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Dihydrokainate
MW:
215.246
logP:
0.293
H-acceptors:
5
H-donors:
3
Rotatable bonds:
4
EAATs:
 
EAAT1:
 
EAAT2:
9.2 µM
EAAT3:
 
EAAT4:
 
EAAT5:
 
L-anti-endo-MPDC
MW:
171.15
logP:
-1.35
H-acceptors:
4
H-donors:
3
Rotatable bonds:
2
EAATs:
 
EAAT1:
 
EAAT2:
1.6 µM
EAAT3:
 
EAAT4:
 
EAAT5:
 
(2R,3S)-2-amino-3-methylpentanedioic acid
MW:
161.16
logP:
-1
H-acceptors:
5
H-donors:
3
Rotatable bonds:
4
EAATs:
 
EAAT1:
 
EAAT2:
18.3 µM
EAAT3:
 
EAAT4:
 
EAAT5:
 
Cell line:
Method: Electrophysiology
Substrate: no
Comment: T3MG had no effect on EAAT1, as such it displays similar properties to those of kainate and dihydrokainate.
DL-TBzOAsp
MW:
253.21
logP:
-0.2
H-acceptors:
5
H-donors:
3
Rotatable bonds:
3
EAATs:
 
EAAT1:
286 µM
EAAT2:
126 µM
EAAT3:
 
EAAT4:
 
EAAT5:
 
DL-TBOA
MW:
239.08
logP:
-0.24
H-acceptors:
4
H-donors:
3
Rotatable bonds:
3
EAATs:
 
EAAT1:
42 µM
EAAT2:
5.7 µM
EAAT3:
6 µM
EAAT4:
 
EAAT5:
 
L-TNOA1
MW:
291.3
logP:
-0.67
H-acceptors:
4
H-donors:
3
Rotatable bonds:
3
EAATs:
 
EAAT1:
15 µM
EAAT2:
1.3 µM
EAAT3:
4.8 µM
EAAT4:
 
EAAT5:
 
Cell line: cloned transporters expressed in COS1
Method: Radioactive labelling
Substrate: no
Comment: It acts as a blocker on all three transporter types.
DL-TBOA
MW:
239.08
logP:
-0.24
H-acceptors:
4
H-donors:
3
Rotatable bonds:
3
EAATs:
 
EAAT1:
48 µM
EAAT2:
7 µM
EAAT3:
8 µM
EAAT4:
 
EAAT5:
 
L-TMOA
MW:
163.13
logP:
-1.97
H-acceptors:
4
H-donors:
3
Rotatable bonds:
2
EAATs:
 
EAAT1:
69 µM
EAAT2:
2 µM
EAAT3:
8.4 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: yes
Comment: L-TMOA proved to be a substrate for EAAT1 and EAAT3, while it was a blocker for EAAT2.
L-TMOA
MW:
163.13
logP:
-1.97
H-acceptors:
4
H-donors:
3
Rotatable bonds:
2
EAATs:
 
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
1.2 µM
EAAT5:
1 µM
Cell line:
Method: Electrophysiology
Substrate: yes
Comment: On EAAT4 it acts as competitive substrate,
on EAAT5 it is non-transportable blocker, that blocks leak currents.
DL-TBOA
MW:
239.08
logP:
-0.24
H-acceptors:
4
H-donors:
3
Rotatable bonds:
3
EAATs:
 
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
4.4 µM
EAAT5:
3.2 µM
Cell line:
Method: Electrophysiology
Substrate: no
Comment: DL-TBOA is the only non-transportable blocker for EAAT4 that does not affect the leak current