molecule
    FDA Approval approved

    Publications:

  • DTC: DEXTROMETHORPHAN

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL52440 ChEMBL Drug ID

    Drug Info:

    Publications:
    Nagy LD et al., 2011, Substituted imidazole of 5-fluoro-2-[4-[(2-phenyl-1H-imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine Inactivates cytochrome P450 2D6 by protein adduction., Drug Metab Dispos

  • NCI: DEXTROMETHORPHAN

    • Version: 14-September-2017

    Alternate Names:
    C423 NCI drug code

    Drug Info:

    Publications:
    Yin et al., 1999, Effect of dextromethorphan, a NMDA antagonist, on DNA repair in rat photochemical thrombotic cerebral ischemia., Brain Res.
    Vengurlekar et al., 2002, A sensitive LC-MS/MS assay for the determination of dextromethorphan and metabolites in human urine--application for drug interaction studies assessing potential CYP3A and CYP2D6 inhibition., J Pharm Biomed Anal
    Uhr et al., 2004, P-glycoprotein is a factor in the uptake of dextromethorphan, but not of melperone, into the mouse brain: evidence for an overlap in substrate specificity between P-gp and CYP2D6., J. Psychopharmacol. (Oxford)

  • PharmGKB: dextromethorphan

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev

  • TTD: Dextromethorphan

    • Version: 2020.06.01

    Alternate Names:
    D09OBB TTD Drug ID

    Drug Info:

    Publications:

  • GuideToPharmacology: 178103535

    • Version: 29-September-2020

    Alternate Names:
    DEXTROMETHORPHAN GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL52440

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Dextromethorphan

    • Version: 04-September-2020

    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.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2021-04-13