TABLE 3.

Summary of in vitro human D₃R affinity, D₃R selectivity and occupancy^* of some antipsychotics, partial agonists, highly preferring/selective D₃R agonists, antagonists.

Compounds	hD2R Ki (nM)	hD3R Ki (nM)	hD3R selectivity	Species	D3R occupancy	References
D3R preferring agonists
(+)-PHNO	0.35	0.17	2.2	Rat	YES	(82, 129)
(-)-Pramipexole	42	1.85	23	Rat	YES	(82, 140)
Selective D3R antagonists
ABT-925	600	2.9	207	Human	YES	(98, 174)
GSK598809	740	6.2	119	Human	YES	(116)
SB-277011A	1047	11	95	Rat	YES	(82, 175, 176)
F17464	12	0.16	72	Human	YES	(145)
Partial agonists
Aripiprazole	0.9	1.6	0.56	Rat, human	Low	(82, 143),
Brexpiprazole	0.3	1.1	0.27	Human	Low	(54)
BP897	61	0.92	66	Human	Moderate	(85)
Cariprazine	0.49	0.09	5.8	Rat, human	YES	(53, 82)
DD-CAR	1.41	0.056	25	Rat	YES	(173)
Antipsychotics
Asenapine	1.4	1.8	0.78	Rat	YES	Table 2
Blonanserin	0.28	0.28	1	Rat, human	YES	(41, 142)
Clozapine	431	283	1.5	Rat, human	Low	(82, 140)
Haloperidol	2.0	5.8	0.34	Rat	YES	(82, 175)
Olanzapine	21	34.7	0.6	Rat, human	Low	(82, 141, 175)
Risperidone	6.2	6.9	0.9	Rat, human	Low	(82, 141, 175)
Quetiapine	417	389	1.1	Rat	Low	(82)
Ziprasidone	4.0	7.4	0.54	Rat	Low	(82)
D2R antagonist
SV-156**	4.04	250	0.02	Rat	NO	(82)

*Rat or human brain occupancy determinations were carried out by [³H](+)-PHNO (rat) or [¹¹C](+)-PHNO (human).

**Compound 9 in Vangveravong et al. (118).