. Author manuscript; available in PMC: 2009 Dec 25.

Published in final edited form as: J Med Chem. 2008 Dec 25;51(24):7806–7819. doi: 10.1021/jm8008629

Table 1.

Affinity for cloned D_2L and D₃ receptors expressed in HEK cells measured by inhibition of [³H]spiperone binding. Results are means ± SEM for 3–8 experiments each performed in triplicate.

Compound	K_i, (nM), D_2L [³H]Spiperone	K_i, (nM), D₃ [³H]Spiperone	D_2L/D₃
(±)-7-OH-DPAT	311 ± 47	6.19 ± 1.4	50.2
(−)-5-OH-DPAT	220 ± 37.7	4.73 ± 0.64	46.5
2	2,780 ± 457	395 ± 75	7.03
1	347 ± 51	96.0 ± 4.7	3.61
(−)-6	809 ± 65	38.6 ± 0.7	21
(+)-6	40.6 ± 3.6	1.77 ± 0.42	22.9
(−)-7	26.0 ± 7.5	0.825 ± 0.136	31.5
(+)-7	238 ± 14	18.4 ± 1.0	12.9
9	219 ± 30	72.2 ± 17.2	3
(−)-10	243 ± 65	4.15 ± 0.76	58.6
(+)-10	1,979 ± 567	44.0 ± 10.6	45.0
11	234 ± 40	0.925 ± 0.234	253
(±)-24a	3,326 ± 788	419 ± 119	7.94
(±)-24b	148 ± 30	187 ± 24	0.79
(±)-35a	2,522 ± 554	473 ± 167	5.33
(±)-35b	338 ± 35	256 ± 69	1.3
(±)-35c	289 ± 56	102 ± 20	2.83
(±)-8	49.1 ± 10.3	14.9 ± 4.3	3.30
(+)-8	835 ± 182	89.3 ± 19.4	9.35
(−)-8	23.6 ± 1.1	4.95 ± 1.08	4.77
(±)-43a	1,712 ± 355	736 ± 206	2.33
(±)-43b	136 ± 23	168 ± 24	0.80