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Identification
NameBaclofen
Accession NumberDB00181  (APRD00551)
TypeSmall Molecule
GroupsApproved
Description

Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant. Baclofen stimulates GABA-B receptors leading to decreased frequency and amplitude of muscle spasms. It is especially useful in treating muscle spasticity associated with spinal cord injury. It appears to act primarily at the spinal cord level by inhibiting spinal polysynaptic afferent pathways and, to a lesser extent, monosynaptic afferent pathways.

Structure
Thumb
Synonyms
(+-)-Baclofen
4-Amino-3-(4-chlorophenyl)butyric acid
Baclofene
Baclofeno
Baclofenum
beta-(4-Chlorophenyl)gaba
beta-(Aminomethyl)-4-chlorobenzenepropanoic acid
beta-(Aminomethyl)-P-chlorohydrocinnamic acid
beta-(P-Chlorophenyl)-gamma-aminobutyric acid
DL-4-Amino-3-P-chlorophenylbutanoic acid
DL-Baclofen
gamma-Amino-beta-(P-chlorophenyl)butyric acid
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ava-baclofentablet20 mgoralAvanstra Inc2011-10-112014-08-21Canada
Ava-baclofentablet10 mgoralAvanstra Inc2011-10-112014-08-21Canada
Baclofentablet10 mgoralApotex Inc1994-12-312014-08-23Canada
Baclofentablet20 mgoralSanis Health Inc2010-02-25Not applicableCanada
Baclofentablet10 mgoralSanis Health Inc2010-02-25Not applicableCanada
Baclofentablet20 mgoralApotex Inc1994-12-312014-08-23Canada
Baclofen Tablets - 10mgtablet10 mgoralBdh Inc.1995-12-312000-08-03Canada
Baclofen Tablets - 20mgtablet20 mgoralBdh Inc.1995-12-312000-08-03Canada
Baclofen Tablets 10mgtablet10 mgoralPrempharm Inc1997-01-052005-08-05Canada
Baclofen Tablets 20mgtablet20 mgoralPrempharm Inc1997-01-052005-08-05Canada
Baclofen-10 - Tabtablet10 mgoralPro Doc Limitee1996-12-31Not applicableCanada
Baclofen-20 - Tabtablet20 mgoralPro Doc Limitee1996-12-31Not applicableCanada
Co Baclofen Tablets 10mgtablet10 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Co Baclofen Tablets 20mgtablet20 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Dom-baclofen-tab 10mgtablet10 mgoralDominion Pharmacal1995-12-31Not applicableCanada
Dom-baclofen-tab 20mgtablet20 mgoralDominion Pharmacal1995-12-31Not applicableCanada
Ftp-baclofentablet20 mgoralFtp Pharmacal Inc.1998-10-092004-08-03Canada
Ftp-baclofentablet10 mgoralFtp Pharmacal Inc.1998-10-092004-08-03Canada
Gablofeninjection50 ug/mLintrathecalMallinckrodt Inc (Brand Pharmaceuticals)2010-11-19Not applicableUs
Gablofeninjection2000 ug/mLintrathecalMallinckrodt Inc (Brand Pharmaceuticals)2010-11-19Not applicableUs
Gablofeninjection1000 ug/mLintrathecalMallinckrodt Inc (Brand Pharmaceuticals)2012-07-10Not applicableUs
Gablofeninjection500 ug/mLintrathecalMallinckrodt Inc (Brand Pharmaceuticals)2010-11-19Not applicableUs
Lioresalinjection2 mg/mLintrathecalMedtronic Neuromodulation2003-05-08Not applicableUs
Lioresalinjection.05 mg/mLintrathecalMedtronic Neuromodulation1996-11-07Not applicableUs
Lioresalinjection2 mg/mLintrathecalMedtronic Neuromodulation1992-06-17Not applicableUs
Lioresalinjection.5 mg/mLintrathecalMedtronic Neuromodulation1992-06-17Not applicableUs
Lioresal D.S. Tab 20mgtablet20 mgoralNovartis Pharmaceuticals Canada Inc1985-12-31Not applicableCanada
Lioresal Intrathecal 0.05mg/mlsolution0.05 mgintrathecalNovartis Pharmaceuticals Canada Inc1994-12-31Not applicableCanada
Lioresal Intrathecal 0.5mg/mlsolution0.5 mgintrathecalNovartis Pharmaceuticals Canada Inc1994-12-31Not applicableCanada
Lioresal Intrathecal 2mg/mlsolution2 mgintrathecalNovartis Pharmaceuticals Canada Inc1994-12-31Not applicableCanada
Lioresal Tab 10mgtablet10 mgoralNovartis Pharmaceuticals Canada Inc1978-12-31Not applicableCanada
Med Baclofen Tab 10mgtablet10 mgoralMedican Pharma Incorporated1995-12-312011-03-29Canada
Med Baclofen Tab 20mgtablet20 mgoralMedican Pharma Incorporated1995-12-312011-03-29Canada
Mylan-baclofentablet20 mgoralMylan Pharmaceuticals Ulc1994-12-31Not applicableCanada
Mylan-baclofentablet10 mgoralMylan Pharmaceuticals Ulc1994-12-31Not applicableCanada
Novo-baclofentablet20 mgoralNovopharm Limited1997-01-312015-10-26Canada
Novo-baclofentablet10 mgoralNovopharm Limited1997-01-312015-10-26Canada
Penta-baclofen Tabletstablet20 mgoralPentapharm Ltd.Not applicableNot applicableCanada
Penta-baclofen Tabletstablet10 mgoralPentapharm Ltd.Not applicableNot applicableCanada
PHL-baclofentablet20 mgoralPharmel Inc1998-02-16Not applicableCanada
PHL-baclofentablet10 mgoralPharmel Inc1998-02-16Not applicableCanada
PMS-baclofentablet10 mgoralPharmascience Inc1994-12-31Not applicableCanada
PMS-baclofen Tab 20mgtablet20 mgoralPharmascience Inc1994-12-31Not applicableCanada
Ratio-baclofentablet20 mgoralTeva Canada Limited1997-12-16Not applicableCanada
Ratio-baclofentablet10 mgoralTeva Canada Limited1997-12-16Not applicableCanada
