Identification

Summary

Baclofen is a GABA-ergic agonist used to manage severe spasticity of cerebral or spinal origin in adult and pediatric patients.

Brand Names
Fleqsuvy, Gablofen, Kemstro, Lioresal, Lyvispah, Ozobax
Generic Name
Baclofen
DrugBank Accession Number
DB00181
Background

Baclofen is a gamma-aminobutyric acid (GABA) agonist used as a skeletal muscle relaxant. Although originally designed in 1962 to treat epilepsy, baclofen was not effective in treating this condition but instead was shown to reduce spasticity in selected patients.8 Baclofen was reintroduced in 1971 as a treatment for spasticity and was later approved by the FDA in 1977.6,8 Baclofen is used to manage severe muscle spasms of cerebral or spinal cord origins, including multiple sclerosis and traumatic brain injury.11

Baclofen was investigated for use in alcohol dependence and withdrawal; however, evidence is limited and there is inconsistent evidence to suggest its clinical efficacy in managing alcohol dependence or withdrawal symptoms.1,2,8

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 213.661
Monoisotopic: 213.05565634
Chemical Formula
C10H12ClNO2
Synonyms
  • (+-)-Baclofen
  • 4-Amino-3-(4-chlorophenyl)butyric acid
  • Baclofen
  • Baclofène
  • 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

Pharmacology

Indication

Oral baclofen is indicated for the treatment of spasticity resulting from multiple sclerosis and is particularly useful for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity. It may also be used to treat patients with spinal cord injuries and other spinal cord diseases. Baclofen should not be used to treat skeletal muscle spasms resulting from rheumatic disorders.12

Intrathecal baclofen is also indicated for the management of severe spasticity of the cerebral or spinal original in patients 4 years of age and older. It is reserved for patients unresponsive to oral baclofen therapy, or those who experience intolerable central nervous system side effects at effective doses. For use in spasticity due to traumatic brain injury, baclofen should be considered after at least one year of injury.11

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Baclofen is an antispasmodic agent that induces muscle relaxation. It reduces the release of excitatory neurotransmitters in the pre-synaptic neurons and stimulates inhibitory neuronal signals in the post-synaptic neurons.6 Oral formulations of baclofen are the most commonly used form of the drug. In one cross-section study, intrathecal baclofen was more effective than oral baclofen in relieving spasticity directly at the level of the spinal cord.8 Baclofen has CNS depression properties and can cause sedation with tolerance, somnolence, ataxia, and respiratory and cardiovascular depression.13 Baclofen also mediates some antinociceptive effects and stimulates gastric acid secretion.15

Baclofen exhibits anti-inflammatory and neuroprotective activities: it inhibits the release of pro-inflammatory cytokines from microglia and astrocytes, and decreases oxidative stress in rats.5

Mechanism of action

The exact mechanism of action of baclofen is unclear. Baclofen is an agonist at the beta subunit of gamma-aminobutyric acid (GABA) receptors expressed on pre- and post-synaptic neurons.3 Upon binding to GABAB receptors, baclofen causes an influx of potassium into the neuron, leading to hyperpolarization of the neuronal membrane and decreased calcium influx at presynaptic nerve terminals. This results in a decreased rate of action potential threshold being reached by presynaptic neurons and reduced action potential of postsynaptic motor neurons that innervate the muscle spindles. Baclofen thereby inhibits the transmission of both mono- and polysynaptic reflexes at the spinal cord, relaxing spasticity.8 Baclofen may act on some voltage-gated calcium channels; however, the clinical significance of this is unclear.6

TargetActionsOrganism
AGamma-aminobutyric acid type B receptor subunit 2
agonist
Humans
UC-X-C chemokine receptor type 4
allosteric modulator
Humans
UGamma-aminobutyric acid type B receptor subunit 1
agonist
Humans
Absorption

Baclofen has an oral bioavailability of 70% to 85%. Following oral administration, it is rapidly absorbed through the gastrointestinal tract with peak plasma concentrations being reached two to three hours after ingestion.6 Peak effect is observed about four hours after intrathecal administration.8 The absorption is dose-dependent and increases with higher doses.6 There is intersubject variation in absorption.13

