????
|
|
???? ??
- ???
- 208-210°C
- ?? ?
- 364.3±32.0 °C(Predicted)
- ??
- 1.2069 (rough estimate)
- ???
- 1.5500 (estimate)
- ?? ??
- 2-8°C
- ???
- 1M HCl: 50mg/mL
- ??? ??
- ??
- ??? ??
- ??? ??
- ?? ?? (pKa)
- pKa 3.87±0.1(H2O) (Uncertain)
- ??
- ???? ?? ??? ???
- ???
- ?? NaOH ?? ?? HCl? ?????. pH 7.6?? ? 4mg/ml? ?? ?????.
- Merck
- 14,937
- ???
- ???
- InChI
- InChI=1S/C10H12ClNO2/c11-9-3-1-7(2-4-9)8(6-12)5-10(13)14/h1-4,8H,5-6,12H2,(H,13,14)
- InChIKey
- KPYSYYIEGFHWSV-UHFFFAOYSA-N
- SMILES
- C1(C=CC(Cl)=CC=1)C(CN)CC(=O)O
- CAS ??????
- 1134-47-0(CAS DataBase Reference)
- NIST
- Baclofen(1134-47-0)
??
- ?? ? ?? ??
- ?? ? ???? ?? (GHS)
| ??? ?? | T,Xn | ||
|---|---|---|---|
| ?? ???? ?? | 61-25-36/37/38-42/43-20/21/22 | ||
| ????? | 53-22-36/37/39-45-52-36-26 | ||
| ????(UN No.) | UN 2811 6.1/PG 3 | ||
| WGK ?? | 3 | ||
| RTECS ?? | MW5084200 | ||
| ?? ?? | 6.1(b) | ||
| ???? | III | ||
| HS ?? | 2922492050 | ||
| ?? | LD50 in male mice, rats (mg/kg): 45, 78 i.v.; 103, 115 s.c.; 200, 145 orally (Tadokoro) | ||
| ???? ?? | KE-01454 |
???? C??? ??, ??, ??
??? ??
Off-White Solid??
Baclofen may be used as a pharmaceutical secondary reference standard for the determination of the analyte in plasma samples by liquid chromatography tandem mass spectrometry and tablet formulations by UV spectroscopy, respectively.??
ChEBI: A monocarboxylic acid that is butanoic acid substituted by an amino group at position 4 and a 4-chlorophenyl group at position 3. It acts as a central nervous system depressant, GABA agonist and muscle relaxant.Biological Functions
Baclofen (Lioresal) is the parachlorophenol analogue of the naturally occurring neurotransmitter γ-aminobutyric acid (GABA).?? ??
Odorless or practically odorless white to off-white crystalline powder.??? ?? ??
Insoluble in water.?? ???
Baclofen is an amine. Amines are chemical bases. They neutralize acids to form salts plus water. These acid-base reactions are exothermic. The amount of heat that is evolved per mole of amine in a neutralization is largely independent of the strength of the amine as a base. Amines may be incompatible with isocyanates, halogenated organics, peroxides, phenols (acidic), epoxides, anhydrides, and acid halides. Flammable gaseous hydrogen is generated by amines in combination with strong reducing agents, such as hydrides.????
Flash point data for Baclofen are not available. Baclofen is probably combustible.???? ??
Selective GABA B receptor agonist. Skeletal muscle relaxant.Mechanism of action
Baclofen appears to affect the neuromuscular axis by acting directly on sensory afferents, γ-motor neurons, and collateral neurons in the spinal cord to inhibit both monosynaptic and polysynaptic reflexes. The principal effect is to reduce the release of excitatory neurotransmitters by activation of presynaptic GABAB receptors. This seems to involve a G protein and second-messenger link that either increases K+ conductance or decreases Ca++ conductance.Clinical Use
Baclofen is an agent of choice for treating spinal spasticity and spasticity associated with multiple sclerosis. It is not useful for treating spasticity of supraspinal origin. Doses should be increased gradually to a maximum of 100 to 150 mg per day, divided into four doses.???
Side effects are not a major problem, and they can be minimized by graduated dosage increases.They include lassitude, slight nausea, and mental disturbances (in including confusion, euphoria, and depression). The drowsiness is less pronounced than that produced by diazepam—an important therapeutic advantage. Hypotension has been noted, particularly following overdose. Elderly patients and patients with multiple sclerosis may require lower doses and may display increased sensitivity to the central side effects. Baclofen may increase the frequency of seizures in epileptics.Safety Profile
Poison by ingestion,subcutaneous and intravenous routes. Human systemiceffects by ingestion: blood pressure lowering, coma,muscle weakness, pulse rate decrease, respiratorydepression. When heated to decomposition it emits toxicfumes of Cl-?? ??
Baclofen is rapidly and effectively absorbed after oral administration. It is lipophilic and able to penetrate the blood-brain barrier.Approximately 35% of the drug is excreted unchanged in the urine and feces.???? ?? ?? ? ???
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???( 554)?? ??
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???? ?? ??:
???????? ?????????? ??-???-N-??? ? ????
Chloromethyl butyrate
CHLOROPHENYLSILANE 97
4-Phenylbutyric acid
(R)-Baclofen
BACLOFEN (-), [BUTYL-4-14C]
(S)-Baclofen,S(+)-Baclofen
BACLOFEN IMPURITY A
R(+)-Baclofen.Hydrochloride
METHYL 3-(4-CHLOROPHENYL)-2-METHOXYCARBONYL-4-NITROBUTANOATE
1-[(TERT-BUTYL)OXYCARBONYL]-4-(4-CHLOROPHENYL)PYRROLINE-3-CARBOXYLIC ACID
(2R,3S)-BETA-P-CHLOROPHENYLGLUTAMIC ACID
Trans (+/-) 4-(4-Chlorophenyl)Pyrrolidine-3-Methylcarboxylate Hydrochloride
4-(4-CHLOROPHENYL)PYRROLIDINE-3-METHYLCARBOXYLATE HYDROCHLORIDE
FMOC-BACLOFIN