Tiagabine
Tiagabine
MW:
375.55
logP:
3.417
H-acceptors:
3
H-donors:
1
Rotatable bonds:
6
IUPAC: 1-[4,4-bis[(3-methyl-2-thienyl)]but-3-enyl]piperidine-3-carboxylic acid
Synonyms:
TIAGABINE, 115103543, 115103-54-3, Tiagabine [INN], Tiagabina [INN-Spanish], Tiagabinum [INN-Latin], (-)-(R)-1-(4,4-Bis(3-methyl-2-thienyl)-3-butenyl)nipecotic acid, 3-Piperidinecarboxylic acid, 1-(4,4-bis(3-methyl-2-thienyl)-3-butenyl)-, (R)-

Reference GATs GAT1 GAT2 GAT3 GAT4 Method Brain region Comment
Borden, 1996    0.67  1670  1410  2040 Radioactive labelling  
White et al., 2002  0.36         Radioactive labelling cultured neurons 
White et al., 2002  0.18         Radioactive labelling cultured astrocytes 
White et al., 2002    0.8  300  >300  800 Radioactive labelling  

GATs or EAATs means measurements on brain homogenates, slices, cultured neurons or astrocytes, i.e. not cloned transporters.

IC50 and Ki values are given in µM.

Ki values are indicated as italic.

Compounds affecting transport indirectly are shown in red.