Administration of oral baclofen suspension with a high-fat meal resulted in 9% decrease in AUC and 33% decrease in Cmax compared to the fasted state.13

Volume of distribution

The volume of distribution of baclofen is 0.7 L/kg.15 As baclofen is mainly water-soluble, it does not readily cross the blood-brain barrier.7 Drug concentrations of baclofen in the cerebrospinal fluid are approximately 8.5 times lower than in the plasma.15

Protein binding

The protein binding is approximately 30%.15

Metabolism

Approximately 15% of the oral dose is metabolized in the liver, mainly by deamination.8 Deamination yields the main metabolite, β-(p-chlorophenyl)-4-hydroxybutyric acid, which is pharmacologically inactive.15

Hover over products below to view reaction partners

Route of elimination

About 70-80% of baclofen is eliminated in an unchanged form by renal excretion 6,8 within 72 hours of administration. About 5% of the dose is excreted via the kidneys as metabolites.15 There is intersubject variation in elimination.13

Half-life

The half-life is 2-6 hours after oral administration and 1-5 hours following intrathecal administration.8 The apparent elimination half-life of baclofen oral suspension or granules is about 5.6 hours.13

Clearance

The systemic clearance (CL/F) was 180 mL/min and the renal clearance was 103 mL/min following oral administration.10

Adverse Effects
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Toxicity

The oral LD50 in rats is 145 mg/kg.14

Baclofen withdrawal symptoms typically occur within hours to days following interruption of either oral or intrathecal drug formulations.8 Abrupt discontinuation of baclofen is not advised.11 Clinical manifestations of baclofen overdose may include altered mental status, somnolence, seizure, hypothermia, respiratory depression, and coma. Overdose from baclofen oral tablets resulted in vomiting, lightheadedness, drowsiness, muscular hypotonia, accommodation disorders, coma, respiratory depression, and seizures.6,13 Most overdose symptoms are neurological but uncommon cardiovascular effects such as hypertension, bradycardia, and tachycardia may be observed.9 In case of overdose, symptomatic treatment and gastric decontamination should be initiated. When the patient is alert, gastric emptying should be performed by inducing emesis and then performing lavage while maintaining an adequate airway and respiration. Emesis should not be induced in unconscious patients.6,13

