Selective GABAB receptor agonist
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.
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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).
Storing and Using Your Product
Soluble in water (20mM) and in DMSO (10mM)
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
References for (R)-Baclofen
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.PubMedID: 25026094
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.PubMedID: 3016189
GABAB agonism promotes sleep and reduces cataplexy in murine narcolepsy.Black SW et al (2014) J Neurosci 34(19) : 6485-94.PubMedID: 24806675
Limiting habenular hyperactivity ameliorates maternal separation-driven depressive-like symptoms.Tchenio et al(2017) Nat Commun 8(1) : 1135PubMedID: 29074844