Riva-baclofentablet20 mgoralLaboratoire Riva Inc2003-03-03Not applicableCanada
Riva-baclofentablet10 mgoralLaboratoire Riva Inc2003-03-03Not applicableCanada
Sandoz Baclofentablet20 mgoralSandoz Canada IncorporatedNot applicableNot applicableCanada
Sandoz Baclofentablet10 mgoralSandoz Canada IncorporatedNot applicableNot applicableCanada
Val-baclofen Intrathecalsolution2 mgintrathecalValeant Canada Lp Valeant Canada S.E.C.2014-06-06Not applicableCanada
Val-baclofen Intrathecalsolution0.5 mgintrathecalValeant Canada Lp Valeant Canada S.E.C.2014-06-06Not applicableCanada
Val-baclofen Intrathecalsolution0.05 mgintrathecalValeant Canada Lp Valeant Canada S.E.C.2014-06-06Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-baclofen Tablets - 10mgtablet10 mgoralApotex Inc1994-12-31Not applicableCanada
Apo-baclofen Tablets - 20mgtablet20 mgoralApotex Inc1994-12-31Not applicableCanada
Baclofentablet10 mg/1oralPreferred Pharmaceuticals, Inc2004-07-01Not applicableUs
Baclofentablet10 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2011-04-11Not applicableUs
Baclofentablet10 mg/1oralDIRECT RX2014-01-01Not applicableUs
Baclofentablet10 mg/1oralMarlex Pharmaceuticals Inc2014-12-01Not applicableUs
Baclofentablet10 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-07-15Not applicableUs
Baclofentablet10 mg/1oralIVAX Pharmaceuticals, Inc.1988-07-21Not applicableUs
Baclofentablet10 mg/1oralCardinal Health2010-07-15Not applicableUs
Baclofentablet20 mg/1oralMed Health Pharma, LLC2011-01-01Not applicableUs
Baclofentablet10 mg/1oralPreferred Pharmaceuticals, Inc.2014-10-22Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2011-10-10Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2011-04-04Not applicableUs
Baclofentablet10 mg/1oralAidarex Pharmaceuticals LLC2005-08-30Not applicableUs
Baclofentablet20 mg/1oralMarlex Pharmaceuticals Inc2014-12-01Not applicableUs
Baclofentablet20 mg/1oralDIRECT RX2014-01-01Not applicableUs
Baclofentablet10 mg/1oralSt Marys Medical Park Pharmacy2014-01-15Not applicableUs
Baclofentablet20 mg/1oralCardinal Health1998-07-21Not applicableUs
Baclofentablet10 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2007-07-01Not applicableUs
Baclofentablet20 mg/1oralMajor Pharmaceuticals2015-07-15Not applicableUs
Baclofentablet20 mg/1oralQualitest Pharmaceuticals2005-08-30Not applicableUs
Baclofentablet10 mg/1oralPhysicians Total Care, Inc.2010-03-05Not applicableUs
Baclofentablet20 mg/1oralAvera Mc Kennan Hospital2015-03-31Not applicableUs
Baclofentablet10 mg/1oralMed Health Pharma, LLC2011-01-01Not applicableUs
Baclofentablet20 mg/1oralPd Rx Pharmaceuticals, Inc.2005-08-30Not applicableUs
Baclofentablet20 mg/1oralRebel Distributors Corp.2004-07-01Not applicableUs
Baclofentablet10 mg/1oralDIRECT RX2014-01-01Not applicableUs
Baclofentablet10 mg/1oralNew Horizon Rx Group, LLC2013-08-25Not applicableUs
Baclofentablet20 mg/1oralAmerican Health Packaging2015-02-15Not applicableUs
Baclofentablet10 mg/1oralMajor Pharmaceuticals2015-07-15Not applicableUs
Baclofentablet10 mg/1oralQualitest Pharmaceuticals2005-08-30Not applicableUs
Baclofentablet20 mg/1oralPhysicians Total Care, Inc.2009-04-17Not applicableUs
Baclofentablet10 mg/1oralAmerican Health Packaging2012-09-032015-12-29Us
Baclofentablet20 mg/1oralUnit Dose Services2010-07-15Not applicableUs
Baclofentablet20 mg/1oralAv Kare, Inc.2014-08-25Not applicableUs
Baclofentablet10 mg/1oralRebel Distributors Corp.2004-07-01Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2015-12-16Not applicableUs
Baclofentablet10 mg/1oralClinical Solutions Wholesale2010-10-20Not applicableUs
Baclofentablet10 mg/1oralAmerican Health Packaging2015-02-15Not applicableUs
Baclofentablet20 mg/1oralBryant Ranch Rrepack2007-07-01Not applicableUs
Baclofentablet10 mg/1oralState of Florida DOH Central Pharmacy2014-01-01Not applicableUs
Baclofentablet20 mg/1oralMc Kesson Contract Packaging2011-12-12Not applicableUs
Baclofentablet10 mg/1oralUnit Dose Services1988-07-21Not applicableUs
Baclofentablet10 mg/1oralAv Kare, Inc.2014-08-25Not applicableUs
Baclofentablet20 mg/1oralNorthstar Rx LLC2011-01-01Not applicableUs
Baclofentablet20 mg/1oralREMEDYREPACK INC.2015-06-15Not applicableUs
Baclofentablet10 mg/1oralClinical Solutions Wholesale2010-10-20Not applicableUs
Baclofentablet20 mg/1oralAmerican Health Packaging2012-09-032016-02-29Us
Baclofentablet10 mg/1oralBryant Ranch Rrepack2007-07-01Not applicableUs
Baclofentablet20 mg/1oralMajor Pharmaceuticals1998-07-21Not applicableUs
Baclofentablet20 mg/1oralLannett Company, Inc.2005-12-01Not applicableUs
Baclofentablet10 mg/1oralRebel Distributors Corp2010-07-15Not applicableUs
Baclofentablet10 mg/1oralNorthstar Rx LLC2011-01-01Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2015-03-20Not applicableUs
