Page last updated: 2024-11-06

Arbaclofen

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Arbaclofen is a novel, orally bioavailable, selective agonist of the GABAB receptor. It is under investigation for the treatment of pain, spasticity, and other neurological disorders. Arbaclofen's mechanism of action involves binding to the GABAB receptor, which is a G protein-coupled receptor that plays a role in regulating neuronal excitability. Upon activation, the GABAB receptor inhibits the release of excitatory neurotransmitters and activates potassium channels, leading to a reduction in neuronal activity. Arbaclofen has been shown to produce analgesic and anti-spastic effects in preclinical studies. Its potential therapeutic benefits have led to ongoing clinical trials for various conditions, including chronic pain, spinal cord injury, and multiple sclerosis. The research on Arbaclofen is driven by the need for safe and effective treatments for these debilitating disorders. Arbaclofen's selectivity for the GABAB receptor and its oral bioavailability make it a promising candidate for drug development.'

Cross-References

ID SourceID
PubMed CID44602
CHEMBL ID301742
CHEBI ID190735
SCHEMBL ID351220

Synonyms (74)

Synonym
bdbm50032964
4-amino-3-(4-chloro-phenyl)-butyric acid
(r)-4-amino-3-(4-chloro-phenyl)-butyric acid
HY-17354
p-chlorophenyl gaba
gtpl1064
c10h12clno2
NCGC00024796-01
tocris-0796
benzenepropanoic acid, beta-(aminomethyl)-4-chloro-, (r)-
benzeneporopanoic acid, (beta-(aminomethyl)-4-chloro-, (betar)-
d-baclofen
r-(-)-baclofen
(r)-(-)-baclofen
(-)-baclofen
(r)-4-amino-3-(4-chlorophenyl)butanoic acid
(r)-baclofen
stx-209
stx209
CHEMBL301742 ,
baclofen, r(-)-
baclofen (r)-form
baclofen, r-
baclofen, (r)-
69308-37-8
(3r)-4-amino-3-(4-chlorophenyl)butanoic acid
arbaclofen
CHEBI:190735
A9172
(3r)-4-azaniumyl-3-(4-chlorophenyl)butanoate
agi-006
unii-nyu6utw25b
stx 209
nyu6utw25b ,
arbaclofen [usan:inn]
r-baclofen ,
(r)-4-amino-3-(4-chlorophenyl)butanoicacid
D09791
arbaclofen (usan)
(r)-4-amino-3-(4-chlorophenyl)butyric acid
baclofen (r)-form [mi]
benzenepropanoic acid, .beta.-(aminomethyl)-4-chloro-, (r)-
arbaclofen [usan]
benzenepropanoic acid, .beta.-(aminomethyl)-4-chloro-, (.beta.r)-
arbaclofen [who-dd]
arbaclofen [inn]
(-)-(3r)-4-amino-3-(4-chlorophenyl)butanoic acid
CS-0889
AKOS015893035
S3072
[3h](r)-(-)-baclofen
gtpl3428
SCHEMBL351220
KPYSYYIEGFHWSV-QMMMGPOBSA-N
2c0 ,
DTXSID90219366
HB0952
AC-22385
AB01566870_01
mfcd01321057
sr-01000597441
SR-01000597441-1
C21605
(r)-4-amino-3-(4-chlorophenyl)butan-oic acid
DB08891
r-baclofen rs
m03bx01
(betar)-beta-(aminomethyl)-4-chlorobenzenepropanoic acid
Q27074844
B5102
CS-13178
AMY40581
CCG-266673
r-(+)-baclofen (free base)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
organooxygen compoundAn organochalcogen compound containing at least one carbon-oxygen bond.
organonitrogen compoundAny heteroorganic entity containing at least one carbon-nitrogen bond.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
USP1 protein, partialHomo sapiens (human)Potency7.94330.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency33.49830.000811.382244.6684AID686979
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency0.79430.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency2.51190.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency15.84890.00636.904339.8107AID883
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency15.84890.00638.235039.8107AID883
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid type B receptor subunit 2Rattus norvegicus (Norway rat)IC50 (µMol)0.08600.00001.01016.8100AID71400; AID71401
Gamma-aminobutyric acid type B receptor subunit 1Rattus norvegicus (Norway rat)IC50 (µMol)0.08600.00001.05326.8100AID71400; AID71401
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)EC50 (µMol)1.00000.53001.87365.3700AID729173
Gamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)EC50 (µMol)1.00000.07941.62765.3700AID729173
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
negative regulation of adenylate cyclase activityGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
neuron-glial cell signalingGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
osteoblast differentiationGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
negative regulation of cell population proliferationGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
positive regulation of glutamate secretionGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
negative regulation of gamma-aminobutyric acid secretionGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
negative regulation of epinephrine secretionGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
negative regulation of dopamine secretionGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
response to nicotineGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
response to ethanolGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
negative regulation of synaptic transmissionGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
positive regulation of growth hormone secretionGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
neuron-glial cell signalingGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
G protein-coupled GABA receptor activityGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
protein bindingGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
protein heterodimerization activityGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
transmembrane signaling receptor activityGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
G protein-coupled GABA receptor activityGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
G protein-coupled GABA receptor activityGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
protein bindingGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
protein heterodimerization activityGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
extracellular matrix protein bindingGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
cytoplasmGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
G protein-coupled GABA receptor complexGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
G protein-coupled receptor heterodimeric complexGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
GABA receptor complexGamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)
extracellular spaceGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
endoplasmic reticulum membraneGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
synaptic vesicleGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
axolemmaGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
mitochondrial membraneGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
presynaptic membraneGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
neuronal cell bodyGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
dendritic spineGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
dendritic shaftGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
Schaffer collateral - CA1 synapseGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
glutamatergic synapseGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
G protein-coupled GABA receptor complexGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
G protein-coupled receptor heterodimeric complexGamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (25)

