Table 1.
IC50 Values for PMP inhibition of KARs
| Receptor | IC50 mean (µm) (SD) | Confidence interval (µm) | p Value |
|---|---|---|---|
| GluK1 | 19 ± 5.3 | 13–33 | |
| GluK2 | 26 ± 9.8 | 17–56 | |
| GluK3 | 41 ± 5.7 | 34–56 | |
| GluK1/GluK5 | 2.8 ± 0.32 | 2.2–3.5 | <0.0001a |
| GluK2/GluK5 | 0.85 ± 0.09 | 0.69–1.0 | <0.0001a |
| GluK3/GluK5 | 14 ± 7.5 | 7.3–37 | 0.03a |
| GluK1/Neto1 | 11 ± 4.1 | 6.9–23 | 0.13a |
| GluK1/Neto2 | 19 ± 4.3 | 13–29 | 0.94a |
| GluK2/Neto1 | 5.4 ± 0.94 | 3.9–7.6 | <0.0001a |
| GluK2/Neto2 | 5.8 ± 0.84 | 4.4–7.7 | <0.0001a |
| GluK1/GluK5/Neto2 | 0.99 ± 0.15 | 0.73–1.3 | <0.0001b |
| GluK2/GluK5/Neto1 | 0.69 ± 0.16 | 0.45–1.1 | 0.001b |
| GluK2(N557D) | 2.8 ± 0.32 | 2.2–3.5 | <0.0001c |
| GluK2(N557D)/GluK5 | 1.1 ± 0.28 | 0.72–1.8 | 0.19c |
| GluK2/GluK5(D540N) | 3.0 ± 0.43 | 2.3–4.0 | <0.0001c |
| GluA4(i) | 0.56 ± 0.12 | 0.36–0.85 | 0.51d |
| DRG neurons | 11 ± 1.0 | 9.4–13 | |
| Mossy fiber EPSCKAR | 2.9 ± 0.76 | 1.9–4.9 |
Statistical comparisons between IC50 values derived from best fits to the inhibition-response data were made pairwise using the extra sum-of-squares F test.
aHeteromeric receptors compared against their homomeric counterparts.
bNeto-containing heteromeric receptors compared against their Neto-less counterparts.
cMutant receptors compared against their wild-type counterparts.
dGluA4(i) AMPA receptors compared against GluK2/GluK5/Neto1 KARs.