Baclofentablet20 mg/1oralClinical Solutions Wholesale, Llc2010-10-20Not applicableUs
Baclofentablet10 mg/1oralDispensing Solutions, Inc.2005-08-30Not applicableUs
Baclofentablet10 mg/1oralProficient Rx LP2005-12-01Not applicableUs
Baclofentablet10 mg/1oralMajor Pharmaceuticals1998-07-21Not applicableUs
Baclofentablet10 mg/1oralLannett Company, Inc.2007-07-01Not applicableUs
Baclofentablet20 mg/1oralA S Medication Solutions1988-07-21Not applicableUs
Baclofentablet20 mg/1oralState of Florida DOH Central Pharmacy2014-01-01Not applicableUs
Baclofentablet10 mg/1oralMc Kesson Contract Packaging2011-11-14Not applicableUs
Baclofentablet20 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-11-15Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2015-02-25Not applicableUs
Baclofentablet10 mg/1oralClinical Solutions Wholesale, Llc2010-10-20Not applicableUs
Baclofentablet20 mg/1oralDispensing Solutions, Inc.2005-08-30Not applicableUs
Baclofentablet20 mg/1oralProficient Rx LP2005-12-01Not applicableUs
Baclofentablet20 mg/1oralUpsher Smith Laboratories, Inc.2010-10-20Not applicableUs
Baclofentablet20 mg/1oralMylan Pharmaceuticals Inc.2010-02-18Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2016-03-25Not applicableUs
Baclofentablet10 mg/1oralH.J. Harkins Company, Inc.2010-07-15Not applicableUs
Baclofentablet10 mg/1oralPreferred Pharmaceuticals, Inc.2012-03-28Not applicableUs
Baclofentablet10 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-05-19Not applicableUs
Baclofentablet20 mg/1oralRebel Distributors Corp2010-07-15Not applicableUs
Baclofentablet20 mg/1oralSTAT Rx USA LLC1991-09-18Not applicableUs
Baclofentablet20 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2005-12-01Not applicableUs
Baclofentablet10 mg/1oralProficient Rx LP1988-07-21Not applicableUs
Baclofentablet10 mg/1oralUpsher Smith Laboratories, Inc.2010-10-20Not applicableUs
Baclofentablet10 mg/1oralMylan Pharmaceuticals Inc.2010-02-18Not applicableUs
Baclofentablet10 mg/1oralCardinal Health2015-07-15Not applicableUs
Baclofentablet20 mg/1oralH.J. Harkins Company, Inc.2010-07-15Not applicableUs
Baclofentablet10 mg/1oralPreferred Pharmaceuticals, Inc2012-04-30Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2012-03-15Not applicableUs
Baclofentablet20 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2010-10-20Not applicableUs
Baclofentablet10 mg/1oralSTAT Rx USA LLC1991-09-18Not applicableUs
Baclofentablet20 mg/1oralREMEDYREPACK INC.2014-12-04Not applicableUs
Baclofentablet10 mg/1oralPd Rx Pharmaceuticals, Inc.2010-07-15Not applicableUs
Baclofentablet20 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2011-05-31Not applicableUs
Baclofentablet20 mg/1oralDIRECT RX2014-01-01Not applicableUs
Baclofentablet20 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-07-15Not applicableUs
Baclofentablet20 mg/1oralIVAX Pharmaceuticals, Inc.1988-07-21Not applicableUs
Baclofentablet20 mg/1oralREMEDYREPACK INC.2013-02-11Not applicableUs
Baclofentablet20 mg/1oralPreferred Pharmaceuticals, Inc2012-04-30Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2012-03-13Not applicableUs
Baclofentablet20 mg/1oralAidarex Pharmaceuticals LLC2005-08-30Not applicableUs
Baclofentablet10 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Baclofentablet20 mg/1oralSt Marys Medical Park Pharmacy2014-04-20Not applicableUs
Baclofentablet20 mg/1oralCardinal Health1988-07-21Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Equipto - Baclofen External Cream Compounding KitkittopicalAlvix Laboratories, LLC2015-01-20Not applicableUs
International Brands
NameCompany
BaclonUniao Quimica (Brazil)
KemstroSchwarz (United States)
Lioresal IntrathecalNovartis Pharmaceuticals
Nu-BaclofenNu-Pharm
Brand mixtures
NameLabellerIngredients
Gapeam BudibacAlvix Laboratories, LLC
SaltsNot Available
Categories
UNIIH789N3FKE8
CAS number1134-47-0
WeightAverage: 213.661
Monoisotopic: 213.05565634
Chemical FormulaC10H12ClNO2
InChI KeyInChIKey=KPYSYYIEGFHWSV-UHFFFAOYSA-N
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)
IUPAC Name
4-amino-3-(4-chlorophenyl)butanoic acid
SMILES
NCC(CC(O)=O)C1=CC=C(Cl)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as gamma amino acids and derivatives. These are amino acids having a (-NH2) group attached to the gamma carbon atom.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentGamma amino acids and derivatives
Alternative Parents
Substituents
  • Gamma amino acid or derivatives
  • 3-phenylpropanoic-acid
  • Phenylpropylamine
  • Aralkylamine
  • Halobenzene
  • Chlorobenzene
  • Amino fatty acid
  • Fatty acyl
  • Benzenoid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Primary aliphatic amine
  • Carbonyl group
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor 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.
