TABLE 7

Binding affinity for h-D_2L and h-D₁ receptors (K_i, nM)

K_i ratios (D₁/D₂) have also been listed in comparison with the ratio of the ED₅₀ for suppression of grooming over the ED₅₀ for blockade of agitation at 40 min

Compound	Binding Affinity (K_i, nM)		K_i Ratio D₁/D₂	ED₅₀ Ratio^{^a} GRO_>50/AGI₄₀
Compound	h-D₂	h-D₁	K_i Ratio D₁/D₂	ED₅₀ Ratio^{^a} GRO_>50/AGI₄₀
	nM ( 95% CL) [n]
Amisulpride	9.9 (6.6–14.5) [7]	>6000 [2]	>606	14
Aripiprazole	0.49 (0.20–1.20) [7]	485 (272–867) [2]	990	191
Azaperone	77 (46–128) [7]	Not available	—	9.1
Chlorpromazine	14.6 (7.6–28.0) [13]	73 (–) [1]	5.0	12
Chlorprothixene	3.4 (1.19–9.9) [2]	Not available	—	14
Clozapine	144 (109–190) [11]	174 (113–270) [2]	1.2	0.33
Droperidol	2.89 (1.49–5.6) [8]	Not available	—	>613
Haloperidol	1.70 (1.31–2.21) [18]	88 (49–161) [2]	52	219
JNJ-37822681	146 (116–183) [9]	>6000 [2]	>41	64
JNJ-39269646	202 (158–259) [9]	>6000 [1]	>30	55
Melperone	Not available	Not available	—	12
Olanzapine	57 (35–93) [9]	64 (59–69) [104]	1.1	48
Paliperidone	8.0 (7.3–8.9) [50]	604 (285–1282) [2]	76	48
Perphenazine	1.71 (0.62–4.8) [5]	96 (–) [1]	56	251
Pimozide	2.86 (0.37–22.1) [5]	Not available	—	>52
Quetiapine	563 (443–715) [7]	834	1.5	14
Raclopride	11.8 (8.5–16.5) [7]	>6000 [1]	>508	>820
Remoxipride	488 (375–635) [3]	>6000 [2]	>12	>625
Risperidone	5.3 (4.9–5.7) [152]	170 (119–243) [13]	>32	28
Sertindole	5.4 (2.47–12.0) [6]	834 (774–899) [2]	154	3.0
Ziprasidone	4.4 (3.4–5.9) {16]	74 (23–236) [2]	17	56
Zotepine	5.0 (2.54–9.8) [6]	82 (63–105) [2]	16	19

↵^a Ratio of the ED₅₀ for suppression of grooming (GRO) over the ED₅₀ for blockade of agitation (AGI) at 40 minutes (Table 6, last column).