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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 2.

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

Compd. Ar [3H]DTBZ VMAT2 [3H]DA Uptake
Ki ± SEM (μM)a Ki ± SEM (μM)a
14a graphic file with name nihms-445754-t0001.jpg 0.56 ± 0.08 0.19 ± 0.05
14b 1.28 ± 0.13 0.86 ± 0.12
15a graphic file with name nihms-445754-t0002.jpg 1.30 ± 0.05 0.16 ± 0.04
15b 5.61 ± 0.62 0.76 ± 0.04
16a graphic file with name nihms-445754-t0003.jpg 1.00 ± 0.16 0.19 ± 0.06
16b 1.08 ± 0.38 1.03 ± 0.16
17a graphic file with name nihms-445754-t0004.jpg 1.04 ± 0.73 0.49 ± 0.06
17b 1.87 ± 0.69 0.79 ± 0.08
18a graphic file with name nihms-445754-t0005.jpg 0.46 ± 0.22 0.14 ± 0.02
18b 2.73 ± 0.68 0.52 ± 0.04
19a graphic file with name nihms-445754-t0006.jpg 8.29 ± 2.79 0.029 ± 0.008
19b 7.74 ± 2.34 0.18 ± 0.04
20a graphic file with name nihms-445754-t0007.jpg 10.4 ± 0.65 0.14 ± 0.04
20b 13.9 ± 0.38 0.09 ± 0.04
21a graphic file with name nihms-445754-t0008.jpg 0.31 ± 0.07 0.03 ± 0.002
21b 0.13 ± 0.07 0.08 ± 0.01
22a graphic file with name nihms-445754-t0009.jpg > 100 0.79 ± 0.23
22b 90.2 ± 9.70 2.25 ± 1.30
23 graphic file with name nihms-445754-t0010.jpg 1.75 ± 0.36 0.023 ± 0.006
23a 0.53 ± 0.053 0.060 ± 0.006
24 graphic file with name nihms-445754-t0011.jpg 0.93 ± 0.22 0.039 ± 0.002
24a 0.21 ± 0.02 0.16 ± 0.035
25 graphic file with name nihms-445754-t0012.jpg 5.24 ± 1.81 0.043 ± 0.003
25a 0.62 ± 0.10 0.104 ± 0.004
28 13.1 ± 7.4 0.048 ± 0.005
28a - 91 ± 40 0.57 ± 0.05
a

Each Ki value represents data from at least three independent experiments, evaluated in duplicate; The data of 14a–22a and 14b–22b were taken from reference 16.