PharmacodynamicsBaclofen 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.
Mechanism of actionBaclofen 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.
Related Articles
AbsorptionRapidly and almost completely absorbed from the GI tract.
Volume of distribution
  • 59 L
Protein binding30%
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.

Route of eliminationIn a study using radiolabeled baclofen, approximately 85% of the dose was excreted unchanged in the urine and feces. Baclofen is excreted primarily by the kidney as unchanged drug; 70 - 80% of a dose appears in the urine as unchanged drug. The remainder is excreted as unchanged drug in the feces or as metabolites in the urine and feces.
Half life2.5-4 hours
Clearance
  • 180 mL/min
ToxicityLD50=45 mg/kg (male mice, IV); LD50=78 mg/kg (male rat, IV)
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.978
Blood Brain Barrier+0.9339
Caco-2 permeable+0.5668
P-glycoprotein substrateNon-substrate0.7373
P-glycoprotein inhibitor INon-inhibitor0.9825
P-glycoprotein inhibitor IINon-inhibitor0.9842
Renal organic cation transporterNon-inhibitor0.8435
CYP450 2C9 substrateNon-substrate0.8746
CYP450 2D6 substrateNon-substrate0.8426
CYP450 3A4 substrateNon-substrate0.7618
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.736
CYP450 2C19 inhibitorNon-inhibitor0.8215
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9204
Ames testNon AMES toxic0.8621
CarcinogenicityNon-carcinogens0.7401
BiodegradationNot ready biodegradable0.7362
Rat acute toxicity3.1364 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9478
hERG inhibition (predictor II)Non-inhibitor0.8578
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Medtronic inc
  • Schwarz pharma inc
  • Actavis totowa llc
  • Caraco pharmaceutical laboratories ltd
  • Impax laboratories inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Lannett holdings inc
  • Matrix laboratories ltd
  • Mylan pharmaceuticals inc
  • Northstar healthcare holdings ltd
  • Teva pharmaceuticals usa inc
  • Usl pharma inc
  • Vintage pharmaceuticals inc
  • Watson laboratories inc
  • Novartis pharmaceuticals corp
Packagers
Dosage forms
FormRouteStrength
Tabletoral10 mg/1
Tabletoral20 mg/1
Kittopical
Injectionintrathecal1000 ug/mL
Injectionintrathecal2000 ug/mL
Injectionintrathecal50 ug/mL
Injectionintrathecal500 ug/mL
Kittopical
Injectionintrathecal.05 mg/mL
Injectionintrathecal.5 mg/mL
Injectionintrathecal2 mg/mL
Solutionintrathecal0.05 mg
Solutionintrathecal0.5 mg
Solutionintrathecal2 mg
Tabletoral10 mg
Tabletoral20 mg
Prices
Unit descriptionCostUnit
Lioresal it 0.05 mg/1 ml amp84.0USD ml
Lioresal it 10 mg/5 ml kit51.6USD ml
Lioresal Intrathecal 2 mg/ml44.64USD ml
Lioresal Intrathecal 0.05 mg/ml14.89USD ml
Baclofen powder14.38USD g
Lioresal it 10 mg/20 ml kit12.9USD ml
Lioresal Intrathecal 0.5 mg/ml11.16USD ml
Lioresal D.S. 20 mg Tablet1.4USD tablet
Baclofen 20 mg tablet0.92USD tablet
Lioresal 10 mg Tablet0.72USD tablet
Apo-Baclofen 20 mg Tablet0.59USD tablet
Mylan-Baclofen 20 mg Tablet0.59USD tablet
Nu-Baclo 20 mg Tablet0.59USD tablet
Phl-Baclofen 20 mg Tablet0.59USD tablet
Pms-Baclofen 20 mg Tablet0.59USD tablet
Ratio-Baclofen 20 mg Tablet0.59USD tablet
Baclofen 10 mg tablet0.51USD tablet
Apo-Baclofen 10 mg Tablet0.3USD tablet
Mylan-Baclofen 10 mg Tablet0.3USD tablet
Nu-Baclo 10 mg Tablet0.3USD tablet
Phl-Baclofen 10 mg Tablet0.3USD tablet
Pms-Baclofen 10 mg Tablet0.3USD tablet
Ratio-Baclofen 10 mg Tablet0.3USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6024981 No1998-04-092018-04-09Us
US6221392 No1998-04-092018-04-09Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point206-208 °CKeberle, H., Faigle, J.W. and Wilhelm, M.; U.S. Patent 3,471,548; October 7, 1969; assigned to Ciba Corporation. Keberle, H., Faigle, J.W. and Wilhelm, M.; U.S. Patent 3,634,428; January 11, 1972; assigned to Ciba Corporation.
