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Substance Name: Baclofen [USAN:USP:INN:BAN:JAN]
RN: 1134-47-0
UNII: H789N3FKE8
InChIKey: KPYSYYIEGFHWSV-UHFFFAOYSA-N
Note
- A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.
Molecular Formula
- C10-H12-Cl-N-O2
Molecular Weight
- 213.6628
- All
- Classifications
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- Names & Synonyms
- Registry Numbers
- Structure Descriptors
- Toxicity
- Physical Properties
Classification Codes
- Central Nervous System Agents
- Drug / Therapeutic Agent
- GABA Agents
- GABA Agonists
- GABA-B Receptor Agonists
- Human Data
- Muscle Relaxants, Central
- Neuromuscular Agents
- Neurotransmitter Agents
- Peripheral Nervous System Agents
- Relaxant (Muscle)
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Names and Synonyms
Name of Substance
- Baclofen
- Baclofen [USAN:USP:INN:BAN:JAN]
MeSH Heading
- Baclofen
Synonyms
- (+-)-Baclofen
- 4-Amino-3-(4-chlorophenyl)butyric acid
- Apo-Baclofen
- Atrofen
- Ba 34647
- Ba-34,647
- Ba-34647
- Baclofen
- Baclofene
- Baclofene [INN-French]
- Baclofeno
- Baclofeno [INN-Spanish]
- Baclofenum
- Baclofenum [INN-Latin]
- Baclon
- beta-(4-Chlorophenyl)gaba
- beta-(Aminomethyl)-4-chlorobenzenepropanoic acid
- beta-(Aminomethyl)-p-chlorohydrocinnamic acid
- beta-(p-Chlorophenyl)-gamma-aminobutyric acid
- BRN 2104494
- C 34647Ba
- CCRIS 3722
- Ciba 34,647-Ba
- DL-4-Amino-3-p-chlorophenylbutanoic acid
- DL-Baclofen
- EINECS 214-486-9
- Gabalon
- Gablofen
- gamma-Amino-beta-(p-chlorophenyl)butyric acid
- IPX 056
- IPX056
- Kemstro
- Lioresal
- Lioresal Intrathecal
- NSC 755906
- UNII-H789N3FKE8
Systematic Names
- Baclofen
- Benzenepropanoic acid, beta-(aminomethyl)-4-chloro-
- Benzenepropanoic acid, beta-(aminomethyl)-4-chloro-(9CI)
- Butanoic acid, 4-amino-3-(4-chlorophenyl)-
- Hydrocinnamic acid, beta-(aminomethyl)-p-chloro-
Registry Numbers
CAS Registry Number
- 1134-47-0
FDA UNII
- H789N3FKE8
System Generated Number
- 0001134470
Structure Descriptors
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-NSmiles
NCC(CC(=O)Toxicity
Organism | Test Type | Route | Reported Dose (Normalized Dose) | Effect | Source |
---|---|---|---|---|---|
man | TDLo | oral | 571ug/kg (0.571mg/kg) | LUNGS, THORAX, OR RESPIRATION: DYSPNEA | Annals of Pharmacotherpy. Vol. 27, Pg. 883, 1993. |
man | TDLo | oral | 4286ug/kg (4.286mg/kg) | CARDIAC: PULSE RATE BEHAVIORAL: COMA VASCULAR: BP LOWERING NOT CHARACTERIZED IN AUTONOMIC SECTION | American Journal of Emergency Medicine. Vol. 4, Pg. 552, 1986. |
man | TDLo | oral | 14mg/kg (14mg/kg) | BEHAVIORAL: MUSCLE WEAKNESS BEHAVIORAL: COMA | Journal of Toxicology, Clinical Toxicology. Vol. 20, Pg. 59, 1983. |
man | TDLo | oral | 3429mg/kg (3429mg/kg) | BEHAVIORAL: COMA LUNGS, THORAX, OR RESPIRATION: RESPIRATORY OBSTRUCTION CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP | Journal of Toxicology, Clinical Toxicology. Vol. 32, Pg. 291, 1994. |
man | TDLo | unreported | 857ug/kg/2D-I (0.857mg/kg) | BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS" BRAIN AND COVERINGS: CHANGES IN SURFACE EEG | Italian Journal of Neurological Sciences. Vol. 12, Pg. 323, 1991. |
mouse | LD50 | intravenous | 31mg/kg (31mg/kg) | BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX) LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION BEHAVIORAL: ATAXIA | Gekkan Yakuji. Pharmaceuticals Monthly. Vol. 21, Pg. 2069, 1979. |
mouse | LD50 | oral | 200mg/kg (200mg/kg) | Drugs in Japan Vol. 6, Pg. 576, 1982. | |
mouse | LD50 | subcutaneous | 103mg/kg (103mg/kg) | Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 11, Pg. 181, 1980. | |
rat | LD50 | intravenous | 78mg/kg (78mg/kg) | Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 11, Pg. 181, 1980. | |
rat | LD50 | oral | 145mg/kg (145mg/kg) | Drugs in Japan Vol. 6, Pg. 576, 1982. | |
rat | LD50 | subcutaneous | 115mg/kg (115mg/kg) | Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 11, Pg. 181, 1980. | |
women | TDLo | oral | 8mg/kg (8mg/kg) | LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION CARDIAC: PULSE RATE | Postgraduate Medical Journal. Vol. 57, Pg. 580, 1981. |
women | TDLo | oral | 9mg/kg (9mg/kg) | LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD BEHAVIORAL: COMA | Postgraduate Medical Journal. Vol. 56, Pg. 865, 1980. |
women | TDLo | oral | 18mg/kg (18mg/kg) | LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION BEHAVIORAL: COMA | Journal of Toxicology, Clinical Toxicology. Vol. 22, Pg. 11, 1984. |
women | TDLo | parenteral | 25ug/kg/2D-I (0.025mg/kg) | SENSE ORGANS AND SPECIAL SENSES: MYDRIASIS (PUPILLARY DILATION): EYE BEHAVIORAL: COMA | International Journal of Clinical Pharmacology, Therapy and Toxicology. Vol. 29, Pg. 274, 1991. |
Physical Properties
Physical Property | Value | Units | Temp (deg C) | Source |
---|---|---|---|---|
Melting Point | 206-208 | deg C | EXP | |
log P (octanol-water) | -0.96 | (none) | EXP | |
Water Solubility | 2090 | mg/L | 25 | EST |
Vapor Pressure | 2.36E-09 | mm Hg | 25 | EST |
Henry's Law Constant | 5.94E-12 | atm-m3/mole | 25 | EST |
Atmospheric OH Rate Constant | 3.77E-11 | cm3/molecule-sec | 25 | EST |
Physical property data is provided to ChemIDplus by SRC, Inc.