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. 2014 Jul 28;9(7):e103244. doi: 10.1371/journal.pone.0103244

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 β3α6+α6α3cyt+β2 β3α6+α6211L,α3cyt+β2 β3α6211L,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).