water solubility2090 mg/LNot Available
logP1.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.712 mg/mLALOGPS
logP-0.82ALOGPS
logP-0.78ChemAxon
logS-2.5ALOGPS
pKa (Strongest Acidic)3.89ChemAxon
pKa (Strongest Basic)9.79ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area63.32 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity54.83 m3·mol-1ChemAxon
Polarizability21.13 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
MSMass Spectrum (Electron Ionization)splash10-000i-2900000000-963f049a4367a1d5a5f5View in MoNA
References
Synthesis Reference

Wayne Levadoux, Denis Groleau, Michael Trani, Robert Lortie, “Streptomyces microorganism useful for the preparation of®-baclofen from the racemic mixture.” U.S. Patent US5843765, issued April, 1994.

US5843765
General References
  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:12692303 ]
  2. Mezler M, Muller T, Raming K: Cloning and functional expression of GABA(B) receptors from Drosophila. Eur J Neurosci. 2001 Feb;13(3):477-86. [PubMed:11168554 ]
  3. See S, Ginzburg R: Skeletal muscle relaxants. Pharmacotherapy. 2008 Feb;28(2):207-13. doi: 10.1592/phco.28.2.207. [PubMed:18225966 ]
External Links
ATC CodesM03BX01
AHFS Codes
  • 12:20.12
PDB EntriesNot Available
FDA labelDownload (135 KB)
MSDSDownload (73.4 KB)
Interactions
Drug Interactions
Drug
AcetaminophenThe risk or severity of adverse effects can be increased when Baclofen is combined with Acetaminophen.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Baclofen is combined with Acetylsalicylic acid.
AlfentanilThe risk or severity of adverse effects can be increased when Baclofen is combined with Alfentanil.
AlprazolamThe risk or severity of adverse effects can be increased when Baclofen is combined with Alprazolam.
AmitriptylineThe risk or severity of adverse effects can be increased when Baclofen is combined with Amitriptyline.
AmobarbitalThe risk or severity of adverse effects can be increased when Baclofen is combined with Amobarbital.
AmoxapineThe risk or severity of adverse effects can be increased when Baclofen is combined with Amoxapine.
AripiprazoleThe risk or severity of adverse effects can be increased when Baclofen is combined with Aripiprazole.
AsenapineThe risk or severity of adverse effects can be increased when Baclofen is combined with Asenapine.
AtropineThe risk or severity of adverse effects can be increased when Baclofen is combined with Atropine.
AzelastineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BrexpiprazoleThe risk or severity of adverse effects can be increased when Baclofen is combined with Brexpiprazole.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
BromazepamThe risk or severity of adverse effects can be increased when Baclofen is combined with Bromazepam.
BrompheniramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Brompheniramine.
BuprenorphineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BuspironeThe risk or severity of adverse effects can be increased when Baclofen is combined with Buspirone.
ButabarbitalThe risk or severity of adverse effects can be increased when Baclofen is combined with Butabarbital.
ButalbitalThe risk or severity of adverse effects can be increased when Baclofen is combined with Butalbital.
ButorphanolThe risk or severity of adverse effects can be increased when Baclofen is combined with Butorphanol.
CaffeineThe risk or severity of adverse effects can be increased when Baclofen is combined with Caffeine.
CarbamazepineThe risk or severity of adverse effects can be increased when Baclofen is combined with Carbamazepine.
CarbidopaThe risk or severity of adverse effects can be increased when Baclofen is combined with Carbidopa.
CarbinoxamineThe risk or severity of adverse effects can be increased when Baclofen is combined with Carbinoxamine.
CarisoprodolThe risk or severity of adverse effects can be increased when Baclofen is combined with Carisoprodol.
CetirizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Cetirizine.
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Baclofen is combined with Chlordiazepoxide.
ChlorphenamineThe risk or severity of adverse effects can be increased when Baclofen is combined with Chlorphenamine.
ChlorpromazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Chlorpromazine.
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Chlorzoxazone.
CitalopramThe risk or severity of adverse effects can be increased when Baclofen is combined with Citalopram.
ClemastineThe risk or severity of adverse effects can be increased when Baclofen is combined with Clemastine.
ClidiniumThe risk or severity of adverse effects can be increased when Baclofen is combined with Clidinium.
ClobazamThe risk or severity of adverse effects can be increased when Baclofen is combined with Clobazam.
ClofedanolThe risk or severity of adverse effects can be increased when Baclofen is combined with Clofedanol.
ClomipramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Clomipramine.
ClonazepamThe risk or severity of adverse effects can be increased when Baclofen is combined with Clonazepam.
ClonidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Clonidine.
ClorazepateThe risk or severity of adverse effects can be increased when Baclofen is combined with Clorazepate.
ClozapineThe risk or severity of adverse effects can be increased when Baclofen is combined with Clozapine.
CodeineThe risk or severity of adverse effects can be increased when Baclofen is combined with Codeine.
CyclizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Cyclizine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Baclofen is combined with Cyclobenzaprine.
CyproheptadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Cyproheptadine.
DantroleneThe risk or severity of adverse effects can be increased when Baclofen is combined with Dantrolene.
DesfluraneThe risk or severity of adverse effects can be increased when Baclofen is combined with Desflurane.
DesipramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Desipramine.
DesloratadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Desloratadine.
DexbrompheniramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Dexbrompheniramine.
