TABLE 2

Displacement of [3H]A-585539 binding to rat and human brain: comparison with [3H]MLA



[3H]A-585539

[3H]MLA
Rat
Human
Rat
Compound
Ki,
95% CI
nH
n
KI
95% CI
nH
n
Ki
95% CI
nH
n
nM nM nM
A-585539 0.071 0.06-0.09 0.8 4 ND 1.01 0.6-1.6 1.0 4
MLA 0.19 0.16-0.23 1.1 10 2.5 1.8-3.6 0.9 9 2 1.5-2.7 1.1 10
TC-5280 0.36 0.33-0.38 0.9 3 ND 1.2 0.9-1.5 1.6 3
Epibatidine 2.7 2.1-3.4 1.0 8 1.1 0.7-1.7 0.8 3 21 13-33 1.4 4
PNU 282987 6.5 5.8-7.2 0.9 7 3.2 2.2-4.5 0.9 6 46.4 33-66 1.1 6
A-582941 10.8 6.2-19 1.1 9 16.7 13-22 1.1 6 88 59-130 1.7 11
α-Bungarotoxin 12.2 9.4-16 2.1 3 17.7 8.1-39 0.9 2 17.4 14-21 1.2 3
Anatoxin-A 19.8 16-24 1.2 5 9.7 7.1-13 1.1 4 122 97-150 1.6 6
Varenicline 33.4 23-49 1.2 6 15.6 12.0-20 0.9 6 144 100-210 1.3 7
A-85380 33.6 20-57 1.1 4 17.6 6.4-48 0.9 2 299 150-610 1.6 4
(±)-AR-R17779 128 100-160 1.0 5 40.5 27-60 1.0 6 1390 1100-1760 1.5 5
(-)-Nicotine 176 62-500 1.1 8 159 110-230 1.0 6 1450 850-2500 1.6 6
DMPP
308
220-420
1.5
4
153
110-210
1.7
3
1580
1200-2100
1.6
4
  • CI, 95% confidence interval; n = number of determinations, each carried out in duplicate; DMPP, 1,1-dimethyl-4-phenylpiperazinium; ND, not determined.