HS α4β2 nAChR | LS α4β2 nAChR | |||||
---|---|---|---|---|---|---|
EC50 (95% CI) | I/ImaxACh | nH | EC50 (95% CI) | I/ImaxACh | nH | |
μM | ||||||
Ach | 4 (3.6-5.7) | 1 ± 0.004 | 0.84 ± 0.02 | 88 (71-109) | 1.1 ± 0.005 | 0.94 ± 0.01 |
Nicotine | 1 (0.8-1.3) | 0.28 ± 0.01 | 0.78 ± 0.07 | 34 (23-50) | 0.62 ± 0.03 | 0.83 ± 0.07 |
Epibatidine | 0.02 (0.01-0.03) | 0.6 ± 0.02 | 0.86 ± 0.09 | 1.3 (0.4-4) | 2.2 ± 0.2 | 0.54 ± 0.1 |
TC-2559 | 2 (1-3) | 2.6 ± 0.2 | 0.76 ± 0.2 | 2.7 (1.2-6.1) | 0.22 ± 0.02 | 0.83 ± 0.2 |
A-85380 | 0.03 (0.02-0.04 | 1.3 ± 0.06 | 1 ± 0.1 | 3.3 (2-5) | 1.6 ± 0.06 | 0.58 ± 0.05 |
Cytisine | N.D. | N.E. | 12 (4-34) | 0.22 ± 0.03 | 0.74 ± 0.04 | |
3-Br-Cytisine | 0.008 (0.005-0.01) | 0.2 ± 0.009 | 0.8 ± 0.1 | 0.05 (0.04-0.08) | 0.29 ± 0.01 | 0.73 ± 0.04 |
5-I-Cytisine | N.D. | N.E. | 3.2 (2-4) | 0.53 ± 0.01 | 0.99 ± 0.08 | |
5-Br-Cytisine | N.D. | N.E. | 13 (10-16) | 0.31 ± 0.01 | 1.7 ± 0.4 | |
5-Cl-Cytisine | N.D. | N.E. | 14 (94-192) | 0.21 ± 0.01 | 1.50 ± 0.3 |
N.D., not determined; N.E., no effect detected at highest concentration tested (1 mM).