Dexchlorpheniramine maleateThe risk or severity of adverse effects can be increased when Baclofen is combined with Dexchlorpheniramine maleate.
DiazepamThe risk or severity of adverse effects can be increased when Baclofen is combined with Diazepam.
DifenoxinThe risk or severity of adverse effects can be increased when Baclofen is combined with Difenoxin.
DihydrocodeineThe risk or severity of adverse effects can be increased when Baclofen is combined with Dihydrocodeine.
DimenhydrinateThe risk or severity of adverse effects can be increased when Baclofen is combined with Dimenhydrinate.
DiphenhydramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Diphenhydramine.
DiphenoxylateThe risk or severity of adverse effects can be increased when Baclofen is combined with Diphenoxylate.
DoxepinThe risk or severity of adverse effects can be increased when Baclofen is combined with Doxepin.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
EfavirenzThe risk or severity of adverse effects can be increased when Baclofen is combined with Efavirenz.
EntacaponeThe risk or severity of adverse effects can be increased when Baclofen is combined with Entacapone.
EscitalopramThe risk or severity of adverse effects can be increased when Baclofen is combined with Escitalopram.
EstazolamThe risk or severity of adverse effects can be increased when Baclofen is combined with Estazolam.
EszopicloneThe risk or severity of adverse effects can be increased when Baclofen is combined with Eszopiclone.
EthanolBaclofen may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthosuximideThe risk or severity of adverse effects can be increased when Baclofen is combined with Ethosuximide.
EthotoinThe risk or severity of adverse effects can be increased when Baclofen is combined with Ethotoin.
EzogabineThe risk or severity of adverse effects can be increased when Baclofen is combined with Ezogabine.
FelbamateThe risk or severity of adverse effects can be increased when Baclofen is combined with Felbamate.
FentanylThe risk or severity of adverse effects can be increased when Baclofen is combined with Fentanyl.
FexofenadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Fexofenadine.
FlibanserinThe risk or severity of adverse effects can be increased when Baclofen is combined with Flibanserin.
FlunarizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Flunarizine.
FluoxetineThe risk or severity of adverse effects can be increased when Baclofen is combined with Fluoxetine.
FlupentixolThe risk or severity of adverse effects can be increased when Baclofen is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Fluphenazine.
FlurazepamThe risk or severity of adverse effects can be increased when Baclofen is combined with Flurazepam.
Fluticasone PropionateBaclofen may increase the central nervous system depressant (CNS depressant) activities of Fluticasone Propionate.
FluvoxamineThe risk or severity of adverse effects can be increased when Baclofen is combined with Fluvoxamine.
FosphenytoinThe risk or severity of adverse effects can be increased when Baclofen is combined with Fosphenytoin.
GabapentinThe risk or severity of adverse effects can be increased when Baclofen is combined with Gabapentin.
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Baclofen is combined with gabapentin enacarbil.
Gamma Hydroxybutyric AcidGamma Hydroxybutyric Acid may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
GuanfacineThe risk or severity of adverse effects can be increased when Baclofen is combined with Guanfacine.
HaloperidolThe risk or severity of adverse effects can be increased when Baclofen is combined with Haloperidol.
HydrocodoneBaclofen may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydromorphoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Hydromorphone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
IloperidoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Iloperidone.
ImipramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Imipramine.
IsofluraneThe risk or severity of adverse effects can be increased when Baclofen is combined with Isoflurane.
KetamineThe risk or severity of adverse effects can be increased when Baclofen is combined with Ketamine.
LacidipineBaclofen may increase the hypotensive activities of Lacidipine.
LamotrigineThe risk or severity of adverse effects can be increased when Baclofen is combined with Lamotrigine.
LevetiracetamThe risk or severity of adverse effects can be increased when Baclofen is combined with Levetiracetam.
LevocetirizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Levocetirizine.
LevodopaThe risk or severity of adverse effects can be increased when Baclofen is combined with Levodopa.
LevorphanolThe risk or severity of adverse effects can be increased when Baclofen is combined with Levorphanol.
LoratadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Loratadine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Baclofen.
LoxapineThe risk or severity of adverse effects can be increased when Baclofen is combined with Loxapine.
LurasidoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Lurasidone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
MaprotilineThe risk or severity of adverse effects can be increased when Baclofen is combined with Maprotiline.
MeclizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Meclizine.
MeprobamateThe risk or severity of adverse effects can be increased when Baclofen is combined with Meprobamate.
MetaxaloneThe risk or severity of adverse effects can be increased when Baclofen is combined with Metaxalone.
MethadoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Methadone.
MethocarbamolThe risk or severity of adverse effects can be increased when Baclofen is combined with Methocarbamol.
MethohexitalThe risk or severity of adverse effects can be increased when Baclofen is combined with Methohexital.
MethotrimeprazineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethsuximideThe risk or severity of adverse effects can be increased when Baclofen is combined with Methsuximide.
MetyrosineBaclofen may increase the sedative activities of Metyrosine.
MidazolamThe risk or severity of adverse effects can be increased when Baclofen is combined with Midazolam.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
MirtazapineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MorphineThe risk or severity of adverse effects can be increased when Baclofen is combined with Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
NalbuphineThe risk or severity of adverse effects can be increased when Baclofen is combined with Nalbuphine.
NitrazepamThe risk or severity of adverse effects can be increased when Baclofen is combined with Nitrazepam.
Nitrous oxideThe risk or severity of adverse effects can be increased when Baclofen is combined with Nitrous oxide.
NortriptylineThe risk or severity of adverse effects can be increased when Baclofen is combined with Nortriptyline.
