DGIdb - DEXTROMETHORPHAN Drug Record

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 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

(5 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)
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.
Church et al., 2005, Spreading depression expands traumatic injury in neocortical brain slices., J. Neurotrauma
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
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.
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
Wong et al., 1988, Dextrorphan and dextromethorphan, common antitussives, are antiepileptic and antagonize N-methyl-D-aspartate in brain slices., Neurosci. Lett.
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
Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
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
Yin et al., 1999, Effect of dextromethorphan, a NMDA antagonist, on DNA repair in rat photochemical thrombotic cerebral ischemia., Brain Res.

DEXTROMETHORPHAN SIGMAR1

Interaction Score: 9.11

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 15716633 11752352 17016423 17139284 10064839

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD
DEXTROMETHORPHAN ERCC6

Interaction Score: 6.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9974119

Sources:
NCI
DEXTROMETHORPHAN GRIN3A

Interaction Score: 2.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name AVP-923

Novel drug target Established target

Trial Name morphine/dextromethorphan,MorphiDex

PMIDs:
2897648 17016423 17139284 10064839 18812887

Sources:
TdgClinicalTrial TEND

DEXTROMETHORPHAN GRIN2C

Interaction Score: 0.27

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 ABCB1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15582917

Sources:
NCI
DEXTROMETHORPHAN CYP2D6

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Combination therapy Dextromethorphan,Quinidine

PMIDs:
21422192

Sources:
DTC FDA
DEXTROMETHORPHAN CYP3A4

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9187528 12151071

Sources:
NCI PharmGKB

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:

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

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

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

DEXTROMETHORPHAN Drug Record

DEXTROMETHORPHAN chembl:CHEMBL52440 Approved

Alternate Names:

Drug Info:

Publications:

DEXTROMETHORPHAN SIGMAR1

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 15716633 11752352 17016423 17139284 10064839

Sources: TdgClinicalTrial TEND GuideToPharmacology TTD

DEXTROMETHORPHAN ERCC6

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9974119

Sources: NCI

DEXTROMETHORPHAN GRIN3A

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 2897648 17016423 17139284 10064839 18812887

Sources: TdgClinicalTrial TEND

DEXTROMETHORPHAN GRIN2C

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 ABCB1

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15582917

Sources: NCI

DEXTROMETHORPHAN CYP2D6

Interaction Types & Directionality: n/a

Interaction Info: Combination therapy Dextromethorphan,Quinidine

PMIDs: 21422192

Sources: DTC FDA

DEXTROMETHORPHAN CYP3A4

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9187528 12151071

Sources: NCI PharmGKB

TEND: DEXTROMETHORPHAN

Alternate Names: DEXTROMETHORPHAN Primary Drug Name

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

Publications:

TdgClinicalTrial: DEXTROMETHORPHAN

Alternate Names:

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

Publications:

DTC: DEXTROMETHORPHAN

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

Alternate Names: C423 NCI drug code

Drug Info:

PharmGKB: dextromethorphan

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

Alternate Names: D09OBB TTD Drug ID

Drug Info:

Publications:

GuideToPharmacology: 178103535

Alternate Names: DEXTROMETHORPHAN GuideToPharmacology Ligand Name

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL52440

Alternate Names:

Drug Info:

Publications:

FDA: Dextromethorphan

Alternate Names:

Drug Info:

Publications:

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 15716633 11752352 17016423 17139284 10064839

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

PMIDs:
9974119

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name AVP-923

Novel drug target Established target

Trial Name morphine/dextromethorphan,MorphiDex

PMIDs:
2897648 17016423 17139284 10064839 18812887

Sources:
TdgClinicalTrial TEND

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

Interaction Types & Directionality:

n/a

PMIDs:
15582917

Sources:
NCI

Interaction Types & Directionality:

n/a

Interaction Info:

Combination therapy Dextromethorphan,Quinidine

PMIDs:
21422192

Sources:
DTC FDA

Interaction Types & Directionality:

n/a

PMIDs:
9187528 12151071

Sources:
NCI PharmGKB

Alternate Names:

DEXTROMETHORPHAN Primary Drug Name

Drug Info:

Year of Approval approved before 1982

Drug Class antitussive agents

Drug Info:

Drug Indications antitussive agent

Drug Class Small molecule

FDA Approval approved

Alternate Names:

CHEMBL52440 ChEMBL Drug ID

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

Alternate Names:

C423 NCI drug code

Publications:

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

Alternate Names:

D09OBB TTD Drug ID

Alternate Names:

DEXTROMETHORPHAN GuideToPharmacology Ligand Name