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
1,2-BenzodiazepineBaclofen may increase the central nervous system depressant (CNS depressant) activities of 1,2-Benzodiazepine.
AbacavirBaclofen may decrease the excretion rate of Abacavir which could result in a higher serum level.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Baclofen.
AcebutololThe risk or severity of adverse effects can be increased when Baclofen is combined with Acebutolol.
AceclofenacAceclofenac may decrease the excretion rate of Baclofen which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Baclofen which could result in a higher serum level.
AcetaminophenBaclofen may decrease the excretion rate of Acetaminophen which could result in a higher serum level.
AcetazolamideBaclofen may increase the central nervous system depressant (CNS depressant) activities of Acetazolamide.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Baclofen.
AcetophenazineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Acetophenazine.
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Food Interactions
  • Avoid alcohol.
  • Take with food. Take with food or milk to reduce gastric irritation.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Baclofen hydrochloride64OSE3996V28311-31-1WMNUVYYLMCMHLU-UHFFFAOYSA-N
Product Images
International/Other Brands
Baclon (Uniao Quimica (Brazil)) / Lioresal Intrathecal (Novartis Pharmaceuticals) / Nu-Baclofen (Nu-Pharm)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BaclofenTablet20 mgOralApotex Corporation1994-12-312014-08-23Canada flag
BaclofenTablet20 mgOralSanis Health Inc2010-02-25Not applicableCanada flag
BaclofenTablet20 mg/1OralCaraco Pharmaceutical Laboratories, Ltd.2007-03-30Not applicableUS flag
BaclofenTablet20 mg/1OralVintage Pharmaceuticals, LLC2007-05-172007-05-17US flag
BaclofenTablet10 mgOralApotex Corporation1994-12-312014-08-23Canada flag
BaclofenTablet10 mgOralSanis Health Inc2010-02-25Not applicableCanada flag
BaclofenTablet10 mg/1OralCaraco Pharmaceutical Laboratories, Ltd.2007-03-30Not applicableUS flag
BaclofenTablet10 mg/1OralVintage Pharmaceuticals, LLC2007-05-172007-05-17US flag
Baclofen InjectionSolution2 mg / mLIntrathecalHikma Canada Limited2017-08-25Not applicableCanada flag
Baclofen InjectionSolution10 mg / 5 mLIntrathecalSterimax Inc2014-06-06Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-baclofenTablet20 mgOralApotex Corporation1994-12-31Not applicableCanada flag
Apo-baclofenTablet10 mgOralApotex Corporation1994-12-31Not applicableCanada flag
Ava-baclofenTablet20 mgOralAvanstra Inc2011-10-112014-08-21Canada flag
Ava-baclofenTablet10 mgOralAvanstra Inc2011-10-112014-08-21Canada flag
BaclofenTablet5 mg/1OralLifestar Pharma Llc2022-01-26Not applicableUS flag
BaclofenTablet20 mg/1OralMed Pharma Co., Ltd.2011-01-01Not applicableUS flag
BaclofenTablet20 mg/1OralPhysicians Total Care, Inc.2009-04-17Not applicableUS flag
BaclofenTablet10 mg/1OralAmerincan Health Packaging2012-09-032015-10-31US flag
BaclofenTablet20 mg/1OralCardinal Health1988-07-212015-05-31US flag
BaclofenTablet20 mg/1OralNucare Pharmaceuticals, Inc.2005-12-01Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Equipto - Baclofen External Cream Compounding KitBaclofen (1 g/1g)KitTopicalAlvix Laboratories2015-01-202018-03-08US flag
Gapeam BudibacBaclofen (1 g/1g) + Amantadine hydrochloride (1 g/1g) + Bupivacaine hydrochloride anhydrous (1 g/1g) + Cyclobenzaprine hydrochloride (1 g/1g) + Diclofenac sodium (1 g/1g) + Gabapentin (1 g/1g) + Pentoxifylline (1 g/1g)KitTopicalAlvix Laboratories2014-12-052018-03-08US flag
Innoprax-5Baclofen (3 g/3g) + Amantadine hydrochloride (8 g/8g) + Diclofenac sodium (3 g/3g) + Gabapentin (6 g/6g) + Lidocaine hydrochloride (5 g/5g)KitTopicalAccumix Pharmaceuticals2014-12-152015-07-17US flag

Categories

ATC Codes
M03BX01 — Baclofen
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This 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.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Gamma amino acids and derivatives
Alternative Parents
Phenylpropanoic acids / Chlorobenzenes / Aralkylamines / Amino fatty acids / Aryl chlorides / Amino acids / Monocarboxylic acids and derivatives / Carboxylic acids / Organopnictogen compounds / Organochlorides
show 4 more
Substituents
3-phenylpropanoic-acid / Amine / Amino acid / Amino fatty acid / Aralkylamine / Aromatic homomonocyclic compound / Aryl chloride / Aryl halide / Benzenoid / Carbonyl group
show 18 more
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
monocarboxylic acid, primary amino compound, monochlorobenzenes, gamma-amino acid (CHEBI:2972)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
H789N3FKE8
CAS number
1134-47-0
InChI Key
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

