DGIdb - NALBUPHINE Drug Record

NALBUPHINE chembl:CHEMBL895 Approved

Alternate Names:

NUBAIN
NALBUPHINE
NUBAIN®
NALBUFINA
NALBUPHIN
NALBUPHINUM
N-CYCLOBUTYLMETHYL-4,5ALPHA-EPOXY-3,6ALPHA,14-MORPHINANTRIOL
rxcui:7238
drugbank:00844
chembl:CHEMBL895
chemidplus:20594-83-6
pubchem.compound:5311304

Drug Info:

Year of Approval	1979
Drug Class	analgesics, opioid
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	analgesic

(2 More Sources)

Publications:

Hoehe et al., 1993, Opiates increase plasma catecholamines in humans., Psychoneuroendocrinology
Tao et al., 2006, Nalbuphine is effective in decreasing the rewarding effect induced by morphine in rats., Drug Alcohol Depend
Picker, 1997, Discriminative stimulus effects of the mixed-opioid agonist/antagonist dezocine: cross-substitution by mu and delta opioid agonists., J. Pharmacol. Exp. Ther.
Peng et al., 2007, Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors., J. Med. Chem.
Meerpohl et al., 2008, [News from the cochrane library: mu opioid antagonists for opioid-induced bowel dysfunction]., Z Gastroenterol
Smith et al., 2009, The effects of repeated opioid administration on locomotor activity: I. Opposing actions of mu and kappa receptors., J. Pharmacol. Exp. Ther.
Mello et al., 2005, Effects of the mixed mu/kappa opioid nalbuphine on cocaine-induced changes in subjective and cardiovascular responses in men., Neuropsychopharmacology
McNicol et al., 2008, Mu-opioid antagonists for opioid-induced bowel dysfunction., Cochrane Database Syst Rev
Zernig et al., 1997, Clocinnamox inhibits the intravenous self-administration of opioid agonists in rhesus monkeys: comparison with effects on opioid agonist-mediated antinociception., Psychopharmacology (Berl.)
Kishioka et al., 2000, Diltiazem enhances the analgesic but not the respiratory depressant effects of morphine in rhesus monkeys., Eur. J. Pharmacol.
Béguin C et al., 2012, Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues., Bioorg Med Chem Lett
Chen et al., 2005, Dextromethorphan differentially affects opioid antinociception in rats., Br. J. Pharmacol.
Gear et al., 1999, The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain., Pain
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
De Souza et al., 1988, Nalbuphine: an autoradiographic opioid receptor binding profile in the central nervous system of an agonist/antagonist analgesic., J. Pharmacol. Exp. Ther.
Chen et al., 1993, The opioid receptor binding of dezocine, morphine, fentanyl, butorphanol and nalbuphine., Life Sci.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

NALBUPHINE OPRK1

Interaction Score: 1.79

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
22204910 15655510 8388112 16517095 10534607 17407276 19403853 15602503 17016423 17139284

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology TTD
NALBUPHINE OPRM1

Interaction Score: 1.11

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
8388112 16517095 9399970 17407276 18810678 19403853 15602503 18425947 9084061 10844102

Sources:
TdgClinicalTrial TEND GuideToPharmacology
NALBUPHINE OPRD1

Interaction Score: 0.98

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
2826773 8093631 11752352

Sources:
TdgClinicalTrial TEND GuideToPharmacology
NALBUPHINE CYP1A2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
NALBUPHINE CYP2D6

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
NALBUPHINE CYP3A4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC

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

NALBUPHINE Primary Drug Name

Drug Info:

Drug Class analgesics, opioid

Year of Approval 1979

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

Drug Info:

Drug Indications analgesic

Drug Class Small Molecule

FDA Approval approved

Publications:

DTC: NALBUPHINE

Version: 02-September-2020

Alternate Names:

CHEMBL895 ChEMBL Drug ID

Drug Info:

Publications:

Béguin C et al., 2012, Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues., Bioorg Med Chem Lett

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

GuideToPharmacology: 135650680
- Version: 29-September-2020
Alternate Names:

NALBUPHINE GuideToPharmacology Ligand Name

Drug Info:

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

D01KQA TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL895
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

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

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

agonist (activating)
antagonist (inhibitory)

agonist (activating)
antagonist (inhibitory)

NALBUPHINE Drug Record

NALBUPHINE chembl:CHEMBL895 Approved

Alternate Names:

Drug Info:

Publications:

NALBUPHINE OPRK1

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 22204910 15655510 8388112 16517095 10534607 17407276 19403853 15602503 17016423 17139284

Sources: DTC TdgClinicalTrial TEND GuideToPharmacology TTD

NALBUPHINE OPRM1

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

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

PMIDs: 8388112 16517095 9399970 17407276 18810678 19403853 15602503 18425947 9084061 10844102

Sources: TdgClinicalTrial TEND GuideToPharmacology

NALBUPHINE OPRD1

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

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

PMIDs: 2826773 8093631 11752352

Sources: TdgClinicalTrial TEND GuideToPharmacology

NALBUPHINE CYP1A2

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

NALBUPHINE CYP2D6

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

NALBUPHINE CYP3A4

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

TEND: NALBUPHINE

Alternate Names: NALBUPHINE Primary Drug Name

Drug Info: Drug Class analgesics, opioid Year of Approval 1979

Publications:

TdgClinicalTrial: NALBUPHINE

Alternate Names:

Drug Info: Drug Indications analgesic Drug Class Small Molecule FDA Approval approved

Publications:

DTC: NALBUPHINE

Alternate Names: CHEMBL895 ChEMBL Drug ID

Drug Info:

GuideToPharmacology: 135650680

Alternate Names: NALBUPHINE GuideToPharmacology Ligand Name

Drug Info:

Publications:

TTD: Nalbuphine

Alternate Names: D01KQA TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL895

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
22204910 15655510 8388112 16517095 10534607 17407276 19403853 15602503 17016423 17139284

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
8388112 16517095 9399970 17407276 18810678 19403853 15602503 18425947 9084061 10844102

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
2826773 8093631 11752352

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

Alternate Names:

NALBUPHINE Primary Drug Name

Drug Info:

Drug Class analgesics, opioid

Year of Approval 1979

Drug Info:

Drug Indications analgesic

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

CHEMBL895 ChEMBL Drug ID

Alternate Names:

NALBUPHINE GuideToPharmacology Ligand Name

Alternate Names:

D01KQA TTD Drug ID