DGIdb - ARBACLOFEN Drug Record

ARBACLOFEN chembl:CHEMBL301742

Alternate Names:

STX209
BACLOFEN (R)-FORM
STX-209
ARBACLOFEN
(R)-(-)-BACLOFEN
(R)-4-AMINO-3-(4-CHLOROPHENYL)BUTANOIC ACID
P-CHLOROPHENYL GABA
(R)-BACLOFEN
chemidplus:69308-37-8
drugbank:08891
chembl:CHEMBL301742
pubchem.compound:44602

Drug Info:

FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	symptomatic treatment for fragile X syndrome

(0 More Sources)

Publications:

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.
Lehmann, 2009, GABAB receptors as drug targets to treat gastroesophageal reflux disease., Pharmacol. Ther.
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.
Pittman, 1999, The action is at the terminal., J. Physiol. (Lond.)
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.
Bowery, 1993, GABAB receptor pharmacology., Annu. Rev. Pharmacol. Toxicol.
Jones et al., 2000, Signal transduction by GABA(B) receptor heterodimers., Neuropsychopharmacology
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.
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.

ARBACLOFEN GABBR2

Interaction Score: 30.91

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name Arbaclofen

Novel drug target Established target

Direct Interaction yes

PMIDs:
15235087 10658574 19303900 10328880 10545129 10751439 8388192 11008066

Sources:
TdgClinicalTrial ChemblInteractions
ARBACLOFEN GABBR1

Interaction Score: 24.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name Arbaclofen

Mechanism of Interaction GABA-B receptor agonist

PMIDs:
10386831 10482760 10444662 10094428 19303900 10545129 8388192 11752352 10494996

Sources:
TdgClinicalTrial ChemblInteractions
ARBACLOFEN CYP2C19

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ARBACLOFEN CYP2D6

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

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

Drug Info:

Drug Indications symptomatic treatment for fragile X syndrome

Drug Class Small molecule

FDA Approval not approved

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

CHEMBL301742 ChEMBL Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL301742
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL301742
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Trial Name	Arbaclofen
Novel drug target	Established target
Direct Interaction	yes

ARBACLOFEN Drug Record

ARBACLOFEN chembl:CHEMBL301742

Alternate Names:

Drug Info:

Publications:

ARBACLOFEN GABBR2

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name Arbaclofen Novel drug target Established target Direct Interaction yes

PMIDs: 15235087 10658574 19303900 10328880 10545129 10751439 8388192 11008066

Sources: TdgClinicalTrial ChemblInteractions

ARBACLOFEN GABBR1

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 10386831 10482760 10444662 10094428 19303900 10545129 8388192 11752352 10494996

Sources: TdgClinicalTrial ChemblInteractions

ARBACLOFEN CYP2C19

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

ARBACLOFEN CYP2D6

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

TdgClinicalTrial: ARBACLOFEN

Alternate Names:

Drug Info: Drug Indications symptomatic treatment for fragile X syndrome Drug Class Small molecule FDA Approval not approved

Publications:

DTC: ARBACLOFEN

Alternate Names: CHEMBL301742 ChEMBL Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL301742

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL301742

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name Arbaclofen

Novel drug target Established target

Direct Interaction yes

PMIDs:
15235087 10658574 19303900 10328880 10545129 10751439 8388192 11008066

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name Arbaclofen

Mechanism of Interaction GABA-B receptor agonist

PMIDs:
10386831 10482760 10444662 10094428 19303900 10545129 8388192 11752352 10494996

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Drug Info:

Drug Indications symptomatic treatment for fragile X syndrome

Drug Class Small molecule

FDA Approval not approved

Alternate Names:

CHEMBL301742 ChEMBL Drug ID