References

Synthesis Reference
US5843765
General References
  1. Brennan JL, Leung JG, Gagliardi JP, Rivelli SK, Muzyk AJ: Clinical effectiveness of baclofen for the treatment of alcohol dependence: a review. Clin Pharmacol. 2013 Jul 3;5:99-107. doi: 10.2147/CPAA.S32434. Print 2013. [Article]
  2. Liu J, Wang LN: Baclofen for alcohol withdrawal. Cochrane Database Syst Rev. 2017 Aug 20;8:CD008502. doi: 10.1002/14651858.CD008502.pub5. [Article]
  3. Chen K, Li HZ, Ye N, Zhang J, Wang JJ: Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro. Brain Res Bull. 2005 Oct 30;67(4):310-8. doi: 10.1016/j.brainresbull.2005.07.004. [Article]
  4. Fu Z, Yang H, Xiao Y, Zhao G, Huang H: The gamma-aminobutyric acid type B (GABAB) receptor agonist baclofen inhibits morphine sensitization by decreasing the dopamine level in rat nucleus accumbens. Behav Brain Funct. 2012 Jul 10;8:20. doi: 10.1186/1744-9081-8-20. [Article]
  5. de Beaurepaire R: A Review of the Potential Mechanisms of Action of Baclofen in Alcohol Use Disorder. Front Psychiatry. 2018 Oct 17;9:506. doi: 10.3389/fpsyt.2018.00506. eCollection 2018. [Article]
  6. Ghanavatian S, Derian A: Baclofen . [Article]
  7. Ertzgaard P, Campo C, Calabrese A: Efficacy and safety of oral baclofen in the management of spasticity: A rationale for intrathecal baclofen. J Rehabil Med. 2017 Mar 6;49(3):193-203. doi: 10.2340/16501977-2211. [Article]
  8. Romito JW, Turner ER, Rosener JA, Coldiron L, Udipi A, Nohrn L, Tausiani J, Romito BT: Baclofen therapeutics, toxicity, and withdrawal: A narrative review. SAGE Open Med. 2021 Jun 3;9:20503121211022197. doi: 10.1177/20503121211022197. eCollection 2021. [Article]
  9. Leung NY, Whyte IM, Isbister GK: Baclofen overdose: defining the spectrum of toxicity. Emerg Med Australas. 2006 Feb;18(1):77-82. doi: 10.1111/j.1742-6723.2006.00805.x. [Article]
  10. Kochak GM, Rakhit A, Wagner WE, Honc F, Waldes L, Kershaw RA: The pharmacokinetics of baclofen derived from intestinal infusion. Clin Pharmacol Ther. 1985 Sep;38(3):251-7. doi: 10.1038/clpt.1985.167. [Article]
  11. FDA Approved Drug Products: Gablofen (baclofen) for intrathecal injection [Link]
  12. FDA Approved Drug Products: Lyvispah (baclofen) oral granules [Link]
  13. FDA Approved Drug Products: FLEQSUVY (baclofen) oral suspension [Link]
  14. Cayman Chemical: Baclofen MSDS [Link]
  15. EMC Summary of Product Characteristics: Baclofen Oral Tablets [Link]
Human Metabolome Database
HMDB0014327
KEGG Drug
D00241
PubChem Compound
2284
PubChem Substance
46508181
ChemSpider
2197
BindingDB
24182
RxNav
1292
ChEBI
2972
ChEMBL
CHEMBL701
Therapeutic Targets Database
DAP000257
PharmGKB
PA448533
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Baclofen

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceSpasticity, Muscle1
4CompletedSupportive CareCerebral Palsy (CP) / Excessive crying / Pain1
4CompletedSupportive CareSpasticity, Muscle1
4CompletedTreatmentAlcohol Dependency1
4CompletedTreatmentAlcohol Use Disorders (AUD) / Hepatitis C Virus (HCV) Infection1
4CompletedTreatmentBack Pain Lower Back1
4CompletedTreatmentRecurrent Crying Spells1
4CompletedTreatmentRumination Disorders / Supra-gastric Belching1
4CompletedTreatmentSevere Spasticity1
4CompletedTreatmentSpastic Hemiplegia / Stroke; Sequelae1

