| Identification | Back Directory | [Name]
4-amino-3-(4-chlorophenyl)butanoic acid hydron chloride | [CAS]
28311-31-1 | [Synonyms]
Baclofen hydrochloride salt
13C6]-Baclofen hydrochloride salt
4-amino-3-(4-chlorophenyl)butanoic acid hydron chloride
Benzenepropanoic acid, b-(aminomethyl)-4-chloro-, hydrochloride
Baclofen hydrochloride,Gamma-aminobutyric acid Receptor,GABA,γ-Aminobutyric acid Receptor,spasticity,γ-aminobutyric acid,Baclofen,Lipophilic,GABA Receptor,GABABR,bbb,inhibit,blood brain barrier,Inhibitor,orally | [Molecular Formula]
C10H13Cl2NO2 | [MDL Number]
MFCD01722193 | [MOL File]
28311-31-1.mol | [Molecular Weight]
250.12 |
| Hazard Information | Back Directory | [Uses]
Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research[1][2][3]. | [in vivo]
Baclofen (i.p.; 10 μg/g; twice daily for 3 consecutive days) hydrochloride ameliorates motor deficits in YAC128 HD transgenic mice[3].
| Animal Model: | Wild type (WT) and mutant (MT) male YAC128 mice at 13-18 months of age[3] | | Dosage: | 10 μg/g | | Administration: | IP; twice daily at 9:00 a.m. and 5:00 p.m., for 3 consecutive days; then single dose on the fourth day at 9:00 a.m | | Result: | Ameliorated motor deficits in YAC128 HD transgenic mice.
Increased proteasome activity and reduces neuronal intranuclear inclusions (NIIs) in YAC128 HD transgenic mice.
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| [References]
[1] Mehdi Farokhnia, et al. A deeper insight into how GABA-B receptor agonism via baclofen may affect alcohol seeking and consumption: lessons learned from a human laboratory investigation. Mol Psychiatry. 2018 Oct 31. DOI:10.1038/s41380-018-0287-y
[2] Bexis, S., et al., Baclofen prevents MDMA-induced rise in core body temperature in rats. Drug Alcohol Depend, 2004. 74(1): p. 89-96. DOI:10.1016/j.drugalcdep.2003.12.004
[3] Woori Kim, et al. Baclofen, a GABAB receptor agonist, enhances ubiquitin-proteasome system functioning and neuronal survival in Huntington's disease model mice. Biochem Biophys Res Commun. 2014 Jan 10;443(2):706-11. DOI:10.1016/j.bbrc.2013.12.034 |
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