OlanzapineThe risk or severity of adverse effects can be increased when Baclofen is combined with Olanzapine.
OlopatadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Olopatadine.
OrphenadrineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OxazepamThe risk or severity of adverse effects can be increased when Baclofen is combined with Oxazepam.
OxycodoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Oxycodone.
OxymorphoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Oxymorphone.
PaliperidoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Paliperidone.
ParaldehydeBaclofen may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Baclofen is combined with Paroxetine.
PentazocineThe risk or severity of adverse effects can be increased when Baclofen is combined with Pentazocine.
PentobarbitalThe risk or severity of adverse effects can be increased when Baclofen is combined with Pentobarbital.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
PerphenazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Perphenazine.
PethidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Pethidine.
PhenobarbitalThe risk or severity of adverse effects can be increased when Baclofen is combined with Phenobarbital.
PhenytoinThe risk or severity of adverse effects can be increased when Baclofen is combined with Phenytoin.
PimozideThe risk or severity of adverse effects can be increased when Baclofen is combined with Pimozide.
PipotiazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Pipotiazine.
PizotifenThe risk or severity of adverse effects can be increased when Baclofen is combined with Pizotifen.
PomalidomideThe risk or severity of adverse effects can be increased when Baclofen is combined with Pomalidomide.
PramipexoleBaclofen may increase the sedative activities of Pramipexole.
PregabalinThe risk or severity of adverse effects can be increased when Baclofen is combined with Pregabalin.
PrimidoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Primidone.
ProchlorperazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Promazine.
PromethazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Promethazine.
PropofolThe risk or severity of adverse effects can be increased when Baclofen is combined with Propofol.
ProtriptylineThe risk or severity of adverse effects can be increased when Baclofen is combined with Protriptyline.
QuazepamThe risk or severity of adverse effects can be increased when Baclofen is combined with Quazepam.
QuetiapineThe risk or severity of adverse effects can be increased when Baclofen is combined with Quetiapine.
RamelteonThe risk or severity of adverse effects can be increased when Baclofen is combined with Ramelteon.
RemifentanilThe risk or severity of adverse effects can be increased when Baclofen is combined with Remifentanil.
ReserpineThe risk or severity of adverse effects can be increased when Baclofen is combined with Reserpine.
RisperidoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Risperidone.
RopiniroleBaclofen may increase the sedative activities of Ropinirole.
RotigotineBaclofen may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Baclofen.
ScopolamineThe risk or severity of adverse effects can be increased when Baclofen is combined with Scopolamine.
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Baclofen is combined with Scopolamine butylbromide.
SecobarbitalThe risk or severity of adverse effects can be increased when Baclofen is combined with Secobarbital.
SertralineThe risk or severity of adverse effects can be increased when Baclofen is combined with Sertraline.
SevofluraneThe risk or severity of adverse effects can be increased when Baclofen is combined with Sevoflurane.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
StiripentolThe risk or severity of adverse effects can be increased when Baclofen is combined with Stiripentol.
SufentanilThe risk or severity of adverse effects can be increased when Baclofen is combined with Sufentanil.
SuvorexantBaclofen may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
TasimelteonThe risk or severity of adverse effects can be increased when Baclofen is combined with Tasimelteon.
TemazepamThe risk or severity of adverse effects can be increased when Baclofen is combined with Temazepam.
TetrabenazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Tetrabenazine.
ThalidomideBaclofen may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Baclofen is combined with Thiothixene.
TiagabineThe risk or severity of adverse effects can be increased when Baclofen is combined with Tiagabine.
TizanidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Tizanidine.
TolcaponeThe risk or severity of adverse effects can be increased when Baclofen is combined with Tolcapone.
TopiramateThe risk or severity of adverse effects can be increased when Baclofen is combined with Topiramate.
TramadolThe risk or severity of adverse effects can be increased when Baclofen is combined with Tramadol.
TriazolamThe risk or severity of adverse effects can be increased when Baclofen is combined with Triazolam.
TrifluoperazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Trifluoperazine.
TrimipramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Trimipramine.
TriprolidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Triprolidine.
VigabatrinThe risk or severity of adverse effects can be increased when Baclofen is combined with Vigabatrin.
VilazodoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Vilazodone.
VortioxetineThe risk or severity of adverse effects can be increased when Baclofen is combined with Vortioxetine.
ZaleplonThe risk or severity of adverse effects can be increased when Baclofen is combined with Zaleplon.
ZiconotideThe risk or severity of adverse effects can be increased when Baclofen is combined with Ziconotide.
ZiprasidoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Ziprasidone.
ZolpidemBaclofen may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
ZonisamideThe risk or severity of adverse effects can be increased when Baclofen is combined with Zonisamide.
ZopicloneThe risk or severity of adverse effects can be increased when Baclofen is combined with Zopiclone.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Baclofen is combined with Zuclopenthixol.
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
G-protein coupled gaba receptor activity
Specific Function:
Component of a heterodimeric G-protein coupled receptor for GABA, formed by GABBR1 and GABBR2. Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such a...
