A GABAB receptor agonist
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(±)-Baclofen

Item No. 18600

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
β-(aminomethyl)-4-chloro-benzenepropanoic acid
CAS Number
1134-47-0
Molecular Formula
C10H12ClNO2
Formula Weight
213.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
Water: 4 mg/ml
λmax
220, 266 nm
SMILES
ClC1=CC=C(C(CN)CC(O)=O)C=C1
InChi Code
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)
InChi Key
KPYSYYIEGFHWSV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 g

    $49

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    5 g

    $143

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    10 g

    $259

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    25 g

    $423

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    Product Description

    (±)-Baclofen is a GABAB receptor agonist (IC50 = 180 nM).1 It induces norepinephrine release from isolated rat atria (IC50 = 4.5 μM). (±)-Baclofen (10 mg/kg) increases muscle rigidity in spastic mice.2 It inhibits the norepinephrine-induced group II flexor reflex in anesthetized rats.3 (±)-Baclofen also reduces cocaine-induced hyperlocomotion in rats and binge-like ethanol intake in mice.4,5 Formulations containing baclofen have been used to treat muscle spasms caused by multiple sclerosis and spinal cord injury.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hill, D.R., and Bowery, N.G. 3H-baclofen and 3H-GABA bind to bicuculline-insensitive GABAB sites in rat brain. Nature 290(5802), (1981).

    2. Biscoe, T.J., and Fry, J.P. Some pharmacological studies on the spastic mouse. Br. J. Pharmacol. 75(1), 23-25 (1982).

    3. Sakitani, K. The effects of centrally acting muscle relaxants on the intrathecal noradrenaline-induced facilitation of the flexor reflex mediated by group II afferent fibers in rats. Jpn. J. Pharmacol. 63(3), 369-376 (1993).

    4. Lhuillier, L., Mombereau, C., Cryan, J.F., et al. GABAB receptor-positive modulation decreases selective molecular and behavioral effects of cocaine. Neuropsychopharmacology 32(2), 388-398 (2007).

    5. Moore, E.M., and Boehm, S.L., II Site-specific microinjection of baclofen into the anterior ventral tegmental area reduces binge-like ethanol intake in male C57BL/6J mice. Behav. Neurosci. 123(3), 555-563 (2009).