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1 INNClassRoute (list)PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that value was calculated using VD=(Cl*t1/2)/0.693)Primary Target and PDB code of Protein-Drug complexTargets from DrugCentral Links
TIAGABINE

TIAGABINE


ATC N03AG06

NERVOUS SYSTEM
ANTICONVULSANT
ENHANCE THE ACTIVITY OF GABA
NEUROPROTECTIVE AGENTS

ORAL

Tmax 0.75 HOUR

F 90 PERCENT

VD 71.5 LITER (65 KILOGRAM)

PPB 96 PERCENT

Cl 6.5 LITER / HOUR

HT 8 HOUR

SOLUBILITY SPARINGLY SOLUBLE IN WATER

GAMMA AMINOBUTYRIC ACID (GABA) UPTAKE CARRIER

PDB 7Y7Z (CRYO-EM STRUCTURE OF HUMAN GABA TRANSPORTER GAT1 BOUND WITH TIAGABINE IN NACL SOLUTION IN AN INWARD-OPEN STATE AT 3.2 ANGSTROM)

LIGAND CODE = TGI (link to the list of PDB complexes)

Download experimental 3D coordinates of TGI with added hydrogens

Sodium- and chloride-dependent GABA transporter 1 UNIPROT P30531 SLC6A1

more at DrugCentral

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ANSM (in French)

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