Mutations were made in the lurcher region of NR2A to test whether this region also controls proton-sensitive gating. The position of mutations within the lurcher region were indexed to the lurcher site (assigned `0'). | |||
---|---|---|---|
Receptor | Δ Lurcher | IC50 | IC50(MUT)/IC50(WT) |
nM | |||
NR1/NR2A | 119 | 1.0 (n = 56) | |
M3-S2 Linker | |||
NR1/NR2A(T646C) | -5 | 356 | 3.0 (n = 17) |
NR1/NR2A(A647C) | -4 | 150 | 1.3 (n = 3) |
NR1/NR2A(N648S) | -3 | 68 | 0.6 (n = 8) |
NR1/NR2A(L649C) | -2 | 194 | 1.6 (n = 4) |
NR1/NR2A(A650C) | -1 | 96 | 0.8 (n = 11) |
NR1/NR2A(A651C) | 0 | 88 | 0.7 (n = 6) |
NR1/NR2A(A651T) | 0 | 571 | 4.8 (n = 50) |
NR 1/ NR2A(F652C) | +1 | 61 | 0.5 (n = 11) |
M4-S2 Linker | |||
NR1/NR2A(H801A) | 338 | 2.8 (n = 6) | |
NR1/NR2A(K804L) | 133 | 1.1 (n = 8) | |
NR1/NR2A(E803A, K804L,E806A) | 108 | 0.9 (n = 21) | |
NR1/NR2A(D813A) | 84 | 0.7 (n = 14) | |
NR1/NR2A(D813A,D815A) | 810 | 6.8 (n = 27) | |
Coexpressed NR1-NR2 Linker Mutants | |||
NR1(T648C)/NR2A(T646C) | -5,-5 | 2098 | 18 (n = 22) |
NR1(T648C)/NR2A(A651T) | -5, 0 | 2461 | 21 (n = 24) |
NR1(T648C)/NR2A(D813A,D815A) | -5 | 9566 | 81 (n = 31) |
NR1(A649C)/NR2A(T646C) | -4 -5 | 2793 | 24 (n = 24) |
NR1(A649C)/NR2A(A651T) | -4,0 | 17288 | 146 (n = 19) |
NR1(A649C)/NR2A(D813A,D815A) | -4 | 3166 | 27 (n = 20) |
NR1(A653T)/NR2A(T646C) | 0,-5 | 2033 | 17 (n = 11) |
NR1(A653T)/NR2A(A651T) | 0,0 | 3300 | 28 (n = 66) |
NR1(A653T)/NR2A(D813A,D815A) | 0 | 5000 | 42 (n = 31) |
MUT, mutant; WT, wild-type.