Table 1. Affinities (Ki) at Dopamine D2 and D3 Receptorsb.
Source and radioligands: D1, rat striatum [3H]SCH23390; D2, rat striatum [3H] domperidone; D3, human D3 clone [3H]domperidone; errors are expressed as standard deviations.
Compounds have been tested and found to have low affinity to D1 (Ki > 5000) except for the following: 1 (Ki = 650 ± 310 nM), 2a (Ki = 490 ± 220 nM), 3b (Ki = 4300 ± 250 nM), 8f (Ki = 3700 ± 1200 nM), and 11e (Ki = 340 ± 44 nM), and no affinity to D1high, except for the following: 1 (Ki = 4.6 ± 1.2 nM), 2a (Ki = 1 ± 0.2 nM), and 2b (Ki = 8.1 ± 0.7nM); data for 1 and 2a obtained from ref (13).
Calculated using the chemical properties feature in CambridgeSoft ChemDraw Ultra, version 12.0.
Data from ref (13).
Data from ref (14).
For preparation, see ref (40).
See ref (25); HEK293T cell homogenate used with [3H]methylspiperone.
The following compounds were also found to have D3high affinity: 2c (Ki = 3.8 ± 2 nM), 3a (Ki = 130 ± 100 nM), 3b (Ki = 1.2 ± 1 nM), 8a (Ki = 1.1 ± 2 nM), 8b (Ki = 1.9 ± 1.5 nM), 8c (Ki = 230 ± 140 nM), and 8d (Ki = 250 ± 19 nM).
Source and radioligands: D3 rat clone [3H] domperidone; data provided by PDSP.