DGIdb - PROPOXYPHENE Drug Record

PROPOXYPHENE chembl:CHEMBL1213351

Alternate Names:

PROPOXYPHENE
DEXTROPROPOXYPHENE
LEVOPROPOXYPHENE
DEXTROPROPOXYPHENUM
(+)-1,2-DIPHENYL-2-PROPIONOXY-3-METHYL-4-DIMETHYLAMINOBUTANE
(S)-ALPHA-(2-(DIMETHYLAMINO)-1-METHYLETHYL)-ALPHA-PHENYLBENZENEETHANOL PROPANOATE
DEXTROPROPOXYPHEN
4-DIMETHYLAMINO-3-METHYL-1,2-DIPHENYL-2-PROPOXYBUTANE
DESTROPROPOSSIFENE
(+)-ALPHA-PROPOXYPHENE
DEXTROPROPOXYPHÈNE
ALPHA-D-4-DIMETHYLAMINO-3-METHYL-1,2-DIPHENYL-2-BUTANOL-PROPIONAT
ALPHA-(+)-4-DIMETHYLAMINO-1,2-DIPHENYL-3-METHYL-2-BUTANOL PROPIONATE ESTER
DEXTROPROPOXIFENO
(+)-4-DIMETHYLAMINO-1,2-DIPHENYL-3-METHYL-2-PROPIONYLOXYBUTANE
DARVON®
D-PROPOXYPHENE
chembl:CHEMBL1213351
chemidplus:469-62-5
rxcui:8785
pubchem.compound:10100
drugbank:00647

Drug Info:

FDA Approval	Approved before 1982
Drug Class	small molecule
Drug Indications	Antitussive Agents
Drug Indications	Analgesics, Opioid
Drug Class	antitussive agents
Drug Class	analgesics, opioid
Year of Approval	approved before 1982
Drug Categories	diphenylpropylamine derivatives
Drug Groups	investigational
Drug Categories	agents that reduce seizure threshold
Drug Categories	cytochrome p-450 cyp2d6 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2d6 substrates
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	high-risk opioids
Drug Categories	opioid agonist
Drug Categories	opioids
Drug Categories	serotonergic drugs shown to increase risk of serotonin syndrome

(3 More Sources)

Publications:

Ulens et al., 1999, Norpropoxyphene-induced cardiotoxicity is associated with changes in ion-selectivity and gating of HERG currents., Cardiovasc. Res.
Tyers, 1980, A classification of opiate receptors that mediate antinociception in animals., Br. J. Pharmacol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Walker et al., 1999, Naltrexone and beta-funaltrexamine antagonism of the antinociceptive and response rate-decreasing effects of morphine, dezocine, and d-propoxyphene., Psychopharmacology (Berl.)
Bannwarth et al., 2009, The dextropropoxyphene controversy., Joint Bone Spine
Picker, 1997, Discriminative stimulus effects of the mixed-opioid agonist/antagonist dezocine: cross-substitution by mu and delta opioid agonists., J. Pharmacol. Exp. Ther.
Codd et al., 1995, Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception., J. Pharmacol. Exp. Ther.
Neil, 1984, Affinities of some common opioid analgesics towards four binding sites in mouse brain., Naunyn Schmiedebergs Arch. Pharmacol.
Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem
Yin OQ et al., 2010, CYP3A5 but not CYP2D6 polymorphism contributes significantly to the variability in dextropropoxyphene disposition., J Clin Pharmacol
Zhang J et al., 1999, Binding and hydrolysis of meperidine by human liver carboxylesterase hCE-1., J Pharmacol Exp Ther

PROPOXYPHENE CES1

Interaction Score: 0.95

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10381793

Sources:
DrugBank
PROPOXYPHENE OPRM1

Interaction Score: 0.78

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10690289 6249436 11752352 10379623 19604717 9399970 7562497

Sources:
TEND TdgClinicalTrial DrugBank
PROPOXYPHENE OPRD1

Interaction Score: 0.55

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6151117

Sources:
TEND TdgClinicalTrial DrugBank
PROPOXYPHENE OPRK1

Interaction Score: 0.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6151117 11752352

Sources:
TEND TdgClinicalTrial DrugBank
PROPOXYPHENE CYP3A5

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18695978 20133509

Sources:
PharmGKB

DrugBank: DB00647

Version: 5.1.7

Alternate Names:

DEXTROPROPOXYPHENE DrugBank Drug Name

469-62-5 CAS Number

642 Tab Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups illicit

Publications:

Neil, 1984, Affinities of some common opioid analgesics towards four binding sites in mouse brain., Naunyn Schmiedebergs Arch. Pharmacol.

