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L-Serine O-sulfate
MW:
185.157
logP:
-3.77
H-acceptors:
7
H-donors:
3
Rotatable bonds:
4
EAATs:
 
EAAT1:
107 µM
EAAT2:
1157 µM
EAAT3:
150 µM
EAAT4:
 
EAAT5:
 
3-Hydroxyaspartic acid
MW:
149.102
logP:
-4.061
H-acceptors:
6
H-donors:
4
Rotatable bonds:
3
EAATs:
 
EAAT1:
32 µM
EAAT2:
19 µM
EAAT3:
25 µM
EAAT4:
 
EAAT5:
 
dichloromercury
MW:
271.495
logP:
0
H-acceptors:
0
H-donors:
0
Rotatable bonds:
0
EAATs:
 
EAAT1:
31 µM
EAAT2:
99 µM
EAAT3:
62 µM
EAAT4:
 
EAAT5:
 
t-PDC
MW:
159.14
logP:
-0.985
H-acceptors:
5
H-donors:
3
Rotatable bonds:
2
EAATs:
4 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
t-PDC
MW:
159.14
logP:
-0.985
H-acceptors:
5
H-donors:
3
Rotatable bonds:
2
EAATs:
 
EAAT1:
79 µM
EAAT2:
8 µM
EAAT3:
61 µM
EAAT4:
 
EAAT5:
 
Dihydrokainate
MW:
215.246
logP:
0.293
H-acceptors:
5
H-donors:
3
Rotatable bonds:
4
EAATs:
 
EAAT1:
>3000 µM
EAAT2:
23 µM
EAAT3:
>3000 µM
EAAT4:
 
EAAT5:
 
t-PDC
MW:
159.14
logP:
-0.985
H-acceptors:
5
H-donors:
3
Rotatable bonds:
2
EAATs:
 
EAAT1:
 
EAAT2:
 
EAAT3:
74 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Electrophysiology
Substrate: no
Comment: They used Xenopus Oocytes for the expression of the human EAAT3 gene. The affinity of the transporter was highly dependent on membrane potential.
3-Hydroxyasprtic acid
MW:
149.102
logP:
-4.061
H-acceptors:
6
H-donors:
4
Rotatable bonds:
3
EAATs:
 
EAAT1:
 
EAAT2:
 
EAAT3:
28 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Electrophysiology
Substrate: n/a
Comment: They used Xenopus Oocytes for the expression of the human EAAT3 gene. The affinity of the transporter was highly dependent on membrane potential.
acetic acid [4-azido-6-[(5-methyl-2,4-dioxo-1H-pyrimidin-1-yl)]tetrahydropyran-2-yl]methyl ester
MW:
323.305
logP:
-2.33
H-acceptors:
7
H-donors:
1
Rotatable bonds:
5
EAATs:
 
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
4.4 µM
EAAT5:
3.2 µM
Cell line:
Method: Electrophysiology
Substrate: no
Comment: DL-TBOA is a non-transportable blocker. It does not affect the leak currents of EAAT4. The leak currents of EAAT5 are blocked though by the application of DL-TBOA. It does not interfere with metabotropic and ionotropic glutamate receptors, and IC50 valueus for EAAT1-3 were between 7 and 48 micromoles.
Dihydrokainate
MW:
215.246
logP:
0.293
H-acceptors:
5
H-donors:
3
Rotatable bonds:
4
EAATs:
28 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
Brain region: rat forebrain
Method: Radioactive labelling
Substrate: no
Comment: The radioactive substrate was 3H-aspartate.
The synaptosomal preparation used exhibited the greatest correspondance with EAAT2.