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. 2011 Jan 12;2(3):189–194. doi: 10.1021/ml1001689

Table 1. Affinities (Ki) at Dopamine D2 and D3 Receptorsb.

graphic file with name ml-2010-001689_0004.jpg
a

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.

b

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).

c

Calculated using the chemical properties feature in CambridgeSoft ChemDraw Ultra, version 12.0.

d

Data from ref (13).

e

Data from ref (14).

f

For preparation, see ref (40).

g

See ref (25); HEK293T cell homogenate used with [3H]methylspiperone.

h

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).

i

Source and radioligands: D3 rat clone [3H] domperidone; data provided by PDSP.