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
  • Actavis Group
  • Advanced Pharmaceutical Services Inc.
  • Aidarex Pharmacuticals LLC
  • Alphapharm Party Ltd.
  • Amerisource Health Services Corp.
  • Apotheca Inc.
  • A-S Medication Solutions LLC
  • Bryant Ranch Prepack
  • Caraco Pharmaceutical Labs
  • Cardinal Health
  • Caremark LLC
  • Comprehensive Consultant Services Inc.
  • Corepharma LLC
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Genpharm LP
  • Heartland Repack Services LLC
  • Innoviant Pharmacy Inc.
  • Ivax Pharmaceuticals
  • Keltman Pharmaceuticals Inc.
  • Lake Erie Medical and Surgical Supply
  • Lannett Co. Inc.
  • Major Pharmaceuticals
  • Mckesson Corp.
  • Medisca Inc.
  • Medtronic
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Northstar Rx LLC
  • Novartis AG
  • Nucare Pharmaceuticals Inc.
  • Palmetto Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Pharmaceutical Packaging Center
  • Physicians Total Care Inc.
  • Piramal Healthcare
  • Preferred Pharmaceuticals Inc.
  • Prepak Systems Inc.
  • Prescription Dispensing Service Inc.
  • Qualitest
  • Rebel Distributors Corp.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Sandhills Packaging Inc.
  • Southwood Pharmaceuticals
  • St Mary's Medical Park Pharmacy
  • Stat Rx Usa
  • UDL Laboratories
  • United Research Laboratories Inc.
  • USL Pharma Inc.
  • Vangard Labs Inc.
  • Vintage Pharmaceuticals Inc.
  • Watson Pharmaceuticals
Dosage Forms
FormRouteStrength
Injection, solutionIntrathecal10 mg/20mL
Injection, solutionIntrathecal1000 ug/1mL
Injection, solutionIntrathecal40 mg/20mL
TabletOral5 mg/1
InjectionIntrathecal10 mg/20mL
InjectionIntrathecal40 mg/20mL
SolutionIntrathecal0.05 mg
SolutionIntrathecal10 mg
SolutionIntrathecal40 mg
SolutionIntrathecal0.05 mg / 1 mL
SolutionIntrathecal10 mg / 5 mL
SolutionIntrathecal10 mg / 20 mL
Injection, solutionIntrathecal0.05 mg/ml
SolutionIntrathecal0.05 mg/ml
Injection, solutionIntrathecal0.5 mg/ml
SolutionIntrathecal0.5 mg/ml
Injection, solutionIntrathecal2 mg/ml
SolutionIntrathecal2 mg/ml
Injection, solutionParenteral
SolutionParenteral
InjectionParenteral
TabletOral20 mg / tab
TabletOral25 MG
Injection, solution
InjectionIntrathecal
SolutionOral1 mg
TabletOral10 mg/1
TabletOral20 mg/1
KitTopical1 g/1g
SuspensionOral5 mg/1mL
InjectionIntrathecal1000 ug/1mL
InjectionIntrathecal2000 ug/1mL
InjectionIntrathecal50 ug/1mL
InjectionIntrathecal500 ug/1mL
Injection, solutionIntrathecal2000 ug/1mL
Injection, solutionIntrathecal50 ug/1mL
Injection, solutionIntrathecal500 ug/1mL
KitTopical
Tablet, orally disintegratingOral10 mg/1
Tablet, orally disintegratingOral20 mg/1
InjectionIntrathecal0.05 mg/1mL
InjectionIntrathecal0.5 mg/1mL
InjectionIntrathecal2 mg/1mL
Injection, solutionIntrathecal0.05 MG/1ML
Injection, solutionIntrathecal10 MG/5ML
InjectionIntrathecal10 mg/5mL
TabletOral
TabletOral10 mg
TabletOral5 mg
SolutionIntrathecal0.05 mg / mL
SolutionIntrathecal0.5 mg / mL
SolutionIntrathecal2 mg / mL
SolutionIntrathecal
GranuleOral10 mg/1
GranuleOral20 mg/1
GranuleOral5 mg/1
TabletOral20 mg
SolutionOral5 mg/5mL
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)Region
US6221392No2001-04-242018-04-09US flag
US6024981No2000-02-152018-04-09US flag
US10610502No2020-04-072039-08-30US flag
US10792262No2020-10-062039-07-29US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility4 mg/mLhttps://cdn.caymanchem.com/cdn/msds/18600m.pdf
logP1.3http://www.hmdb.ca/metabolites/HMDB0014327
Caco2 permeability0.9 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6186984/
pKa9.62 + 0.1 (amino group) and 3.87 + 0.1 (carboxyl group)http://www.labriva.com/monographies/02242151eng.pdf
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 FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-000i-2900000000-963f049a4367a1d5a5f5
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-03dr-0950000000-33d21cbb6740c1f1aee1
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-03di-1590000000-8a64733764308ba98f9a
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0f6t-0900000000-6647c58db763b4df68a0
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0udi-0900000000-72d6d878c9c2f29d846a
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-014i-1900000000-18f69033596a03ee643a
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-014i-1900000000-997473c303f07afcdf4e
LC-MS/MS Spectrum - LC-ESI-IT , positiveLC-MS/MSsplash10-0002-0900000000-d1da4625d180fe0af521
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-03di-0190000000-bd0fff49defde62ed0fa
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0ik9-0790000000-1a50b0b7f24aaaf6a87e

