Table 1.

Comparison of In Vitro Potencies of Antipsychotic Effects with Clinical Plasma Levels The IC₅₀ values are shown for antipsychotic-mediated inhibition of nicotine-evoked Rb + efflux from α4β2/SH-EP1 cells, ACh-induced α7 current in oocytes, nicotine-evoked dopamine (DA) release from striatal synaptosomes and epibatidine-evoked norepinephrine (NE) release from hippocampal slices. Numbers in parentheses represent 95% confidence intervals. Maximum plasma concentrations (ng/mL) of antipsychotics represent values achieved in clinical studies, reported in the literature (supporting references at right). Maximum plasma levels (μM) were calculated from reported concentrations and known molecular weights of the individual compounds (left column).

Anti-psychotic	Rb + Flux IC50 (μM)	α7 Current IC50 (μM)	DA Release IC50 (μM)	NE Release IC50 (μM)	Max. Plasma Levels (ng/mL)	Max. Plasma Levels (μM)	References
Clozapine	5.2 (2.8–9.9)	8.4 (3.8–18.8)	5.3 (2.4–11.6)	2.2	574	1.8	Diaz et al., 2005
MW = 326.8					880	2.7	Freudenreich et al., 1996
					1088	3.3	Perry et al., 1991
					1310	4.0	Dumortier et al., 1998
					1920	5.9	Wong et al., 2006
N-desmethyl-clozapine	2.1 (0.9–4.7)	3.2 (1.3–7.7)	2.1 (1.1–3.9)	2.2	420	1.3	Flanagan et al., 2003
					580	1.9	Dumortier et al., 1998
MW = 312.8					720	2.3	Wong et al., 2006
Quetiapine	13.1 (9.1–18.9)	ND	5.9 (1.1–20.9)	ND	91	0.24	Lin et al., 2004
MW = 383.5					491	1.3	Aichhorn et al., 2006
					1042	2.7	Grimm et al., 2006
					1454	3.8	Tauscher-Wisniewski et al., 2002
Chlorpromazine	7.6 (4.5–12.7)	9.1 (6.3–13.2)	2.8 (1.8–19.6)	1.7	124	0.4	Della Corte et al., 1993
MW = 355.3					422	1.2	Chetty et al., 1996
					839	2.4	Chetty and Miller, 2001
Haloperidol	8.6 (4.2–17.6)	10.5 (4.5–24.7)	4.8 (1.2–6.7)	0.8	86	0.23	Roh et al., 2001
MW = 375.9

ND = not done.