Receptor | Accessible Surface Area | Ro 40-6129 | Ro 41-0639 | Ro 41-3380 | ||||||
---|---|---|---|---|---|---|---|---|---|---|
KI | n | KI-mut/ KI-α β γ | KI | n | KI-mut/ KI-α β γ | KI | n | KI-mut/ KI-α β γ | ||
nM | nM | nM | ||||||||
αβγ | 115, 1402-a | 2.6 ± 0.7 | 3 | 1.0 | 0.4 ± 0.2 | 3 | 1.0 | 1.9 ± 0.2 | 4 | 1.0 |
αβγ A79C | 135 | 8.6 ± 1.12-160 | 3 | 3.3 | 2.5 ± 0.42-160 | 4 | 6.3 | 18 ± 62-160 | 5 | 9.5 |
αβγ A79L | 170 | 7.3 ± 1.52-160 | 3 | 2.8 | 1.1 ± 0.4 | 3 | 2.8 | 328 ± 872-160 | 3 | 173 |
αβγ A79E | 190 | 3.5 ± 0.6 | 3 | 1.3 | 1.9 ± 0.32-160 | 3 | 4.8 | 119 ± 202-160 | 3 | 63 |
αβγ A79R | 225 | 4.3 ± 1 | 3 | 1.7 | 1.2 ± 0.2 | 3 | 3.0 | 501 ± 2032-160 | 5 | 264 |
αβγ A79Y | 230 | 27 ± 22-160 | 3 | 10 | 7.6 ± 3.42-160 | 3 | 19 | 192 ± 22-160 | 3 | 101 |
αβγ T81C | 135 | 19 ± 42-160 | 3 | 7.3 | 1.2 ± 0.3* | 4 | 3.0 | 16 ± 32-160 | 5 | 8.4 |
KI values were determined by displacement of [3H]flunitrazepam binding. Mutations at γ2A79 are arranged in ascending order of accessible side-chain surface area (Å2; Chothia, 1976). Data represent mean ± S.E.M.