Product Name

Baclofen

CAS Number

1134-47-0

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Product Name:
Baclofen
CAS Number:
1134-47-0
Indication:
For the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity.
Mode of Action:

Baclofen is a direct agonist at GABAB receptors. The precise mechanism of action of Baclofen is not fully known. It is capable of inhibiting both monosynaptic and polysynaptic reflexes at the spinal level, possibly by hyperpolarization of afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect.

Pharmacodynamics:

Baclofen is a muscle relaxant and antispastic. Baclofen is useful for the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity. Although Baclofen is an analog of the putative inhibitory neurotransmitter gamma-aminobutyric acid (GABA), there is no conclusive evidence that actions on GABA systems are involved in the production of its clinical effects. In studies with animals, Baclofen has been shown to have general CNS depressant properties as indicated by the production of sedation with tolerance, somnolence, ataxia, and respiratory and cardiovascular depression. Baclofen is rapidly and extensively absorbed and eliminated. Absorption may be dose-dependent, being reduced with increasing doses. Baclofen is excreted primarily by the kidney in unchanged form and there is relatively large intersubject variation in absorption and/or elimination.

Metabolism:

~ 15% of the dose is metabolized in the liver, primarily by deamination. 70-80% of the dose is excreted unchanged or as metabolites in urine and the remainder is excreted in feces.

Toxicity:

LD50=45 mg/kg (male mice, IV); LD50=78 mg/kg (male rat, IV)

IUPAC:
4-amino-3-(4-chlorophenyl)butanoic acid
ATC:
M03BX01
PubChem:
2284
DrugBank:
DB00181 (APRD00551)
Formula:
C18H31NO4
Molecular Mass:
213.661
SMILES:
NCC(CC(O)=O)C1=CC=C(Cl)C=C1
AHFS Code:
12:20.1
InChi:
KPYSYYIEGFHWSV-UHFFFAOYSA-N
General Reference:
General Reference:

  1. Dzitoyeva S, Dimitrijevic N, Manev H: Gamma-aminobutyric acid B receptor 1 mediates behavior-impairing actions of alcohol in Drosophila: adult RNA interference and pharmacological evidence. Proc Natl Acad Sci U S A. 2003 Apr 29;100(9):5485-90. Epub 2003 Apr 11. Pubmed
  2. Mezler M, Muller T, Raming K: Cloning and functional expression of GABA receptors from Drosophila. Eur J Neurosci. 2001 Feb;13(3):477-86. Pubmed
  3. See S, Ginzburg R: Skeletal muscle relaxants. Pharmacotherapy. 2008 Feb;28(2):207-13. Pubmed

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