DGIdb - BUTORPHANOL Drug Record

BUTORPHANOL chembl:CHEMBL33986 Approved

Alternate Names:

BUTORPHANOL
LEVO-BC-2627
(-)-N-CYCLOBUTYLMETHYL-3,14-DIHYDROXYMORPHINAN
BUTORFANOL
(-)-BUTORPHANOL
BUTORPHANOLUM
(-)-17-(CYCLOBUTYLMETHYL)MORPHINAN-3,14-DIOL
BUTORPHANOL TARTRATE
rxcui:1841
pubchem.compound:5361092
chembl:CHEMBL33986
drugbank:00611
chemidplus:42408-82-2

Drug Info:

Drug Class	analgesics, opioid
Year of Approval	1978
FDA Approval	1978
Drug Class	small molecule
Drug Indications	Analgesics, Opioid

(2 More Sources)

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
Fan et al., 2002, Withdrawal from dependence upon butorphanol uniquely increases kappa(1)-opioid receptor binding in the rat brain., Brain Res. Bull.
Picker, 1997, Discriminative stimulus effects of the mixed-opioid agonist/antagonist dezocine: cross-substitution by mu and delta opioid agonists., J. Pharmacol. Exp. Ther.
Vivian et al., 1999, kappa-Opioid receptor effects of butorphanol in rhesus monkeys., J. Pharmacol. Exp. Ther.
Fan et al., 2002, Butorphanol dependence and withdrawal decrease hippocampal kappa 2-opioid receptor binding., Brain Res.
Picker et al., 1996, Discriminative stimulus effects of butorphanol: influence of training dose on the substitution patterns produced by Mu, Kappa and Delta opioid agonists., J. Pharmacol. Exp. Ther.
Walsh et al., 2008, Evaluation of the mu and kappa opioid actions of butorphanol in humans through differential naltrexone blockade., Psychopharmacology (Berl.)
Narita et al., 1994, Repeated administration of opioids alters characteristics of membrane-bound phorbol ester binding in rat brain., Eur. J. Pharmacol.
Commiskey et al., 2005, Butorphanol: effects of a prototypical agonist-antagonist analgesic on kappa-opioid receptors., J. Pharmacol. Sci.
Wakabayashi et al., 1995, Simultaneous measurement of biogenic amines and their metabolites in rat brain regions after acute administration of and abrupt withdrawal from butorphanol or morphine., Neurochem. Res.
Ohta et al., 1989, [Kappa-type opioid receptor in human placental membrane]., Masui
Park et al., 2000, kappa-opioid agonist stimulated regional distribution of [(35)S]GTPgammas binding in butorphanol continuously infused rat., Brain Res. Bull.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

BUTORPHANOL OPRD1

Interaction Score: 1.54

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12127012 8968334 12470863 17909753 7705457 15942128 11752352 8746803

Sources:
TdgClinicalTrial TEND TTD
BUTORPHANOL OPRK1

Interaction Score: 1.33

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

Details of the Assay for Interaction Displacement of [<sup>3</sup>H]U69593 from human κ opioid receptor expressed in CHO cells.

PMIDs:
12127012 10381785 12470863 8968334 17909753 2555580 7705457 15942128 8746803 10779697

Sources:
TdgClinicalTrial TEND GuideToPharmacology
BUTORPHANOL OPRM1

Interaction Score: 0.88

Interaction Types & Directionality:

agonist (activating)

partial antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
12127012 9399970 10381785 12470863 8968334 17909753 7705457 15942128 8746803

Sources:
TdgClinicalTrial TEND GuideToPharmacology
BUTORPHANOL CYP2C9

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
BUTORPHANOL CYP2C19

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
BUTORPHANOL CYP1A2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
BUTORPHANOL CYP3A4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC

TEND: BUTORPHANOL
- Version: 01-August-2011
Alternate Names:

BUTORPHANOL Primary Drug Name

Drug Info:

