(R)-Baclofen

(HB0952)
Technical documents: SDS CoA Datasheet

Product overview

Name (R)-Baclofen
Description Selective GABAB receptor agonist
Biological description

Active enantiomer of (RS)-Baclofen. Selective GABAB receptor agonist. Decreases ethanol intake in addiction models. Shows anti-cataplexy actions and promotes sleep. Blood-brain barrier permeable.

Alternative names STX 209
Purity >99%
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Images

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Biological Data

Application notes

The GABABB receptor agonist (R)–Baclofen is commonly used at concentrations of 1–50 µM. It can be used to target presynaptic GABAB receptors to inhibit neurotransmitter release. At the Schaffer collateral pathway of the hippocampus, (R)–Baclofen from Hello Bio (applied at 10 µM) led to a reversible reduction in presynaptic glutamate release This was demonstrated as a reduced EPSC amplitude and increase in the amplitude ratio of a 50 ms paired pulse stimulation (see Fig 1 above).

 

#Protocol 1: Assay evoked EPSCs (used for baclofen)

  • Whole cell voltage clamp recordings of CA1 pyramidal neurons from the rat hippocampal brain slice.
  • 50 ms paired EPSCs were evoked via stimulating electrode placed in the CA3 region to stimulate the Schaffer collateral pathway delivering two square (150 µs) pulse with a 50 ms interval every 10 sec at an intensity that gave a reliable EPSC.
  • Neurons were held at -60 mV (the reversal potential of GABA currents).
  • Paired EPSCs were continually stimulated and recorded in response to applications of baclofen until a maximum effect was achieved at which point baclofen was washed out with control solution.
  • EPSC amplitudes were taken from the amplitude of the first pulse and paired pulse ratios calculated by dividing the amplitude of pulse 2 by pulse 1 (P2/P1).

Solubility & Handling

Storage instructions Room temperature
Solubility overview Soluble in water (20mM) and in DMSO (10mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Dilution

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Chemical Data

Chemical name (R)-4-Amino-3-(4-chlorophenyl)butanoic acid
Molecular Weight 213.66
Chemical structure Product image
Molecular Formula C10H12ClNO2
CAS Number 69308-37-8
PubChem identifier 44602
SMILES C1=CC(=CC=C1[C@@H](CC(=O)O)CN)Cl
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
InChiKey KPYSYYIEGFHWSV-QMMMGPOBSA-N
MDL number MFCD01321057
Appearance White solid

References for (R)-Baclofen

References are publications that support the biological activity of the product
  • Intra-nucleus accumbens shell injections of R(+)- and S(-)-baclofen bidirectionally alter binge-like ethanol, but not saccharin, intake in C57Bl/6J mice.

    Kasten CR et al (2014) Behav Brain Res 272 : 238-47.
  • Comparative stereostructure-activity studies on GABAA and GABAB receptor sites and GABA uptake using rat brain membrane preparations.

    Falch E et al (1986) J Neurochem 47(3) : 898-903.
  • GABAB agonism promotes sleep and reduces cataplexy in murine narcolepsy.

    Black SW et al (2014) J Neurosci 34(19) : 6485-94.
Publications
These publications cite the use of (R)-Baclofen purchased from Hello Bio:
  • Limiting habenular hyperactivity ameliorates maternal separation-driven depressive-like symptoms.

    Tchenio et al (2017) Nat Commun 8(1) : 1135
    PubMedID: 29074844
  • NALCN channels enhance the intrinsic excitability of spinal projection neurons.

    Ford et al (2018) Pain 159(9) : 1719-1730
    PubMedID: 29746349
  • Enhanced Postsynaptic GABAB Receptor Signaling in Adult Spinal Projection Neurons after Neonatal Injury.

    Baccei and Brewer (2018) Neuroscience 384 : 329-339
    PubMedID: 29885525

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