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. Author manuscript; available in PMC: 2014 Mar 1.
Published in final edited form as: Medchemcomm. 2013 Mar;4(3):564–568. doi: 10.1039/C3MD20374C

Table 1.

Analogue inhibition of [3H]DTBZ binding to rat synaptic vesicle membranes and inhibition of [3H]DA uptake into rat striatal synaptic vesicles.

Compd. [3H]DTBZ VMAT2 [3H]DA Uptake
Ki ± SEM (μM)a Ki ± SEM (μM)a
1 2.76 ± 0.64b 0.47 ± 0.045b
2 0.97 ± 0.00b 0.045 ± 0.002b
3 2.31 ± 0.21b 0.044 ± 0.008b
4 3.41 ± 0.67c 0.060 ± 0.005
5 1.87 ± 0.25c 0.087 ± 0.04
6 4.4 ± 0.76 0.34 ± 0.13
7 1.43 ± 0.136 0.17 ± 0.01
8 22.57 ± 0.23 4.49 ± 0.35
9 5.59 ± 0.94 0.51 ± 0.089
10 9.59 ± 1.47 0.18 ± 0.024
11 3.49 ± 0.63 0.68 ± 0.18
13 > 100 0.054 ± 0.042
a

Each Ki value represents data from at least three independent experiments, evaluated in duplicate;

b

data taken from reference 10;

c

data taken from reference 12b.