. Author manuscript; available in PMC: 2013 Jul 29.

Published in final edited form as: J Med Chem. 2009 Dec 10;52(23):7878–7882. doi: 10.1021/jm900770h

Table 1.

Interaction of 2 and pyrrolidine analogs with VMAT2.

Analog	[³H]DTBZ; Ki ± SEM (μM)	VMAT2 [³H]-DA Uptake Ki ± SEM (μM)	Ratio [³H]DTBZ binding/[³H]-DA uptake
Tetrabenazine	0.013 ± 0.001	0.054 ± 0.015	0.24
1	2.76 ± 0.64	0.470 ± 0.045	5.87
2	0.97 ± 0.19	0.033 ± 0.041	29.4
3	2.31 ± 0.21	0.023 ± 0.004	100
4	5.32 ± 0.45	4.05 ± 0.612	1.31
5	6.46 ± 1.70	2.11 ± 0.50	3.06
6	3.06 ± 0.17	0.029 ± 0.007	106
7	8.80 ± 2.30	0.270 ± 0.035	32.6
8	3.40 ± 0.030	0.054 ± 0.017	63.0
9	3.97 ± 0.64	0.120 ± 0.015	33.1
10	1.33 ± 0.19	0.035 ± 0.006	38.0
11	14.45 ± 2.13	0.170 ± 0.030	85.0
14	4.34 ± 0.71	1.290 ± 0.240	3.36
15	5.05 ± 1.05	1.940 ± 0.470	2.60
18	2.75 ± 0.63	0.140 ± 0.049	19.6
19	5.61 ± 0.91	0.270 ± 0.053	20.7
22	1.64 ± 0.12	0.0093 ± 0.00075	176
23	2.46 ± 0.42	0.019 ± 0.00091	130
25	0.27 ± 0.0067	0.014 ± 0.0011	19.3
26	2.78 ± 0.63	0.12 ± 0.011	23.2