Baclofen
Baclofen is a GABA derivative that acts as an agonist at GABA-B receptors; it is commonly used in animal models to examine the effects of GABAergic neurotransmission in a variety of fields, including substance dependence, spasticity, pain, and feeding behavior. Baclofen exhibits analgesic, antinociceptive, and antiepileptic/anticonvulsant activities. The analgesic effect of baclofen is mediated by its GABA-B receptor activation, inducing a presynaptic block of action potentials induced by mechanical or thermal stimuli that decreases frequency and amplitude of excitatory post-synaptic currents. Baclofen is used clinically to promote abstinence in alcohol dependent subjects, potentially mediating alcohol craving during withdrawal. This compound is also delivered intrathecally to treat spasticity and dystonia.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18842901
| Cas No. |
1134-47-0 |
|---|---|
| Purity |
≥98% |
| Formula |
C10H12ClNO2 |
| Formula Wt. |
213.66 |
| Chemical Name |
β-(Aminomethyl)-4-chlorobenzenepropanoic acid |
| IUPAC Name |
4-amino-3-(4-chlorophenyl)butanoic acid |
| Synonym |
Baclon; Clofen; Lioresal |
| Melting Point |
206-208°C |
| Solubility |
Soluble in water or NaOH. |
| Appearance |
White to off white powder |
Fukuhara K, Katafuchi T, Yoshimura M. Effects of baclofen on mechanical noxious and innocuous transmission in the spinal dorsal horn of the adult rat: in vivo patch-clamp analysis. Eur J Neurosci. 2013 Aug 20. [Epub ahead of print]. PMID: 23961926.
Kumru H, Kofler M, Flores MC, et al. Effect of intrathecal baclofen on evoked pain perception: an evoked potentials and quantitative thermal testing study. Eur J Pain. 2013 Aug;17(7):1039-47. PMID: 23239275.
Brennan JL, Leung JG, Gagliardi JP, et al. Clinical effectiveness of baclofen for the treatment of alcohol dependence: a review. Clin Pharmacol. 2013 Jul 3;5:99-107. PMID: 23869179.
Uchiyama T, Nakanishi K, Fukawa N, et al. Neuromodulation using intrathecal baclofen therapy for spasticity and dystonia. Neurol Med Chir (Tokyo). 2012;52(7):463-9. PMID: 22850493.
Miner P, Borkuhova Y, Shimonova L, et al. GABA-A and GABA-B receptors mediate feeding elicited by the GABA-B agonist baclofen in the ventral tegmental area and nucleus accumbens shell in rats: reciprocal and regional interactions. Brain Res. 2010 Oct 8;1355:86-96. PMID: 20696149.
Levy RA, Proudfit HK. The analgesic action of baclofen [beta-(4-chlorophenyl)-gamma-aminobutyric acid]. J Pharmacol Exp Ther. 1977 Aug;202(2):437-45. PMID: 886473.
