Table 2.
Pharmacological activity at VMAT2 of analogues 14, 21–24 in comparison with 1
Analogue | [3H]-DTBZ; Ki ± SEM (μM) | VMAT2 [3H]DA uptake Ki ± SEM (μM) |
---|---|---|
1•0.5 H2SO4 | 0.97 ± 0.19 | 0.045 ± 0.002 |
14 | 33.3 ± 16.3 | 3.72 ± 0.32 |
21 | 5.87 ± 1.72 | 5.23 ± 3.03 |
22•HCl | 0.96 ± 0.37 | 0.067 ± 0.015 |
23•HCl | 2.64 ± 1.41 | 0.051 ± 0.005 |
24•C4H4O4 | 26.01 ± 2.88 | 2.13 ± 0.28 |