NCI | Ki | Slope | |
---|---|---|---|
Desensitized | Resting | ||
μM | |||
Quinacrine | 5.8 | 1.18 ± 0.51 | |
Ethidium | 119 | 0.54 ± 0.20 | |
Crystal violet | 11.9 | 0.56 ± 0.50 | |
284 | 2.93 ± 1.20 | ||
[125I]TID | 197 ± 25 | 1.19 ± 0.14 | |
[3H]TCP | 7.0 ± 0.8 | 0.93 ± 0.08 | |
[3H]Dizocilpine | 3.3 ± 0.2 | 0.93 ± 0.04 | |
125I-Dizocilpine | 18.4 ± 1.5 | 0.50 ± 0.02 | |
[3H]Dizocilpine | 8.7 ± 1.2 | 0.62 ± 0.05 | |
[3H]TCP | 3.1 ± 0.2 | 0.88 ± 0.05 |
K i values for dizocilpine using quinacrine, ethidium, and CrV displacement binding were obtained from the Schild plots shown in part B of Figs. 3-6, according to eq. 1. The other K i values for dizocilpine were calculated using the Cheng-Prusoff relationship (eq. 2) and the IC50values obtained from Fig. 2 ([3H]TCP) and from data not shown for [125I]TID and [3H]dizocilpine.K i values for TMB-8 were also calculated using the Cheng-Prusoff relationship (eq. 2) and the IC50 values obtained from Fig. 7A ([3H] and 125I-dizocilpine) and from data not shown for [3H]TCP. The slope values for quinacrine, ethidium, and crystal violet are from the Schild plots shown in part B of Figs. 3-6 , respectively. The remaining slope values, obtained from the slopes of the competition experiments shown in Fig. 2([3H]TCP), Fig. 7A (TMB-8), and for data not shown, are the Hill coefficients (n H).