Ulens et al., 1999, Norpropoxyphene-induced cardiotoxicity is associated with changes in ion-selectivity and gating of HERG currents., Cardiovasc. Res.

Tyers, 1980, A classification of opiate receptors that mediate antinociception in animals., Br. J. Pharmacol.

TdgClinicalTrial: PROPOXYPHENE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications Analgesics, Opioid

Drug Indications Antitussive Agents

Drug Class small molecule

Publications:
TEND: PROPOXYPHENE
- Version: 01-August-2011
Alternate Names:

Drug Info:

Year of Approval approved before 1982

Drug Class analgesics, opioid

Drug Class antitussive agents

Publications:
PharmGKB: dextropropoxyphene
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Yin OQ et al., 2010, CYP3A5 but not CYP2D6 polymorphism contributes significantly to the variability in dextropropoxyphene disposition., J Clin Pharmacol
PharmGKB: propoxyphene
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem
TTD: Dextropropoxyphene
- Version: 2020.06.01
Alternate Names:

D0D4PB TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1213351
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

DEXTROPROPOXYPHENE	DrugBank Drug Name
469-62-5	CAS Number
642 Tab	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	illicit

Trial Name	-
Novel drug target	Established target

Trial Name	-
Novel drug target	Established target

Trial Name	-
Novel drug target	Established target

PROPOXYPHENE Drug Record

PROPOXYPHENE chembl:CHEMBL1213351

Alternate Names:

Drug Info:

Publications:

PROPOXYPHENE CES1

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10381793

Sources: DrugBank

PROPOXYPHENE OPRM1

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10690289 6249436 11752352 10379623 19604717 9399970 7562497

Sources: TEND TdgClinicalTrial DrugBank

PROPOXYPHENE OPRD1

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 6151117

Sources: TEND TdgClinicalTrial DrugBank

PROPOXYPHENE OPRK1

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 6151117 11752352

Sources: TEND TdgClinicalTrial DrugBank

PROPOXYPHENE CYP3A5

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18695978 20133509

Sources: PharmGKB

DrugBank: DB00647

Alternate Names: DEXTROPROPOXYPHENE DrugBank Drug Name 469-62-5 CAS Number 642 Tab Drug Brand

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

TdgClinicalTrial: PROPOXYPHENE

Alternate Names:

Drug Info: Drug Indications Analgesics, Opioid Drug Indications Antitussive Agents Drug Class small molecule

Publications:

TEND: PROPOXYPHENE

Alternate Names:

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

Publications:

PharmGKB: dextropropoxyphene

Alternate Names:

Drug Info:

Publications: Yin OQ et al., 2010, CYP3A5 but not CYP2D6 polymorphism contributes significantly to the variability in dextropropoxyphene disposition., J Clin Pharmacol

PharmGKB: propoxyphene

Alternate Names:

Drug Info:

Publications: Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem

TTD: Dextropropoxyphene

Alternate Names: D0D4PB TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL1213351

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
10381793

Sources:
DrugBank

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10690289 6249436 11752352 10379623 19604717 9399970 7562497

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6151117

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6151117 11752352

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
18695978 20133509

Sources:
PharmGKB

Alternate Names:

DEXTROPROPOXYPHENE DrugBank Drug Name

469-62-5 CAS Number

642 Tab Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups illicit

Drug Info:

Drug Indications Analgesics, Opioid

Drug Indications Antitussive Agents

Drug Class small molecule

Drug Info:

Year of Approval approved before 1982

Drug Class analgesics, opioid

Drug Class antitussive agents

Publications:

Yin OQ et al., 2010, CYP3A5 but not CYP2D6 polymorphism contributes significantly to the variability in dextropropoxyphene disposition., J Clin Pharmacol

Publications:

Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem

Alternate Names:

D0D4PB TTD Drug ID