Assay IDTitleYearJournalArticle
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID71552Inhibition of [3H]muscimol binding to Gamma-aminobutyric acid A (GABA-A) receptor of rat brain membranes1999Journal of medicinal chemistry, Jun-03, Volume: 42, Issue:11
Synthesis and pharmacology of the baclofen homologues 5-amino-4-(4-chlorophenyl)pentanoic acid and the R- and S-enantiomers of 5-amino-3-(4-chlorophenyl)pentanoic acid.
AID79363Sensitivity towards CGP-35348 in isolated longitudinal guinea pig ileum muscle; Sensitive1999Journal of medicinal chemistry, Jun-03, Volume: 42, Issue:11
Synthesis and pharmacology of the baclofen homologues 5-amino-4-(4-chlorophenyl)pentanoic acid and the R- and S-enantiomers of 5-amino-3-(4-chlorophenyl)pentanoic acid.
AID729172Agonist activity at rat GABA-A alpha1beta2gamma2 receptor expressed in human TSA201 cells by whole cell voltage-clamp method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Evaluation of difluoromethyl ketones as agonists of the γ-aminobutyric acid type B (GABAB) receptor.
AID71401Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortex1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
AID71997Inhibition of [3H]muscimol binding to GABA-A receptor of rat cortex1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
AID626684Induction of GABAB receptor-mediated GIRK currents in rat hippocampal pyramidal cell CA1 neurons by patch clamp electrophysiological method2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Discovery of a novel potent GABA(B) receptor agonist.
AID626682Agonist activity against human GABAB receptor expressed in HEK cells assessed as increase in cytoplasmic calcium level2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Discovery of a novel potent GABA(B) receptor agonist.
AID175654Deterioration of rotarod performance of rats 1.2 hour after subcutaneous administration of compound1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
AID175515Deterioration of rotarod performance of rats 0.5-1 hour after subcutaneous administration of compound1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
AID71258Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellum1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
AID71402Inhibitory concentration against binding of (R)-(-)-[3H]-baclofen to GABAB sites on rat whole brain synaptic membrane2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
QSAR and molecular modeling studies of baclofen analogues as GABA(B) agonists. Insights into the role of the aromatic moiety in GABA(B) binding and activation.
AID196573The compound was tested for inhibition of release of [3H]GABA from rat cortical slices after electrical stimulation.1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
AID71400Displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor1999Journal of medicinal chemistry, Jun-03, Volume: 42, Issue:11
Synthesis and pharmacology of the baclofen homologues 5-amino-4-(4-chlorophenyl)pentanoic acid and the R- and S-enantiomers of 5-amino-3-(4-chlorophenyl)pentanoic acid.
AID78843The compound was tested for inhibition of electrically evoked muscle contractions in isolated longitudinal guinea pig ileum muscle1999Journal of medicinal chemistry, Jun-03, Volume: 42, Issue:11
Synthesis and pharmacology of the baclofen homologues 5-amino-4-(4-chlorophenyl)pentanoic acid and the R- and S-enantiomers of 5-amino-3-(4-chlorophenyl)pentanoic acid.
AID88556The compound was tested for blockade of the monosynaptic reflexes in the hemisected neonatal spinal cord1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
AID626685Displacement of [3H]CGP54626 from rat GABAB receptor2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Discovery of a novel potent GABA(B) receptor agonist.
AID1237979Displacement of [3H]baclofen from GABA-B receptor in cat cerebellum2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Activation of the γ-Aminobutyric Acid Type B (GABA(B)) Receptor by Agonists and Positive Allosteric Modulators.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID233587Ratio of IC50 for GABA-B and GABA-A receptors1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
AID729173Agonist activity at human GABA-B B1/B2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 3 hrs by luciferase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Evaluation of difluoromethyl ketones as agonists of the γ-aminobutyric acid type B (GABAB) receptor.
AID626686Antihypothermic activity in CD1 mouse assessed as maximum temperature reduction at 24 mol/kg, ip measured every 15 mins up to 2 hrs and every 30 mins thereafter to 4 hrs2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Discovery of a novel potent GABA(B) receptor agonist.
AID1597739Half life in human at 5 mg administered three times in a day2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Sleep modulating agents.
AID1346001Rat GABAB1 (GABAB receptors)1997Nature, Mar-20, Volume: 386, Issue:6622
Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (9.09)18.7374
1990's3 (27.27)18.2507
2000's1 (9.09)29.6817
2010's4 (36.36)24.3611
2020's2 (18.18)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 43.13

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index43.13 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index5.35 (4.65)
Search Engine Demand Index57.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (43.13)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (18.18%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (81.82%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]