GluN1 | GluN2B | Relative MK-801 | Ifenprodil | EVT-101 | |||||||
---|---|---|---|---|---|---|---|---|---|---|---|
τon | n | IC50 | IC50 ratio (mutant/wt) | Max inhib | n | IC50 | IC50 ratio (mutant/wt) | Max inhib | n | ||
nM | nM | ||||||||||
wt | wt | 1.0 | (9) | 130 ± 4 | 1.0 | 0.95 ± 0.01 | (12) | 12 ± 0.2 | 1.0 | 0.9 ± 0.01 | (12) |
Y109C | wt | 1.1 | (3) | 856 ± 122 | 6.6 | 1.0* | (4) | 7300 ± 260 | 608 | 1.0* | (3) |
Y109S | wt | 0.7 | (3) | 224 ± 36 | 1.7 | 0.97 ± 0.07 | (4) | 9618 ± 700 | 800 | 1.0* | (3) |
I133A | wt | 2.9 | (5) | 80 ± 7 | 0.6 | 0.69 ± 0.02 | (3) | 52 ± 4 | 4.3 | 0.65 ± 0.01 | (4) |
I133C | wt | 0.6 | (4) | 1400 ± 104 | 11 | 1.0* | (4) | 62 ± 22 | 5.2 | 0.48 ± 0.03 | (3) |
I133W | wt | 2.6 | (6) | 32 ± 5 | 0.3 | 0.47 ± 0.02 | (5) | 32 ± 9 | 2.7 | 0.54 ± 0.03 | (3) |
L135A | wt | 5.4 | (7) | 101 ± 9 | 0.8 | 0.90 ± 0.03 | (5) | 25 ± 2 | 2.0 | 0.60 ± 0.01 | (8) |
L135H | wt | 6.0 | (4) | >10000 | >100 | 1.0* | (3) | 71 ± 7 | 5.9 | 0.48 ± 0.01 | (3) |
L135M | wt | 2.4 | (3) | 73 ± 2 | 0.6 | 0.86 ± 0.01 | (3) | n.d | n.d. | ||
L135R | wt | 3.5 | (3) | 300 ± 36 | 2.3 | 1.0* | (3) | 53 ± 6 | 4.4 | 0.69 ± 0.02 | (3) |
L135W | wt | 2.1 | (9) | 767 ± 78 | 5.9 | 1.0* | (5) | 9 ± 1 | 0.7 | 0.86 ± 0.02 | (6) |
wt | Q110G | 0.4 | (3) | 124 ± 3 | 1.0 | 0.99 ± 0.01 | (3) | 502 ± 14 | 42 | 0.97 ± 0.01 | (3) |
wt | F114S | 0.4 | (3) | >10000 | >100 | 1.0* | (4) | 676 ± 10 | 56 | 0.91 ± 0.01 | (3) |
wt | A135G | 3.0 | (3) | 50 ± 3 | 0.4 | 0.80 ± 0.01 | (4) | 72 ± 7 | 6.0 | 0.80 ± 0.02 | (3) |
wt | A135P | 2.1 | (4) | 587 ± 43 | 4.5 | 1.0* | (3) | 404 ± 15 | 34 | 0.78 ± 0.02 | (3) |
wt | F176A | 1.3 | (4) | 7500 ± 58 | 58 | 1.0* | (4) | 11400 ± 1000 | 950 | 1.0* | (3) |
wt | P177C | 2.7 | (8) | >10000 | >100 | 1.0* | (6) | 75 ± 12 | 6.2 | 0.64 ± 0.03 | (5) |
wt | E236C | 0.9 | (4) | 1800 ± 14 | 14 | 1.0* | (4) | 332 ± 2 | 28 | 0.87 ± 0.01 | (4) |
wt, wild type; n, number of cells; n.d., not determined.
↵* Indicates maximal inhibition fixed to 1. Errors are expressed as S.D.