Targets

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Kind
Protein
Organism
Humans
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 coup...
Gene Name
GABBR2
Uniprot ID
O75899
Uniprot Name
Gamma-aminobutyric acid type B receptor subunit 2
Molecular Weight
105820.52 Da
References
  1. 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. [Article]
  2. Bowery NG: GABAB receptor pharmacology. Annu Rev Pharmacol Toxicol. 1993;33:109-47. [Article]
  3. 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. [Article]
  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. [Article]
  5. 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. [Article]
  6. Pittman QJ: The action is at the terminal. J Physiol. 1999 Nov 1;520 Pt 3:629. [Article]
  7. Fu Z, Yang H, Xiao Y, Zhao G, Huang H: The gamma-aminobutyric acid type B (GABAB) receptor agonist baclofen inhibits morphine sensitization by decreasing the dopamine level in rat nucleus accumbens. Behav Brain Funct. 2012 Jul 10;8:20. doi: 10.1186/1744-9081-8-20. [Article]
  8. Chen K, Li HZ, Ye N, Zhang J, Wang JJ: Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro. Brain Res Bull. 2005 Oct 30;67(4):310-8. doi: 10.1016/j.brainresbull.2005.07.004. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Allosteric modulator
General Function
Virus receptor activity
Specific Function
Receptor for the C-X-C chemokine CXCL12/SDF-1 that transduces a signal by increasing intracellular calcium ion levels and enhancing MAPK1/MAPK3 activation. Acts as a receptor for extracellular ubiq...
Gene Name
CXCR4
Uniprot ID
P61073
Uniprot Name
C-X-C chemokine receptor type 4
Molecular Weight
39745.055 Da
References
  1. Guyon A, Kussrow A, Olmsted IR, Sandoz G, Bornhop DJ, Nahon JL: Baclofen and other GABAB receptor agents are allosteric modulators of the CXCL12 chemokine receptor CXCR4. J Neurosci. 2013 Jul 10;33(28):11643-54. doi: 10.1523/JNEUROSCI.6070-11.2013. [Article]
  2. de Beaurepaire R: A Review of the Potential Mechanisms of Action of Baclofen in Alcohol Use Disorder. Front Psychiatry. 2018 Oct 17;9:506. doi: 10.3389/fpsyt.2018.00506. eCollection 2018. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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 coup...
Gene Name
GABBR1
Uniprot ID
Q9UBS5
Uniprot Name
Gamma-aminobutyric acid type B receptor subunit 1
Molecular Weight
108319.4 Da
References
  1. Bowery NG: GABAB receptor pharmacology. Annu Rev Pharmacol Toxicol. 1993;33:109-47. [Article]
  2. 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. [Article]
  3. 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. [Article]
  4. 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. [Article]
  5. 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. [Article]
  6. 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. [Article]
  7. Pittman QJ: The action is at the terminal. J Physiol. 1999 Nov 1;520 Pt 3:629. [Article]
  8. 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. [Article]
  9. Fu Z, Yang H, Xiao Y, Zhao G, Huang H: The gamma-aminobutyric acid type B (GABAB) receptor agonist baclofen inhibits morphine sensitization by decreasing the dopamine level in rat nucleus accumbens. Behav Brain Funct. 2012 Jul 10;8:20. doi: 10.1186/1744-9081-8-20. [Article]
  10. Chen K, Li HZ, Ye N, Zhang J, Wang JJ: Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro. Brain Res Bull. 2005 Oct 30;67(4):310-8. doi: 10.1016/j.brainresbull.2005.07.004. [Article]
  11. Omari TI, Benninga MA, Sansom L, Butler RN, Dent J, Davidson GP: Effect of baclofen on esophagogastric motility and gastroesophageal reflux in children with gastroesophageal reflux disease: a randomized controlled trial. J Pediatr. 2006 Oct;149(4):468-74. doi: 10.1016/j.jpeds.2006.05.029. [Article]

Drug created at June 13, 2005 13:24 / Updated at June 27, 2022 14:55