DGIdb - BACLOFEN Drug Record

BACLOFEN chembl:CHEMBL701 Approved

Alternate Names:

KEMSTRO
LYFLEX
LIORESAL
BA-34647
LIORESAL INTRATH
BACLOSPAS-10
GABLOFEN
BACLOFEN

Drug Info:

Year of Approval	1977
Drug Class	muscle relaxants
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	for treatment of alcohol dependance

(3 More Sources)

Publications:

Seifert et al., 1998, Effects of baclofen on the Hering-Breuer inspiratory-inhibitory and deflation reflexes in rats., Am. J. Physiol.
Parramón et al., 1995, GABAB receptors increase intracellular calcium concentrations in chromaffin cells through two different pathways: their role in catecholamine secretion., J. Neurosci. Res.
Garcia-Gil et al., Perinatal delta9-tetrahydrocannabinol exposure augmented the magnitude of motor inhibition caused by GABA(B), but not GABA(A), receptor agonists in adult rats., Neurotoxicol Teratol
Mott et al., 1999, GABAB-Receptor-mediated currents in interneurons of the dentate-hilus border., J. Neurophysiol.
Motalli et al., 1999, GABA(B) receptor activation promotes seizure activity in the juvenile rat hippocampus., J. Neurophysiol.
Stringer et al., 1999, The reduction in paired-pulse inhibition in the rat hippocampus by gabapentin is independent of GABA(B) receptor receptor activation., Epilepsy Res.
Lehmann, 2009, GABAB receptors as drug targets to treat gastroesophageal reflux disease., Pharmacol. Ther.
Pittman, 1999, The action is at the terminal., J. Physiol. (Lond.)
Bowery, 1993, GABAB receptor pharmacology., Annu. Rev. Pharmacol. Toxicol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Ogasawara et al., 1999, Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer., Pharmacol. Biochem. Behav.
Fu Z et al., 2012, The γ-aminobutyric acid type B (GABAB) receptor agonist baclofen inhibits morphine sensitization by decreasing the dopamine level in rat nucleus accumbens., Behav Brain Funct
Chen K et al., 2005, Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro., Brain Res Bull
Takemura et al., 2001, GABA B receptor-mediated effects on expression of c-Fos in rat trigeminal nucleus following high- and low-intensity afferent stimulation., Neuroscience
Braun et al., 2004, GABAB receptor activation inhibits exocytosis in rat pancreatic beta-cells by G-protein-dependent activation of calcineurin., J. Physiol. (Lond.)
Belley et al., 1999, Synthesis of the nanomolar photoaffinity GABA(B) receptor ligand CGP 71872 reveals diversity in the tissue distribution of GABA(B) receptor forms., Bioorg. Med. Chem.
Martin et al., 1999, Molecular identification of the human GABABR2: cell surface expression and coupling to adenylyl cyclase in the absence of GABABR1., Mol. Cell. Neurosci.
Filippov et al., 2000, Heteromeric assembly of GABA(B)R1 and GABA(B)R2 receptor subunits inhibits Ca(2+) current in sympathetic neurons., J. Neurosci.
Jones et al., 2000, Signal transduction by GABA(B) receptor heterodimers., Neuropsychopharmacology
Rawls et al., 2006, Baclofen and NOS inhibitors interact to evoke synergistic hypothermia in rats., Life Sci.
Rawls et al., 2004, Pronounced hypothermic synergy between systemic baclofen and NOS inhibitor., Eur. J. Pharmacol.
Passariello et al., 1982, A possible role of gamma-aminobutyric acid in the control of the endocrine pancreas., J. Clin. Endocrinol. Metab.
Mizoguchi et al., 2006, BDNF occludes GABA receptor-mediated inhibition of GABA release in rat hippocampal CA1 pyramidal neurons., Eur. J. Neurosci.
Rey-Roldán et al., 1997, In vivo interaction of baclofen, TRH and serotonin on PRL and TSH secretion in the developing and adult male and female rats., Life Sci.
Hwang et al., 1989, Baclofen, gamma-aminobutyric acidB receptors and substance P in the mouse spinal cord., J. Pharmacol. Exp. Ther.

