Table 1. Pharmacological Properties of Various (α6β2)2β3 AChR Constructs.
AChR Construct | |||||||
Agonist | 1 | 4 | 5 | 6 | 7 | 8 | 9 |
β3−α6−β2−α6−β2 | α6α3cyt+β2+β3 | α6211L,α3cyt+β2+β3 | α6α3cyt-C+β2+β3 | β3–α6+α6α3cyt+β2 | β3–α6+α6211L,α3cyt+β2 | β3–α6211L,α3cyt+α6211L,α3cyt+β2 | |
ACh | |||||||
EC50 (µM) | 1.21±0.16 | 0.740±0.096 | 0.33±0.25 | 0.756±0.262 | 1.40±0.348 | 0.669±0.067 | 6.06±2.68 |
Nicotine | |||||||
EC50 (µM) Efficacy (%) | 0.239±0.031 34.5±2.4 | 0.116±0.044 37.8±4.9 | 0.203±0.054 30.7±26.7 | 0.711±0.120 27.5±1.6 | 0.155±0.081 26.2±5.0 | 0.135±0.083 30.5±5.4 | 0.145±0.055 33.3±3.5 |
Cytisine | |||||||
EC50 (µM) Efficacy (%) | 0.189±0.052 17.0±1.0 | 0.219±0.152 14.9±2.9 | 0.256±0.020 10.4±0.2 | 0.336±0.047 32.3±1.3 | 0.160±0.102 12.5±2.1 | 0.198±0.139 9.92±2.10 | 0.221±0.146 9.46±1.99 |
Varenicline | |||||||
EC50 (µM) Efficacy (%) | 0.0620±0.0248 16.1±1.5 | 0.138±0.071 9.37±1.18 | 0.104±0.012 18.3±0.7 | 0.0374±0.0137 27.6±3.0 | 0.138±0.166 15.6±4.9 | 0.0978±0.0951 22.9±6.1 | 0.114±0.036 5.59±0.06 |
Note the EC50 values for construct 6, which contains the α3 cytoplasmic domain, transmembrane domain 4, and the extracellular C-terminal domain, are significantly different from those of construct 1 for nicotine (p = 0.0266).