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. Author manuscript; available in PMC: 2013 Jul 29.
Published in final edited form as: Bioorg Med Chem Lett. 2010 Nov 24;21(1):88–91. doi: 10.1016/j.bmcl.2010.11.070

Table 1.

Inhibition of nicotine-evoked [3H]DA release from superfused rat striatal slices.

Compound DA Release
Head group Linker Inhibition (100 nM)a IC50 (nM) and Imaxbb
bPiDDB 1 graphic file with name nihms258235t1.jpg bis-1,12-dodecane NDc 2.0±1.0d
63%
bPiDB 8 bis-1,10-decane ND 180±110
63%
tPy3PiB 3 tris-linker (unsaturated) 40±12% 0.2±0.07e
67%
7 graphic file with name nihms258235t2.jpg bis-1,12-dodecane 50±21% 0.95±0.30
60%
9 bis-1,10-decane 36±12% 37.4±18.7
65%
16 tris-linker (unsaturated) 83±2% 3.22±1.36
67%
bPyiQB 2 graphic file with name nihms258235t3.jpg rigid bis-linker ND 63±39f
59%
12 bis-1,12-dodecane ND 40±30
53%
13 bis-1,10-decane ND 70±50
95%
18 tris-linker (saturated) 28±11% ND
21 tetrakis-linker ND 56±45
52%
11 graphic file with name nihms258235t4.jpg rigid bis-linker 18±18% ND
14 bis-1,12-dodecane ND 8.59±3.27
76%
15 bis-1,10-decane ND 9.91±9.23
74%
19 tris-linker (saturated) 58±9% 0.35±0.09
58%
22 tetrakis-linker 84±4% 205±132
64%
tkP3HPPB 4 graphic file with name nihms258235t5.jpg tetrakis-linker 41±15% 3.0±3.0g
63%
23 graphic file with name nihms258235t6.jpg tetrakis-linker 40±23% 30±16
64%
a

Percentage inhibition at 100 nM is presented unless otherwise specified. Each value represents data from at least 3 independent experiments, each performed in duplicate.

b

IC50 and Imax from full concentration response assays; data from 4–6 independent experiments.

c

Not determined;

d

taken from results published in ref 15;

e

taken from results published in ref 13;

f

taken from results published in ref 12;

g

taken from results published in ref 14.