(R)-Baclofen (hydrochloride)

Names

[ Name ]:
(R)-Baclofen (hydrochloride)

[Synonym ]:
Arbaclofen HCl
d-Baclofen hydrochloride
MFCD00078579
Arbaclofen hydrochloride
(R)-Baclofen (hydrochloride)

Biological Activity

[Description]:

(R)-Baclofen Hcl(STX-209 Hcl) is a derivative of gamma-aminobutyric acid (GABA) primarily used to treat spasticity and is in the early research stages for use for the treatment of alcoholism.Target: GABABaclofen (brand names Kemstro, Lioresal, Liofen, Gablofen, Beklo and Baclosan) is a derivative of gamma-aminobutyric acid (GABA). It is primarily used to treat spasticity and is in the early research stages for use for the treatment of alcoholism. It is also used by compounding pharmacies in topical pain creams as a muscle relaxant.It is an agonist for the GABAB receptors. Its beneficial effects in spasticity result from actions at spinal and supraspinal sites. Baclofen can also be used to treat hiccups, and has been shown to prevent rises in body temperature induced by the drug MDMA in rats.In addition, research has shown baclofen to be effective in the treatment of alcohol dependence and withdrawal, by inhibiting both withdrawal symptoms andcravings.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor

Signaling Pathways >> Neuronal Signaling >> GABA Receptor

Research Areas >> Neurological Disease

[References]

[1]. Mezler M, et al. Cloning and functional expression of GABA(B) receptors from Drosophila. Eur J Neurosci. 2001 Feb;13(3):477-86.

[2]. Dzitoyeva S, et al. 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.

[Related Small Molecules]

Chemical & Physical Properties

[ Boiling Point ]:
364.3ºC at 760 mmHg

[ Molecular Formula ]:
C₁₀H₁₃Cl₂NO₂

[ Molecular Weight ]:
250.12200

[ Flash Point ]:
174.1ºC

[ Exact Mass ]:
249.03200

[ PSA ]:
63.32000

[ LogP ]:
3.35930

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MW5084350

CHEMICAL NAME :: Hydrocinnamic acid, beta-(aminomethyl)-p-chloro-, hydrochloride, (R)-

CAS REGISTRY NUMBER :: 63701-55-3

LAST UPDATED :: 198503

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C10-H12-Cl-N-O2.Cl-H

MOLECULAR WEIGHT :: 250.14

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 523 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 32,187,1980

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Safety Phrases ]:
S24/25

[ RIDADR ]:
UN 2811 6.1/PG 3

[ RTECS ]:
MW5084350

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

Effects of phaclofen and the enantiomers of baclofen on cardiovascular responses to intrathecal administration of L- and D-baclofen in the rat.

Eur. J. Pharmacol. 196 , 267, (1991)

In a previous study it was found that i.t. administration of L-baclofen decreased arterial pressure and heart rate while D-baclofen differentially increased arterial pressure. The objective of the pre...

Comparative stereostructure-activity studies on GABAA and GABAB receptor sites and GABA uptake using rat brain membrane preparations.

J. Neurochem. 47 , 898, (1986)

The affinities of a number of analogues of gamma-aminobutyric acid (GABA) for GABAA and GABAB receptor sites and GABA uptake were studied using rat brain membrane preparations. Studies on the (S)-(+)-...

3-(p-Chlorophenyl)-4-aminobutanoic acid--resolution into enantiomers and pharmacological activity.

Pol. J. Pharmacol. Pharm. 32 , 187, (1980)

Racemic 3-(p-chlorophenyl)-4-aminobutanoic acid was resolved into enantiomers and their absolute configuration determined. Pharmacological activity of hydrochlorides of the racemic acid and its enanti...