Investigational Drug Details
| Drug ID: | D062 |
| Drug Name: | Pregabalin |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00230 |
| DrugBank Description: | Pregabalin is structurally similar to gamma-aminobutyric acid (GABA) - an inhibitory neurotransmitter.[A173995] It may be used to manage neuropathic pain, postherpetic neuralgia, and fibromyalgia among other conditions.[A187190] Although as per the FDA Label the mechanism of action has not been definitively defined, there is evidence that pregabalin exerts its effects by binding to the α2δ subunit of voltage-dependent calcium channels.[A187190][L7066] Pregabalin is marketed by Pfizer under the trade name Lyrica and Lyrica Cr (extended release).[L1006][L7066] It may have dependence liability if misused but the risk appears to be highest in patients with current or past substance use disorders.[A31161] |
| PubChem ID: | 5486971 |
| CasNo: | 148553-50-8 |
| Repositioning for NAFLD: | Yes |
| SMILES: | CC(C)C[C@H](CN)CC(O)=O |
| Structure: |
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| InChiKey: | AYXYPKUFHZROOJ-ZETCQYMHSA-N |
| Molecular Weight: | 159.2261 |
| DrugBank Targets: | Voltage-dependent calcium channel subunit alpha-2/delta-1 |
| DrugBank MoA: | Although the mechanism of action has not been fully elucidated, studies involving structurally related drugs suggest that presynaptic binding of pregabalin to voltage-gated calcium channels is key to the antiseizure and antinociceptive effects observed in animal models.[L7066] By binding presynaptically to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, pregabalin modulates the release of several excitatory neurotransmitters including glutamate, substance-P, norepinephrine, and calcitonin gene related peptide.[A31163] In addition, pregabalin prevents the alpha2-delta subunit from being trafficked from the dorsal root ganglia to the spinal dorsal horn, which may also contribute to the mechanism of action.[A36628] Although pregabalin is a structural derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABA or benzodiazepine receptors.[A31165] |
| DrugBank Pharmacology: | Although the structure of pregabalin is similar to gamma-aminobutyric acid (GABA), it does not bind to GABA receptors.[A31163][A187190] Instead, it binds the alpha2-delta subunit of presynaptic voltage-gated calcium channels in the central nervous system.[A31163][A187190] Pregabalin does not modulate dopamine receptors, serotonin receptors, opiate receptors, sodium channels or cyclooxygenase activity.[A187190] |
| DrugBank Indication: | Pregabalin is indicated for the management of neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia, fibromyalgia, neuropathic pain associated with spinal cord injury, and as adjunctive therapy for the treatment of partial-onset seizures in patients 1 month of age and older.[L7066] |
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