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1-hydroxy-1,2,3-triazole
MW:
174.16
logP:
666
H-acceptors:
3
H-donors:
4
Rotatable bonds:
3
EAATs:
 
EAAT1:
100 µM
EAAT2:
300 µM
EAAT3:
1000 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: n/a
Comment: The radiactive ligand was 3H-R-aspartic acid.
The compound was found to be inactive at metabotropic receptors, but was a strong agonist for the AMPA and KA ionotropic gluatamate receptors.
This group carried out measurements on native synaptosomal preparation aswell.
1-hydroxy-1,2,3-triazole
MW:
174.16
logP:
666
H-acceptors:
3
H-donors:
4
Rotatable bonds:
3
EAATs:
93 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
Brain region: cortex
Method: Radioactive labelling
Substrate: n/a
Comment: The radiactive ligand was 3H-R-aspartic acid.
The compound was found to be inactive at metabotropic receptors, but was a strong agonist for the AMPA and KA ionotropic gluatamate receptors.
This group carried out measurements on cloned transporters aswell.
S-TPDA
MW:
189.19
logP:
0.51
H-acceptors:
6
H-donors:
3
Rotatable bonds:
2
EAATs:
 
EAAT1:
3000 µM
EAAT2:
4 µM
EAAT3:
3000 µM
EAAT4:
 
EAAT5:
 
2-amino-3-sulfooxy-propanoic acid
MW:
185.16
logP:
-3.77
H-acceptors:
7
H-donors:
3
Rotatable bonds:
4
EAATs:
17 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
2-amino-4-methyl-pentanedioic acid
MW:
161.156
logP:
-2.95
H-acceptors:
5
H-donors:
3
Rotatable bonds:
4
EAATs:
7 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
L-anti-endo-MPDC
MW:
171.15
logP:
-1.35
H-acceptors:
4
H-donors:
3
Rotatable bonds:
2
EAATs:
87.5 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
Brain region: cortex
Method: Radioactive labelling
Substrate: yes
Comment: The measurements were done on cortical astrocytical slice cultures.
The radioactive ligand was L-14C-glutamate.
t-PDC
MW:
159.14
logP:
-0.985
H-acceptors:
5
H-donors:
3
Rotatable bonds:
2
EAATs:
74.1 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
Brain region: cortex
Method: Radioactive labelling
Substrate: yes
Comment: The measurements were done on cortical astrocytical slice cultures.
The radioactive ligand was L-14C-glutamate.
DL-TBOA
MW:
239.08
logP:
-0.24
H-acceptors:
4
H-donors:
3
Rotatable bonds:
3
EAATs:
40.6 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
Brain region: cortex
Method: Radioactive labelling
Substrate: yes
Comment: DL-TBOA proved to be a substrate only in astrocyte cultures.
The radioactive ligand was L-14C-glutamate.
cis-ABDA
MW:
159.14
logP:
-3.356
H-acceptors:
5
H-donors:
3
Rotatable bonds:
2
EAATs:
53 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
N-DPB-N-methyl-exo-THPO
MW:
374.48
logP:
5.09
H-acceptors:
2
H-donors:
1
Rotatable bonds:
6
GATs:
 
GAT1:
2 µM
GAT2:
200 µM
GAT3:
>100 µM
GAT4:
>100 µM