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69308-37-8 ((R)-Baclofen)

1

Identification

(R)-Baclofen (R)-Baclofen
Name (R)-Baclofen
Formula C10H12ClNO2
MW 213.66
CAS No. 69308-37-8
EINECS
Smiles ClC1=CC=C([[email protected]](CC(O)=O)([H])CN)C=C1
Synonyms STX 209;STX-209;STX209; (R)-4-amino-3-(4-chlorophenyl)butanoic acid
InChI InChI=1S/C10H12ClNO2/c11-9-3-1-7(2-4-9)8(6-12)5-10(13)14/h1-4,8H,5-6,12H2,(H,13,14)/t8-/m0/s1
2

Introduction

(R)-Baclofen(STX209) is a selective GABAB receptor agonist.

Background Information

(R)-baclofen is a racemic GABA(B) receptor agonist that has a number of significant pharmacokinetic limitations, including a narrow window of absorption in the upper small intestine and rapid clearance from the blood. (R)-baclofen is primarily used to treat spasticity. In clinical use, arbaclofen placarbil may improve the treatment of patients with gastroesophageal reflux disease, spasticity, and numerous other conditions by prolonging exposure and decreasing the fluctuations in plasma levels of R-baclofen. ......by AbMole BioScience
Arbaclofen, also known as (R)-Baclofen, D-Baclofen and STX209, is a selective GABA-B agonist and is hypothesized to modulate the balance of excitatory to inhibitory neurotransmission, and has shown preliminary evidence of benefit in fragile X syndrome. STX209 may be a potentially effective therapy to treat the core symptoms of FXS. Autism spectrum disorder (ASD) is a behaviorally defined disorder which has increased in prevalence over the last two decades. ......by MedKoo Biosciences, Inc.
A derivative of the neurotransmitter GABA that acts as a GABAB receptor agonist; also blocks α2δ subunit-containing voltage-dependent calcium channel (VDCC) with Ki of 156 uM; A neurotransmitter inhibitor by blocking the release of excitatory transmitters; serves as a central nervous system depressant and skeletal muscle relaxant.Other IndicationApproved ......by ProbeChem
(R)-baclofen is a derivative of gamma-aminobutyric acid primarily used to treat spasticity. ......by Selleck Chemicals LLC
(R)-baclofen is a derivative of gamma-aminobutyric acid primarily used to treat spasticity. ......by Target Molecule Corp.
More active enantiomer of (RS)-Baclofen, a selective GABAB agonist. Racemate also available. ......by Tocris Bioscience Inc.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000018144

Storage condition

Solubility

DMSO >10 mM Water >25 mM by MedChemexpress Co., Ltd.
(25°C) * In vitro Water 8 mg/mL (37.44 mM); DMSO<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM) by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
(R)-Baclofen Seaside Therapeutics Inc Autism 2011/11/30 2013/7/1 Phase 3 Clinical
(R)-Baclofen Seaside Therapeutics Inc Fragile X syndrome 2011/11/30 2013/7/1 Phase 3 Clinical
(R)-Baclofen Seaside Therapeutics Inc Fragile X syndrome 2011/6/30 2013/8/31 Phase 3 Clinical
(R)-Baclofen Seaside Therapeutics Inc Fragile X syndrome 2011/5/31 2013/2/28 Phase 3 Clinical
(R)-Baclofen Seaside Therapeutics Inc Autism 2011/5/31 2012/9/30 Phase 2 Clinical
(R)-Baclofen - Suspended
(R)-Baclofen - No Development Reported
7

Safety Data of (R)-Baclofen

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Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience 50mg/USD120(Out of stock) USA
Abcam 10mg/USD59() USA
Ark Pharm, Inc. USA
CHEMSCENE, LLC 10mg/USD60();50mg/USD216() USA
EMD Millipore 10mg/USD74() USA
Hello Bio Inc. 10mg/USD59() USA
MedChemexpress Co., Ltd. 10mg/USD60();50mg/USD216() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Santa Cruz Biotechnology, Inc. 10mg/USD50() USA
Selleck Chemicals LLC 10mg/USD97(In stock);50mg/USD310(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD60();50mg/USD216() China
Target Molecule Corp. 10mg/USD48();50mg/USD116() USA
Tocris Bioscience Inc. 10mg/USD89() USA
10

Related Products

Other Forms of 69308-37-8

Name CAS No Formula MW
(R)-Baclofen (hydrochloride) 63701-55-3 C10H13Cl2NO2 250.12

Recommended Compounds in GABA Receptor

Name CAS No Formula MW
Tiagabine (hydrochloride) 145821-59-6 C20H26ClNO2S2 412.01
alpha-Asarone 2883-98-9 C12H16O3 208.2536
Zopiclone 43200-80-2 C17H17ClN6O3 388.81
Tiagabine (hydrochloride) 145821-59-6 C20H26ClNO2S2 412.0089
Procaine (hydrochloride) 51-05-8 C13H21ClN2O2 272.77
Procaine 59-46-1 C13H20N2O2 236.31
Ginkgolide A 15291-75-5 C20H24O9 408.4
Nefiracetam 77191-36-7 C14H18N2O2 246.3
Primidone 125-33-7 C12H14N2O2 218.25
(R)-Baclofen (hydrochloride) 63701-55-3 C10H13Cl2NO2 250.12
Etomidate (hydrochloride) 53188-20-8 C14H17ClN2O2 280.75
Etomidate 33125-97-2 C14H16N2O2 244.29
(+)-Bicuculline 485-49-4 C20H17NO6 367.35
Zolpidem 82626-48-0 C19H21N3O 307.39
Etifoxine 21715-46-8 C17H17ClN2O 300.78
Etifoxine (hydrochloride) 56776-32-0 C17H18Cl2N2O 337.24
Clobazam 22316-47-8 C16H13ClN2O2 300.74
Vigabatrin (Hydrochloride) 1391054-02-6 C6H12ClNO2 165.62
Vigabatrin 68506-86-5 C6H11NO2 129.16
Acamprosate (calcium) 77337-73-6 C10H20CaN2O8S2 400.48

Recommended Compounds in Same Indication

Name CAS No Formula MW
Mavoglurant 543906-09-8 C19H23NO3 313.39
Bumetanide 28395-03-1 C17H20N2O5S 364.42
Ampalex 154235-83-3 C14H15N3O 241.29
Aripiprazole 129722-12-9 C23H27Cl2N3O2 448.39
Donepezil (Hydrochloride) 120011-70-3 C24H30ClNO3 415.95
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Route of Synthesis

12

References

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More Information

(R)-Baclofen

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