General
Preferred name
tiagabine
Synonyms
TIAGABINE HYDROCHLORIDE ()
TGB hydrochloride hydrate ()
Tiagabine hydrochloride hydrate ()
NO050328 hydrochloride hydrate ()
NO328 hydrochloride hydrate ()
Gabitril hydrochloride ()
NO328 hydrochloride ()
NO050328 hydrochloride ()
TGB hydrochloride ()
TGB ()
NO050328 ()
Gabitril ()
NO328 ()
Tiagabine HCl ()
TIAGABINE HCl ()
Tiagabine (hydrochloride) ()
Gabitril hydrochloride, NO050328 hydrochloride, NO328 hydrochloride, TGB hydrochloride ()
Abbott-70569.1 ()
NO-050328 ()
Gabatril ()
ABBOTT-70569.HCl ()
NNC-05-0328 ()
ABBOTT-705691 ()
NO-05-0328 ()
ABT-569 ()
NNC-050328 ()
ABBOTT-70569 HYDROCHLORIDE ()
NNC-050328 FREE BASE ()
ABBOTT-705691 FREE BASE ()
ABT-569 FREE BASE ()
ABBOTT-70569-1 ()
ABBOTT-70569 FREE BASE ()
Tiagabina ()
A-70569-1 ()
NO-050328 FREE BASE ()
ABBOTT-70569.HCL ()
GABATRIL ()
Tiagabine-d6 (hydrochloride) ()
P&D ID
PD009653
CAS
145821-59-6
115103-54-3
1006863-69-9
1217808-68-8
Tags
available
drug
Approved by
FDA
First approval
1997
Drug indication
Anxiety disorder
Anxiety
Epilepsy
Drug Status
approved
investigational
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Tiagabine hydrochloride is an anticonvulsant agent and a selective inhibitor of the GAT-1 GABA transporter with a Ki of ¡«0.1 ¦ÌM. Tiagabine hydrochloride potently and selectively inhibits GABA reuptake with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in synaptosomes, neurons and glia, respectively. Tiagabine hydrochloride has neuroprotective properties[1][2][3][4][5][6][7][8].
PRICE 41
DESCRIPTION Tiagabine is classified as a GABA reuptake inhibitor (GRI) as it blocks the GABA transporter 1 (GAT-1; gene symbol SLC6A1). (GtoPdb)
PRICE 43
DESCRIPTION Phosphate reservoir (Tocris Bioactive Compound Library)
DESCRIPTION GABA uptake inhibitor; anticonvulsant (Tocriscreen Plus)
DESCRIPTION Tiagabine HCl is an inhibitor of GABA transporter 1. Tiagabine HCl is used as adjunctive therapies in the treatment of partial seizures. (Enamine Bioactive Compounds)
DESCRIPTION Tiagabine hydrochloride (NO050328 hydrochloride) is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor. (TargetMol Bioactive Compound Library)
DESCRIPTION Tiagabine is a selective gamma-aminobutyric acid (GABA) reuptake inhibitor. (BOC Sciences Bioactive Compounds)
DESCRIPTION Tiagabine (NO050328) is an Anti-epileptic Agent. The physiologic effect of tiagabine is by means of Decreased Central Nervous System Disorganized Electrical Activity. (TargetMol Bioactive Compound Library)
Compound Sets
37
AdooQ Bioactive Compound Library
A13198
BOC Sciences Bioactive Compounds
tiagabine-cas-115103-54-3-item-84-55023
Cayman Chemical Bioactives
22926
30766
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
CHEMBL1695
CHEMBL1027
ChEMBL Drugs
CHEMBL1695
CHEMBL1027
Concise Guide to Pharmacology 2017/18
4685
4818
Concise Guide to Pharmacology 2019/20
4685
4818
Concise Guide to Pharmacology 2021/22
4685
4818
Concise Guide to Pharmacology 2023/24
4685
4818
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB00906
DrugBank Approved Drugs
DB00906
DrugCentral
2648
DrugCentral Approved Drugs
2648
DrugMAP
DMKSQG0
DrugMAP Approved Drugs
DMKSQG0
Enamine Bioactive Compounds
EBC-08666
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EOS101241
EUbOPEN Chemogenomics Library
EUB0002743
Guide to Pharmacology
4685
4818
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1695
CHEMBL1027
Mcule NIBR MoA Box Subset
MCULE-2541016450
MedChem Express Bioactive Compound Library
HY-B0696A
NCATS Inxight Approved Drugs
Z80I64HMNP
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Other bioactive compounds
ReFrame library
Selleckchem Bioactive Compound Library
tiagabine-hydrochloride
TargetMol Bioactive Compound Library
T7000
T2407
Tocris Bioactive Compound Library
4256
Tocriscreen Plus
4256
ZINC Tool Compounds
ZINC000003831531
External IDs
72
Properties
(calculated by RDKit )
Molecular Weight
375.13
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
6
Ring Count
3
Aromatic Ring Count
2
cLogP
5.04
TPSA
40.54
Fraction CSP3
0.45
Chiral centers
1.0
Largest ring
6.0
QED
0.77
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Transporters
Target
GABA Receptor
GABA transporter 1
GABA uptake
GABA
SLC6A1
Trk Receptor
Pathway
Neuronal Signaling
Membrane Transporter/Ion Channel
Neuroscience
Protein Tyrosine Kinase/RTK
MOA
sodium- and chloride-dependent GABA transporter inhibitor
Inhibitor
GAT-1 Inhibitors
GABA uptake inhibitor
Primary Target
GABA Transporters
Member status
member
Indication
seizures
Therapeutic Class
Anticonvulsants
Recommended Cell Concentration
None
Source data