Repositioning Candidate Details
| Candidate ID: | R0067 |
| Source ID: | DB00181 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Baclofen |
| Synonyms: | (+-)-Baclofen; 4-Amino-3-(4-chlorophenyl)butyric acid; Baclofen; 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 |
| Molecular Formula: | C10H12ClNO2 |
| SMILES: | NCC(CC(O)=O)C1=CC=C(Cl)C=C1 |
| Structure: |
|
| DrugBank Description: | Baclofen is a gamma-aminobutyric acid (GABA) agonist used as a skeletal muscle relaxant used for the relief of painful and uncomfortable muscle spasms caused by a variety of conditions. It is particularly useful in treating muscle spasticity associated with spinal cord injury. This drug has recently been studied for the management of alcohol withdrawal, however, a conclusion has not been made regarding baclofen efficacy in this condition. This drug was first approved by the FDA in 1992. |
| CAS Number: | 1134-47-0 |
| Molecular Weight: | 213.661 |
| DrugBank Indication: | 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 of value in the treatment of patients with spinal cord injuries or diseases. Baclofen is also indicated as an intrathecal injection for the management of severe spasticity of cerebral or spinal original in patients 4 years of age and older. Patients who respond to bolus intrathecal doses of baclofen, and who require chronic therapy, can use an implantable intrathecal pump to administer baclofen via long-term infusion. |
| DrugBank Pharmacology: | In neurological diseases associated with spasm of the skeletal muscles, the clinical effects of baclofen occur due to baclofen action on reflex muscle contractions and of significant relief from painful spasm, automatism, as well as clonus. Baclofen, when used as indicated, improves mobility, increasing levels of independence, and facilitates both passive and active physiotherapy. Baclofen also stimulates gastric acid secretion . GABA-B receptor activation by baclofen may produce protective neurological effects. Baclofen also possesses anti-inflammatory properties that may be of interest in the study of addiction treatment . Preclinical studies have shown that GABA-B receptors have roles in memory storage and retrieval, reward, motivation, mood, as well as anxiety. Neuroimaging studies in humans indicate that baclofen produces region-specific alterations in brain activity. |
| DrugBank MoA: | The exact mechanism of action of baclofen is not fully understood at this time , . Many studies indicate that baclofen is a GABA-B receptor agonist , , , , . Despite this, there is no conclusive evidence that the effects of baclofen on GABA systems are involved in the production of its clinical effects . Baclofen is an effective and widely used antispastic agent with a spinal site of action. Its mechanism of action and pharmacological properties are different from the effects of other antispastic agents. In addition, baclofen has central sites of action, shown by its adverse event profile and general CNS depressant properties . GABA-B receptors interact with signal transduction pathways and neurotransmitter systems. Baclofen exerts an antinociceptive effect. The clinical significance of this warrants further research data for clarification. Baclofen depresses monosynaptic and polysynaptic reflex transmission, by various actions, and possibly including the stimulation of GABAβ-receptors. This stimulation results in the inhibition of excitatory neurotransmitter (glutamate and aspartate) release, which may normally contribute to pain and spasticity. Although baclofen is an analog of the inhibitory neurotransmitter gamma-amino-butyric acid (GABA), there are no conclusive data indicating GABA systems are involved in its clinical effects . |
| Targets: | Gamma-aminobutyric acid type B receptor subunit 1 agonist; Gamma-aminobutyric acid type B receptor subunit 2 agonist |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Diseases ID | DO ID | Disease Name | Definition | Class |
|---|