Table 3.
[3H]epibatidine binding |
||||
---|---|---|---|---|
compd | α3β4 Ki (nM) | α4β2 Ki (nM) |
selectivity (fold) (α3β4 Ki/α4β2 Ki) |
α4β2 antagonist potency IC50 (nM) |
207 | 61750 ± 36030 | 1587 ± 301 | 39 | 26320 ± 980 |
208 | 88895 ± 18005 | 3731 ± 237 | 24 | 5319 ± 346 |
301 | 56480 ± 8920 | 118 ± 2 | 478 | 514 ± 84 |
302 | 23765 ± 5345 | 323 ± 152 | 74 | 1465 ± 43 |
303 | 27550 ± 7150 | 433 ± 79 | 64 | 2820 ± 82 |
304 | 63320 ± 3560 | 307 ± 78 | 206 | 3024 ± 125 |
305 | 51893 ± 27353 | 2217 ± 1194 | 23 | 2953 ± 594 |
306 | 59678 ± 15253 | 340 ± 148 | 176 | 2830 ± 75 |
307 | 78085 ± 8355 | 611 ± 220 | 128 | 3405 ± 125 |
308 | 33353 ± 4373 | 257 ± 113 | 130 | 1686 ± 373 |
DHβE | >10000 | 485 ± 33 | >20 | 624 ± 24 |
Experiments were conducted a minimum of two times by methods described in Materials and Methods. Values shown are mean ± SEM for experiments conducted in triplicate at least twice.