Browse
4-[2-[5-ethyl-5-[5-[6-hydroxy-6-(hydroxymethyl)-3,5-dimethyl-tetrahydropyra
MW:
670.871
logP:
5.009
H-acceptors:
11
H-donors:
4
Rotatable bonds:
10
EAATs:
1.3 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
Brain region: forebrain
Method: Radioactive labelling
Substrate: no
Comment: The compound inhibits GABA and Glu uptake by affecting the Na+ gradient of the neuronal membrane (Na+ ionophore).
The synaptosomal uptake system used in the experiments can be most closely associated with GAT1 and EAAT3.
ethyl 3-hydroxy-1,6-dimethyl-5-phenyl-1,6-dihydropiridine-2-carboxylate
MW:
273.33
logP:
0.77
H-acceptors:
3
H-donors:
1
Rotatable bonds:
3
EAATs:
660 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
Z methyl 4-[(2-methoxy-2-oxoethyl)(methyl)amino]-3-phenylpent-2-enoate
MW:
291.15
logP:
1.67
H-acceptors:
3
H-donors:
0
Rotatable bonds:
5
EAATs:
1100 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
Z ethyl 4-[(ethoxycarbonylmethy)methylamino]-2-methyl-3-phenylpent-2-enoate
MW:
319.4
logP:
2.35
H-acceptors:
1
H-donors:
0
Rotatable bonds:
5
EAATs:
420 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
morpholine-6-carboxylic acid
MW:
131.13
logP:
-0.1
H-acceptors:
2
H-donors:
2
Rotatable bonds:
1
GATs:
300 µM
GAT1:
 
GAT2:
 
GAT3:
 
GAT4:
 
isoxazolidine-5-carboxylic acid
MW:
117.1
logP:
-0.52
H-acceptors:
2
H-donors:
2
Rotatable bonds:
1
GATs:
>300 µM
GAT1:
 
GAT2:
 
GAT3:
 
GAT4:
 
(RS)-3-OCH3-GABA
MW:
133.15
logP:
-1.27
H-acceptors:
2
H-donors:
2
Rotatable bonds:
4
GATs:
>300 µM
GAT1:
 
GAT2:
 
GAT3:
 
GAT4:
 
(S)-(+)-DHM
MW:
116.12
logP:
-0.68
H-acceptors:
3
H-donors:
2
Rotatable bonds:
1
GATs:
>300 µM
GAT1:
 
GAT2:
 
GAT3:
 
GAT4:
 
(R)-(-)-DHM
MW:
116.12
logP:
-0.68
H-acceptors:
3
H-donors:
2
Rotatable bonds:
1
GATs:
70 µM
GAT1:
 
GAT2:
 
GAT3:
 
GAT4:
 
(S)-(+)-3-OH-GABA
MW:
119.12
logP:
-1.63
H-acceptors:
2
H-donors:
3
Rotatable bonds:
3
GATs:
29 µM
GAT1:
 
GAT2:
 
GAT3:
 
GAT4: