Table 1.

Binding affinities for dopamine D₂-like receptors

Compound	Ki (nM)a			D2/D3e	Log Pf
	D2b	D3c	D4d
11a	128±8.8	0.7±0.10	187±21	183	3.50
11b	119±3.5	3.9±0.3	608±50	30	2.33
11c	101±15.5	2.9±0.5	372±7.1	35	3.62
11d	125±6.5	5.5±1.3	429 ±19	23	2.77
11e	108±7.5	9.0±0.7	522±51	12	2.19
11f	128±9.7	1.8±0.01	728±100	71	2.41
11g	111±9.2	3.7±0.3	350±47	30	2.64
11h	95.2±3.8	8.8±0.9	159±25	11	2.60
11i	56.5±5.9	7.5±0.7	188±43	8	2.16
11j	138±18.4	2.5±0.4	161±9.1	56	2.86
11k	125±7.0	1.5±0.2	297±35	82	4.01
11l	107±16.3	9.0±0.5	342±37	12	3.59
11m	151±11.2	13.2±1.7	748±36	11	1.01
11n	100±10.0	11.6±2.2	657±10	9	3.52
11o	43.7±7.0	4.8±1.0	177±19	9	2.81
11p	280±13.2	8.0±1.5	403±33	35	3.60
11q	119±7.5	15.0±0.7	641±57	8	1.89
11r	145±8.2	17.9±1.5	830±57	8	2.02
11s	152±25.6	44.2±3.7	441±98	3	1.23
11t	169±10.9	7.2±0.2	706±67	23	1.66
NGB-2904	112±22	2.0±0.4	NDg	56	6.94h

^aMean ± SEM, K_i values were determined by at least three experiments.

^bK_i values for D₂ receptors were measured using human D₂ (long) expressed in HEK cells with [¹²⁵I]ABN as the radioligand.

^cK_i values for D₃ receptors were measured using human D₃ expressed in HEK cells with [¹²⁵I]ABN as the radioligand.

^dK_i values for D₄ receptors were measured using human D_4.4 expressed in HEK cells with [¹²⁵I]ABN as the radioligand.

^eK_i for D₃ receptors/ K_i for D₂ receptors.

^fCalculated C log P values using the program C log P by Advanced Chemistry Development, Inc. Toronto, Canada (ACD/Labs).

^gNot determined.

^hPublished data, Leopoldo et al, 2002. ²⁴