Table 3. Measured inhibition constants of binding (Ki) for the (-)-stepholidine C3 analogues against the dopamine D3 receptor.
Compounds | C3-substituent | Kia,b |
---|---|---|
1a | Et | 40.0 |
1b | n-Pr | 46.0 |
1c | n-Bu | 51.0 |
1d | n-Pen | 33.0 |
1e | n-Hex | 26.0 |
1f | 2-fluroethyl | 86.0 |
a In nM. Experiments were carried out in triplicate—uncertainties are estimated as 13% of reported Ki;
b[3H] N-methylspiperone used as radioligand; chlorpromazine used as a reference compound with Ki = 11.0 nM. The biochemical details of the assay are provided in the main text.