Table 1

Differentiation of substrate and nonsubstrate transport inhibitors by heteroexchange

Experiment[3H]d-Aspartate Efflux[3H]GABA Efflux
% of control % of control
Control100  ± 4100  ± 8
l-Glutamate, 10 μM233  ± 101-a 100  ± 6
GABA, 50 μM102  ± 11252  ± 18c
Kainate, 100 μM81  ± 6104  ± 8
AMPA, 100 μM97  ± 699  ± 7
NMDA, 100 μM91  ± 399  ± 7
trans-ACPD, 100 μM100  ± 1099  ± 7
β-d,l-THA, 20 μM167  ± 81-a 102  ± 5
l-trans-2,4-PDC, 15 μM186  ± 171-a 96  ± 4
l-trans-2,3-PDC, 300 μM96  ± 595  ± 6
DHK, 300 μM94  ± 6101  ± 2
l-Glutamate, 10 μM andl-trans-2,3-PDC, 300 μM129  ± 7b N.D.
l-Glutamate, 10 μM and DHK, 300 μM129  ± 8b N.D.
GABA, 50 μM and l-trans-2,3-PDC, 300 μMN.D.248  ± 28c
GABA, 50 μM and DHK, 300 μMN.D.252  ± 20c

Efflux of radiolabeled substrate from synaptosomes containing either [3H]d-ASP or [3H]GABA was determined as described in Materials and Methods and is expressed as percentage of control (i.e., efflux over a 2-min interval at 37°C in the absence of uptake inhibitors). Initial content of synaptosomes was 1552 ± 62 pmol [3H]d-ASP/mg protein or 3887 ± 263 pmol [3H]GABA/mg protein. Control efflux rates were 114 ± 4 pmol/min/mg protein for [3H]d-ASP and 354 ± 30 pmol/min/mg for [3H]GABA. Values are reported as mean ± S.E.M.,n = 4-57 duplicate determinations. Statistical comparisons were made using an Alternate Welch t test (InStat).

    • 1-a p < .0005 versus [3H]d-ASP control; bp< .0001 versus glutamate-mediated [3H]d-ASP efflux; cp < .001 versus [3H]GABA control. N.D., not determined.