Gene Name:
GABBR1
Uniprot ID:
Q9UBS5
Molecular Weight:
108319.4 Da
References
  1. Bowery NG: GABAB receptor pharmacology. Annu Rev Pharmacol Toxicol. 1993;33:109-47. [PubMed:8388192 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  3. Garcia-Gil L, de Miguel R, Romero J, Perez A, Ramos JA, Fernandez-Ruiz JJ: Perinatal delta9-tetrahydrocannabinol exposure augmented the magnitude of motor inhibition caused by GABA(B), but not GABA(A), receptor agonists in adult rats. Neurotoxicol Teratol. 1999 May-Jun;21(3):277-83. [PubMed:10386831 ]
  4. Lehmann A: GABAB receptors as drug targets to treat gastroesophageal reflux disease. Pharmacol Ther. 2009 Jun;122(3):239-45. doi: 10.1016/j.pharmthera.2009.02.008. Epub 2009 Mar 19. [PubMed:19303900 ]
  5. Motalli R, Louvel J, Tancredi V, Kurcewicz I, Wan-Chow-Wah D, Pumain R, Avoli M: GABA(B) receptor activation promotes seizure activity in the juvenile rat hippocampus. J Neurophysiol. 1999 Aug;82(2):638-47. [PubMed:10444662 ]
  6. Mott DD, Li Q, Okazaki MM, Turner DA, Lewis DV: GABAB-Receptor-mediated currents in interneurons of the dentate-hilus border. J Neurophysiol. 1999 Sep;82(3):1438-50. [PubMed:10482760 ]
  7. Ogasawara T, Itoh Y, Tamura M, Mushiroi T, Ukai Y, Kise M, Kimura K: Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer. Pharmacol Biochem Behav. 1999 Sep;64(1):41-52. [PubMed:10494996 ]
  8. Pittman QJ: The action is at the terminal. J Physiol. 1999 Nov 1;520 Pt 3:629. [PubMed:10545129 ]
  9. Stringer JL, Lorenzo N: The reduction in paired-pulse inhibition in the rat hippocampus by gabapentin is independent of GABA(B) receptor receptor activation. Epilepsy Res. 1999 Feb;33(2-3):169-76. [PubMed:10094428 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
G-protein coupled gaba receptor activity
Specific Function:
Component of a heterodimeric G-protein coupled receptor for GABA, formed by GABBR1 and GABBR2. Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such a...
Gene Name:
GABBR2
Uniprot ID:
O75899
Molecular Weight:
105820.52 Da
References
  1. Belley M, Sullivan R, Reeves A, Evans J, O'Neill G, Ng GY: Synthesis of the nanomolar photoaffinity GABA(B) receptor ligand CGP 71872 reveals diversity in the tissue distribution of GABA(B) receptor forms. Bioorg Med Chem. 1999 Dec;7(12):2697-704. [PubMed:10658574 ]
  2. Braun M, Wendt A, Buschard K, Salehi A, Sewing S, Gromada J, Rorsman P: GABAB receptor activation inhibits exocytosis in rat pancreatic beta-cells by G-protein-dependent activation of calcineurin. J Physiol. 2004 Sep 1;559(Pt 2):397-409. Epub 2004 Jul 2. [PubMed:15235087 ]
  3. Bowery NG: GABAB receptor pharmacology. Annu Rev Pharmacol Toxicol. 1993;33:109-47. [PubMed:8388192 ]
  4. Filippov AK, Couve A, Pangalos MN, Walsh FS, Brown DA, Moss SJ: Heteromeric assembly of GABA(B)R1 and GABA(B)R2 receptor subunits inhibits Ca(2+) current in sympathetic neurons. J Neurosci. 2000 Apr 15;20(8):2867-74. [PubMed:10751439 ]
  5. Jones KA, Tamm JA, Craig DA, Ph D, Yao W, Panico R: Signal transduction by GABA(B) receptor heterodimers. Neuropsychopharmacology. 2000 Oct;23(4 Suppl):S41-9. [PubMed:11008066 ]
  6. Lehmann A: GABAB receptors as drug targets to treat gastroesophageal reflux disease. Pharmacol Ther. 2009 Jun;122(3):239-45. doi: 10.1016/j.pharmthera.2009.02.008. Epub 2009 Mar 19. [PubMed:19303900 ]
  7. Martin SC, Russek SJ, Farb DH: Molecular identification of the human GABABR2: cell surface expression and coupling to adenylyl cyclase in the absence of GABABR1. Mol Cell Neurosci. 1999 Mar;13(3):180-91. [PubMed:10328880 ]
  8. Pittman QJ: The action is at the terminal. J Physiol. 1999 Nov 1;520 Pt 3:629. [PubMed:10545129 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenadine. Transports benzylpenicillin (PCG), estrone-3-sulfate (E1S), cimetidine (CMD), 2,4-dichloro-phenoxyacetate (2,4-D), p-amino-hippurate (PAH), acyclovir (ACV) and ochratoxin (OTA).
Gene Name:
SLC22A8
Uniprot ID:
Q8TCC7
Molecular Weight:
59855.585 Da
References
  1. Ohtsuki S, Asaba H, Takanaga H, Deguchi T, Hosoya K, Otagiri M, Terasaki T: Role of blood-brain barrier organic anion transporter 3 (OAT3) in the efflux of indoxyl sulfate, a uremic toxin: its involvement in neurotransmitter metabolite clearance from the brain. J Neurochem. 2002 Oct;83(1):57-66. [PubMed:12358729 ]
  2. Mori S, Takanaga H, Ohtsuki S, Deguchi T, Kang YS, Hosoya K, Terasaki T: Rat organic anion transporter 3 (rOAT3) is responsible for brain-to-blood efflux of homovanillic acid at the abluminal membrane of brain capillary endothelial cells. J Cereb Blood Flow Metab. 2003 Apr;23(4):432-40. [PubMed:12679720 ]
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Drug created on June 13, 2005 07:24 / Updated on June 26, 2016 01:52