Table III. In vitro binding affinities of A-84543, A-84543 analogues, and nicotine (NIC) at nAChR subtypes expressed in stably transfected HEK cells or on α4β2* nAChRs from rat forebrain tissue (FB).
Binding was done against ~500 pM [3H]EB. Ki values presented are the Mean ± SEM of three independent measurements and were calculated from competition graphs using the Cheng-Prusoff equation where the rat forebrain KD value of 50 pM was used.
| Ki (nM) vs 500pM [3H]EB | ||||||||
|---|---|---|---|---|---|---|---|---|
| Analogues | α2β2 | α2β4 | α3β2 | α3β4 | α4β2 | α4β2*-FB | α4β4 | α7 |
| A-84543 | 2.0±0.3 | 370±40 | 12±1 | 1,900±20 | 1.4±0.2 | 5.4±0.6 | 150±10 | 340±50 |
| H-11MNH | 0.35±0.09 | 76±12 | 1.3±0.3 | 210±40 | 0.39±0.05 | 0.71±0.10 | 31±6 | 65±5 |
| H-11ONM | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 |
| H-11ONH | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 |
| H-11PNH | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 |
| Nicotine | 21±14 | 91±13 | 52±3 | 370±40 | 7.4±0.9 | 9.8±0.8 | 35±3 | 550±10 |
| A-853803 | 0.073±0.01 | 18±4 | 0.21±0.04 | 78±10 | 0.014±0.003 | 0.25±0.05 | 8.1±1.1 | 420±50 |
3
Values for A-85380 have been added for the purpose of comparison from ref. [24]