Summary of second-order rate constants for reaction of MTS compounds with receptors containing γ2D75C, γ2A79C, or γ2T81C in the absence (control) or presence of BZD ligands
| Receptor | Reagent | Control | FLZM | Ro 15–1788 | GABA | ||||
|---|---|---|---|---|---|---|---|---|---|
| k2(m−1s−1) | n | k2(m−1s−1) | n | k2(m−1s−1) | n | k2(m−1s−1) | n | ||
| αβγD75C | MTSEA | 420 ± 200 | 3 | 530 ± 210 | 3 | 510 ± 250 | 3 | 580 ± 70 | 3 |
| αβγA79C | MTSEA-biotin | 1300 ± 200 | 5 | 670 ± 250* | 3 | 600 ± 1002-160 | 3 | 3700 ± 3002-160 | 3 |
| αβγT81C | MTSEA-biotin-CAP | 17,000 ± 4400 | 3 | 12,000 ± 1700 | 3 | 3700 ± 8002-160 | 3 | 22,000 ± 2300 | 3 |
Second-order rate constants (k2) were derived by dividing the fit pseudo-first-order rate constants by the concentration of MTS reagent used (see Materials and Methods). The concentration of MTS compounds used was as follows (in μm): MTSEA, 200; MTSEA-biotin, 200; MTSEA-biotin-CAP, 20. Data represent mean ± SD values.
↵* ,
↵F2-160 Indicate values significantly different from control (MTS alone), with p < 0.05 andp < 0.01, respectively.