Table 2.
Pharmacological profiles of ACh, nicotine and fifteen nicotine derivatives. Results (mean ± S.E.M.) were expressed as the EC50 (μM), Hill slope (nH) and maximum response (Imax, %), number of repeats of each agonist experiment (Nagonist). One oocyte was used in each replicate of experiment.
| No: | Compound name | EC50 (μM) | nH | Imax (%) | Nagonist |
|---|---|---|---|---|---|
| 1: | (S)-5-ethynyl-anabasine | 0.14 ± 0.01 | 1.81 ± 0.24 | 79.33 ± 3.75 | 5 |
| 2: | (S)-5- bromoanabasine | 0.32 ± 0.03 | 4.19 ± 1.58 | 80.69 ± 2.87 | 5 |
| 3: | (S)eSIB 1508Y | 0.37 ± 0.10 | 0.94 ± 0.04 | 100.1 ± 4.36 | 5 |
| 4: | 5-methylnicotine | 0.99 ± 0.17 | 2.09 ± 0.14 | 76.05 ± 1.22 | 5 |
| 5: | (S)-anabasine | 1.26 ± 0.19 | 2.26 ± 0.20 | 84.82 ± 4.20 | 5 |
| 6: | (S)-5-bromonicotine | 2.04 ± 0.12 | 2.46 ± 0.21 | 69.66 ± 3.28 | 5 |
| 7: | 6-methylnicotine | 6.13 ± 0.53 | 3.25 ± 0.24 | 69.74 ± 1.56 | 5 |
| 8: | (S)-nicotine | 6.21 ± 0.56 | 3.39 ± 0.36 | 82.39 ± 2.52 | 5 |
| 9: | ACh | 6.36 ± 0.49 | 2.93 ± 0.13 | 97.42 ± 0.93 | 5 |
| 10: | (S)-1’- methylnicotinium | 10.25 ± 0.62 | 3.52 ± 0.26 | 93.38 ± 5.25 | 5 |
| 11: | (S)-nicotine-5-carboxaldehyde | 11.51 ± 0.63 | 8.61 ± 4.04 | 62.20 ± 6.80 | 5 |
| 12: | 6-AN | 12.18 ± 0.29 | 10.10 ± 0.15 | 6.29 ± 0.62 | 5 |
| 13: | homonicotine | 16.62 ± 1.44 | 6.78 ± 2.50 | 22.01 ± 1.39 | 5 |
| 14: | nornicotine | 25.73 ± 4.71 | 3.25 ± 0.49 | 62.64 ± 3.42 | 5 |
| 15: | N-methyl anabasine | <100 | |||
| 16: | (S)-1- methylnicotinium | <100 | |||
| 17: | (S)-cotinine | <100 |