. | Ki (μmol 1-1) . | . | . | . | . | ||||
---|---|---|---|---|---|---|---|---|---|
Inhibitor . | AeaEAT . | TrnEAT1 . | EAAT12 . | EAAT22 . | EAAT32 . | ||||
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) . | . | . | . | . | ||||
---|---|---|---|---|---|---|---|---|---|
Inhibitor . | AeaEAT . | TrnEAT1 . | EAAT12 . | EAAT22 . | EAAT32 . | ||||
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).
Donly et al. (1997).
Arriza et al. (1994).
Shimamoto et al. (1998).