Table 2.

Inhibition of substrate transport

Ki (μmol 1-1)
InhibitorAeaEATTrnEAT1EAAT12EAAT22EAAT32
DL-TBOA 23.7±2.1  423 5.73 6 
tPDC 91±19 110±15.3 79±7 8±2 61±14 
TBHA 9.2±2.9 32.4±4.8 32±8 19±6 25±5 
SOS 29±5 88.9±21.8 107±8 1157±275 150±52 
CA 6.6±3.3 18.4±4.4 10±3 10±2 19±9 
CSA 7.1±3  14±7 6±1 17±2 
l-Cys 336     
lAβH 97.5±13.7 316±52 369±70 184±27 133±34 
α-AA 524±55     
β-Glu 651±20  297±118 156±37 307±48 
d-Glu 1060±70     
l-Asn 2670±210     
KA >3000  >3000 59±18 >3000 
NMDA >3000     
Ki (μmol 1-1)
InhibitorAeaEATTrnEAT1EAAT12EAAT22EAAT32
DL-TBOA 23.7±2.1  423 5.73 6 
tPDC 91±19 110±15.3 79±7 8±2 61±14 
TBHA 9.2±2.9 32.4±4.8 32±8 19±6 25±5 
SOS 29±5 88.9±21.8 107±8 1157±275 150±52 
CA 6.6±3.3 18.4±4.4 10±3 10±2 19±9 
CSA 7.1±3  14±7 6±1 17±2 
l-Cys 336     
lAβH 97.5±13.7 316±52 369±70 184±27 133±34 
α-AA 524±55     
β-Glu 651±20  297±118 156±37 307±48 
d-Glu 1060±70     
l-Asn 2670±210     
KA >3000  >3000 59±18 >3000 
NMDA >3000     

DL-TBOA, dl-threo-benzoxyaspartic acid; tPDC, trans-pyrrolidine dicarboxylic acid; TBHA, beta hydroxyaspartate;SOS, serine-o-sulfate; CA, cysteic acid; CSA, cysteine sulfinic acid; l-cys, l-cysteine; lAβH, l-aspartate-β-hydroxymate; α-AA, α-amino adipic acid; β-Glu, β-glutamate; d-Glu, d-glutamate; l-Asn, l-asparagine; KA, kainic acid; NMDA, N-methyl-d-aspartate.

AeaEAAT-expressing HeLa cells were exposed to 1 μmol 1-1 cold and 30 nmol 1-13H-labeled d-aspartate in the presence of logarithmically varying concentrations of known glutamate transport inhibitors. Transport was terminated after 5 min, and the Ki values determined from IC50 values as described previously (Cheng and Prusoff, 1973).

Values are compared to those published for TrnEAAT and hEAAT1-3 (see Table 1 for abbreviations).

1

Donly et al. (1997).

2

Arriza et al. (1994).

3

Shimamoto et al. (1998).

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