Pricing updated 2019-03-24. Prices are subject to change without notice.
γ-Aminobutyric acid (GABA) is an inhibitory neurotransmitter that acts through heteromeric ligand-gated ion channels, GABAA and GABAC, and a G protein-coupled receptor, GABAB. (±)-Baclofen is a selective agonist of GABAB (IC50 = 200 nM).1 By activating GABAB, (±)-baclofen causes skeletal muscle relaxation and blocks spasticity.2,3,4 It also modifies animal responses to alcohol and cocaine.5,6
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Berthelot, P., Vaccher, C., Musadad, A., et al. Synthesis and pharmacological evaluation of gamma-
2. Biscoe, T.J., and Fry, J.P. Some pharmacological studies on the spastic mouse British Journal of Pharmacology 75(1), 23-25 (1982).
Sakitani, K. The effects of centrally acting muscle relaxants on the intrathecal noradrenaline-
4. Chou, R., Peterson, K., and Helfand, M. Comparative efficacy and safety of skeletal muscle relaxants for spasticity and musculoskeletal conditions: A systematic review Journal of Pain and Symptom Management 28(2), 140-175 (2004).
Moore, E.M., and Boehm, S.L., II Site-
Lhuillier, L., Mombereau, C., Cryan, J.F., et al. GABAB receptor-