TABLE 4.
LDK1229 binding to the wild-type or mutant CB1 receptors using [3H]CP55,940 or [3H]WIN55,212-2 as a tracer
| Receptor | [3H]CP55,940 | |
|---|---|---|
| Kia | Ki Ratiob | |
| nM | ||
| CB1 wild type | 220 (106–457) | 1:1 |
| K3.28192A | 1316 (1115–1626)c | 1:4c |
| W5.43279A | ND | — |
| W6.48356A | 1987 (895–2736) | 1:9 |
| C7.42386M | 1010 (832–1154) | 1:5 |
ND, not detectable; 39% displacement at 32 µM.
Data are the median and corresponding 95% confidence limits of three independent experiments performed in duplicate. Ki values were determined from competition binding assays using [3H]CP55,940 as tracer at its respective Kd values, as described in Results.
Wild type:mutant.
Binding was performed with [3H]WIN55,212-2 as a tracer. LDK1229 binding to CB1 wild type using [3H]WIN55,212-2 as a tracer yielded a Ki of 324 nM (205–524).