BACLOFEN GABBR2

Interaction Score: 16.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name ALKS 29

Novel drug target Established target

Mechanism of Interaction GABA-B receptor agonist

PMIDs:
15235087 10658574 19303900 10328880 10545129 10751439 8388192 11008066 22559224 16182939

Sources:
TdgClinicalTrial ChemblInteractions TEND
BACLOFEN GABBR1

Interaction Score: 15.02

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name ALKS 29

Novel drug target Established target

Mechanism of Interaction GABA-B receptor agonist

PMIDs:
9486305 7674378 10386831 10482760 10444662 10094428 19303900 10545129 8388192 11752352 10494996 22559224 16182939

Sources:
TdgClinicalTrial ChemblInteractions NCI TEND
BACLOFEN FOS

Interaction Score: 1.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11301212

Sources:
NCI
BACLOFEN TSHB

Interaction Score: 1.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9408051

Sources:
NCI
BACLOFEN GCG

Interaction Score: 0.77

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7042732

Sources:
NCI
BACLOFEN TAC1

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2467977

Sources:
NCI
BACLOFEN NOS1

Interaction Score: 0.49

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16137704 15476754

Sources:
NCI
BACLOFEN BDNF

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17074039

Sources:
NCI
BACLOFEN NFKB1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
BACLOFEN NFE2L2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

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

Drug Info:

Drug Indications for treatment of alcohol dependance

Drug Class Small Molecule

FDA Approval approved

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

Drug Info:

Drug Class muscle relaxants

Year of Approval 1977

Publications:

NCI: BACLOFEN

Version: 14-September-2017

Alternate Names:

C28858 NCI drug code

Drug Info:

Publications:

Parramón et al., 1995, GABAB receptors increase intracellular calcium concentrations in chromaffin cells through two different pathways: their role in catecholamine secretion., J. Neurosci. Res.

Seifert et al., 1998, Effects of baclofen on the Hering-Breuer inspiratory-inhibitory and deflation reflexes in rats., Am. J. Physiol.

Hwang et al., 1989, Baclofen, gamma-aminobutyric acidB receptors and substance P in the mouse spinal cord., J. Pharmacol. Exp. Ther.

DTC: BACLOFEN
- Version: 02-September-2020
Alternate Names:

CHEMBL701 ChEMBL Drug ID

Drug Info:

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

D01AJY TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL701
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL701
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Trial Name	ALKS 29
Novel drug target	Established target
Mechanism of Interaction	GABA-B receptor agonist

BACLOFEN Drug Record

BACLOFEN chembl:CHEMBL701 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name ALKS 29 Novel drug target Established target Mechanism of Interaction GABA-B receptor agonist

PMIDs: 15235087 10658574 19303900 10328880 10545129 10751439 8388192 11008066 22559224 16182939

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name ALKS 29 Novel drug target Established target Mechanism of Interaction GABA-B receptor agonist

PMIDs: 9486305 7674378 10386831 10482760 10444662 10094428 19303900 10545129 8388192 11752352 10494996 22559224 16182939

Sources: TdgClinicalTrial ChemblInteractions NCI TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11301212

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9408051

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 7042732

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2467977

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16137704 15476754

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17074039

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

TdgClinicalTrial: BACLOFEN

Alternate Names:

Drug Info: Drug Indications for treatment of alcohol dependance Drug Class Small Molecule FDA Approval approved

Publications:

TEND: BACLOFEN

Alternate Names:

Drug Info: Drug Class muscle relaxants Year of Approval 1977

Publications:

NCI: BACLOFEN

Alternate Names: C28858 NCI drug code

Drug Info:

DTC: BACLOFEN

Alternate Names: CHEMBL701 ChEMBL Drug ID

Drug Info:

Publications:

TTD: Baclofen

Alternate Names: D01AJY TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL701

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL701

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name ALKS 29

Novel drug target Established target

Mechanism of Interaction GABA-B receptor agonist

PMIDs:
15235087 10658574 19303900 10328880 10545129 10751439 8388192 11008066 22559224 16182939

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name ALKS 29

Novel drug target Established target

Mechanism of Interaction GABA-B receptor agonist

PMIDs:
9486305 7674378 10386831 10482760 10444662 10094428 19303900 10545129 8388192 11752352 10494996 22559224 16182939

Sources:
TdgClinicalTrial ChemblInteractions NCI TEND

Interaction Types & Directionality:

n/a

PMIDs:
11301212

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
9408051

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
7042732

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
2467977

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16137704 15476754

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
17074039

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Drug Info:

Drug Indications for treatment of alcohol dependance

Drug Class Small Molecule

FDA Approval approved

Drug Info:

Drug Class muscle relaxants

Year of Approval 1977

Alternate Names:

C28858 NCI drug code

Alternate Names:

CHEMBL701 ChEMBL Drug ID

Alternate Names:

D01AJY TTD Drug ID