Year of Approval 1978

Drug Class analgesics, opioid

Publications:
TdgClinicalTrial: BUTORPHANOL
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications Analgesics, Opioid

Drug Class small molecule

FDA Approval 1978

Publications:
DTC: BUTORPHANOL
- Version: 02-September-2020
Alternate Names:

CHEMBL33986 ChEMBL Drug ID

Drug Info:

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
GuideToPharmacology: 223365926
- Version: 29-September-2020
Alternate Names:

BUTORPHANOL GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Butorphanol
- Version: 2020.06.01
Alternate Names:

D0X9RG TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL33986
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Novel drug target	Established target
Trial Name	-
Details of the Assay for Interaction	Displacement of [<sup>3</sup>H]U69593 from human κ opioid receptor expressed in CHO cells.

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

agonist (activating)
partial antagonist (inhibitory)

BUTORPHANOL Drug Record

BUTORPHANOL chembl:CHEMBL33986 Approved

Alternate Names:

Drug Info:

Publications:

BUTORPHANOL OPRD1

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 12127012 8968334 12470863 17909753 7705457 15942128 11752352 8746803

Sources: TdgClinicalTrial TEND TTD

BUTORPHANOL OPRK1

Interaction Types & Directionality: agonist (activating)

Interaction Info: Novel drug target Established target Trial Name - Details of the Assay for Interaction Displacement of [<sup>3</sup>H]U69593 from human &kappa; opioid receptor expressed in CHO cells.

PMIDs: 12127012 10381785 12470863 8968334 17909753 2555580 7705457 15942128 8746803 10779697

Sources: TdgClinicalTrial TEND GuideToPharmacology

BUTORPHANOL OPRM1

Interaction Types & Directionality: agonist (activating) partial antagonist (inhibitory)

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

PMIDs: 12127012 9399970 10381785 12470863 8968334 17909753 7705457 15942128 8746803

Sources: TdgClinicalTrial TEND GuideToPharmacology

BUTORPHANOL CYP2C9

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

BUTORPHANOL CYP2C19

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

BUTORPHANOL CYP1A2

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

BUTORPHANOL CYP3A4

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

TEND: BUTORPHANOL

Alternate Names: BUTORPHANOL Primary Drug Name

Drug Info: Year of Approval 1978 Drug Class analgesics, opioid

Publications:

TdgClinicalTrial: BUTORPHANOL

Alternate Names:

Drug Info: Drug Indications Analgesics, Opioid Drug Class small molecule FDA Approval 1978

Publications:

DTC: BUTORPHANOL

Alternate Names: CHEMBL33986 ChEMBL Drug ID

Drug Info:

Publications: Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for &gt;200 compounds., Chem Res Toxicol

GuideToPharmacology: 223365926

Alternate Names: BUTORPHANOL GuideToPharmacology Ligand Name

Drug Info:

Publications:

TTD: Butorphanol

Alternate Names: D0X9RG TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL33986

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12127012 8968334 12470863 17909753 7705457 15942128 11752352 8746803

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

Details of the Assay for Interaction Displacement of [<sup>3</sup>H]U69593 from human κ opioid receptor expressed in CHO cells.

PMIDs:
12127012 10381785 12470863 8968334 17909753 2555580 7705457 15942128 8746803 10779697

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

partial antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
12127012 9399970 10381785 12470863 8968334 17909753 7705457 15942128 8746803

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Alternate Names:

BUTORPHANOL Primary Drug Name

Drug Info:

Year of Approval 1978

Drug Class analgesics, opioid

Drug Info:

Drug Indications Analgesics, Opioid

Drug Class small molecule

FDA Approval 1978

Alternate Names:

CHEMBL33986 ChEMBL Drug ID

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

Alternate Names:

BUTORPHANOL GuideToPharmacology Ligand Name

Alternate Names:

D0X9RG TTD Drug ID