Ki (pKi ± S.E.M.) | |||||
---|---|---|---|---|---|
Compound | α2β2 | α4β2 | α2β4 | α3β4 | α4β4 |
nM | |||||
[3H]Epibatidine | |||||
KD (pM) | 21 ± 4.7 | 41 ± 6.7 | 90 ± 8.7 | 360 ± 35 | 101 ± 7.8 |
Bmax (pmol/mg) | 0.43 ± 0.04 | 1.4 ± 0.12 | 1.4 ± 0.23 | 7.9 ± 0.35 | 0.91 ± 0.12 |
ACh | 4.2 (8.38 ± 0.05) | 33 (7.48 ± 0.11) | 110 (6.97 ± 0.05) | 620 (6.21 ± 0.08) | 58 (7.23 ± 0.12) |
(S)-Nicotine | 3.6 (8.44 ± 0.07) | 8.3 (8.08 ± 0.12) | 83 (7.08 ± 0.01) | 290 (6.54 ± 0.05) | 74 (7.13 ± 0.11) |
(−)-Cytisine | 0.54 (9.26 ± 0.07) | 1.3 (8.89 ± 0.24) | 4.6 (8.34 ± 0.01) | 130 (6.87 ± 0.03) | 6.8 (8.17 ± 0.36) |
(±)-Epibatidine | 0.023 (10.64 ± 0.08) | 0.046 (10.34 ± 0.14) | 0.091 (10.04 ± 0.12) | 0.46 (9.34 ± 0.11) | 0.072 (10.01 ± 0.14) |
Lobeline | 1.6 (8.79 ± 0.05) | 2.2 (8.65 ± 0.22) | 280 (6.56 ± 0.13) | 480 (6.32 ± 0.13) | 120 (6.94 ± 0.21) |
MCC | 24 (7.62 ± 0.09) | 28 (7.55 ± 0.19) | 310 (6.51 ± 0.09) | 2,700 (5.57 ± 0.10) | 620 (6.21 ± 0.06) |
7 | 9.2 (8.04 ± 0.12) | 17 (7.77 ± 0.04) | 100 (6.99 ± 0.02) | 370 (6.43 ± 0.04) | 66 (7.18 ± 0.09) |
13 | 3.6 (8.44 ± 0.08) | 13 (7.89 ± 0.21) | 530 (6.28 ± 0.07) | 10,000 (4.98 ± 0.07) | 2,600 (5.58 ± 0.08) |
14 | 4.2 (8.38 ± 0.09) | 5.6 (8.25 ± 0.02) | 21 (7.68 ± 0.06) | 62 (7.21 ± 0.06) | 13 (7.90 ± 0.08) |
15 | 8.2 (8.09 ± 0.09) | 12 (7.91 ± 0.09) | 23 (7.63 ± 0.03) | 140 (6.85 ± 0.04) | 31 (7.51 ± 0.01) |
16 | 35 (7.46 ± 0.09) | 62 (7.21 ± 0.06) | 300 (6.53 ± 0.12) | 5,000 (5.30 ± 0.03) | 1,800 (5.74 ± 0.01) |
17 | 2,900 (5.53 ± 0.08) | 1,513 (5.82 ± 0.18) | 7,200 (5.14 ± 0.09) | 86,000 (4.06 ± 0.05) | 2,000 (5.71 ± 0.11) |
18 | 35,000 (4.45 ± 0.11) | 52,000 (4.28 ± 0.13) | 54,000 (4.26 ± 0.10) | 81,000 (4.09 ± 0.08) | 42,000 (4.37 ± 0.05) |
19 | 61 (7.21 ± 0.14) | 130 (6.90 ± 0.05) | 1,200 (5.89 ± 0.03) | 19,000 (4.71 ± 0.07) | 3,300 (5.49 ± 0.01) |
20 | 43 (7.37 ± 0.03) | 130 (6.90 ± 0.08) | 260 (6.58 ± 0.06) | 1,500 (5.81 ± 0.06) | 240 (6.63 ± 0.06) |
21 | 56 (7.25 ± 0.08) | 140 (6.85 ± 0.18) | 210 (6.68 ± 0.04) | 1,900 (5.72 ± 0.06) | 340 (6.47 ± 0.11) |