Tiagabine

Category: pharmacological

Aliases: Gabitril

Pharmacological Mechanism

Selective GAT-1 GABA-reuptake inhibitor — increases synaptic GABA dwell time → enhanced inhibitory tone in cortex / hippocampus. FDA-approved for partial seizures (adjunct). Off-label for anxiety + sleep architecture studies. Highly protein-bound (~96%); extensive CYP3A4 metabolism.

Half-Life (t½)

PO: 7h

Dosing Guidelines

• PO: Typical 32 mg (Range: 4–56 mg)

Target Organ Systems

• nervous

Pathways It Modulates

• GABA-A receptor signaling (inhibitor) — GAT-1 (GABA transporter)

Chemical Identifiers

• PubChem CID: 60648
• Formula: C20H25NO2S2
• Molecular weight: 412 g/mol
• InChIKey: PBJUNZJWGZTSKL-MRXNPFEDSA-N
• SMILES: CC1=C(SC=C1)C(=CCCN2CCC[C@H](C2)C(=O)O)C3=C(C=CS3)C

References

• PMID 2299358