Table 1

Ki values and exchange rates for transport inhibitors

CompoundKiConcentrationExchange rate (pmol/mg protein/ 2 min)
μM
l-Glutamate4.9  ± 1100362  ± 12
50344  ± 16
10316  ± 22
2,4-MPDC6.8  ± 3100282  ± 28
75280  ± 30
l-Aspartate1.7  ± 0.6100278  ± 16
20266  ± 22
cis-ACBD30  ± 2100266  ± 4
300270  ± 8
l-cis-2,4-PDC66  ± 6100206  ± 16
500260  ± 22
l-trans-2,4-PDC1.5  ± 0.5100250  ± 28
15208  ± 28
l-β-THA2.0  ± 1100172  ± 24
20162  ± 16
l-trans-2,3-ADC78  ± 6100146  ± 14
800156  ± 26
l-anti-endo-3,4-MPDC4.9  ± 2100120  ± 20
50120  ± 18
Kainate59  ± 61000  ± 1.5
6000  ± 0
cis-5-Me-l-trans-2,3-PDC37  ± 61003  ± 6
3500  ± 0
DHK28  ± 21000  ± 3
30011.4  ± 6
DHK+30060  ± 12
l-Glutamate10
l-trans-2,3-PDC33  ± 61003  ± 6
30019  ± 6
l-trans-2,3-PDC +l-Glutamate300 1076  ± 16

K i values ± S.D. reported in this table represent the average of at least three separate Lineweaver-Burk analyses that were carried out as described in Figure 2. The synaptosomal efflux of d-[3H]aspartate induced by the inhibitors was quantified over a 2-min period at 37°C and was corrected for the efflux that occurred in the absence of added compound (228 ± 8 pmol/mg protein/2 min). Inhibitors were tested both at 100 μM and, to ensure comparable levels of transporter binding, at concentrations approximately 10 times greater than theK i values for which they inhibitedd-[3H]aspartate uptake. Values represent mean ± S.E. from at least four separate determinations conducted in duplicate.