Table 1.

Receptor binding affinity of ITI-007 as measured by radioligand displacement assays: comparison with antipsychotic and antidepressant medications

Receptor	ITI-007a	Risperidoneb	Olanzapineb	Aripiprazoleb	Fluoxetinec
5-HT2A	0.5	0.5	2.5	9	141
D2	32	5.9	31	1.6	>10,000
D1	52	564	128	1,170	>10,000
SERT	62	>1,000	>1,000	240–405	0.9–20
Ratios
D2/5-HT2A	60	12	12.4	0.18	>70
Receptor
H1 histamine	>1,000	14	2	28	1,240
5-HT2C	173	63	7.1	130	69
α1 Adrenergic	73	2.3	60	26	2,260
Ratios
H1/5-HT2A	>2,000	28	1	3	8.8
5-HT2C/5-HT2A	320	126	3	14	0.5
α1/5-HT2A	135	5	24	2.9	16

^aBinding affinities were determined as described in the “Materials and Methods” section;

^bBinding affinities for other compounds were derived from the NIMH Psychoactive Drug Screening Program (PDSP) Database (Roth et al. 2004)

^cBinding affinities for fluoxetine at 5-HT_2A (Owens et al. 1997), D₂ (Sánchez and Hyttel 1999), D₁ (Sánchez and Hyttel 1999), H₁ (Owens et al. 1997, 2002), α₁ adrenergic (Owens et al. 1997, 2002), and 5-HT_2C receptors (Pälvimäki et al. 1996; Bonhaus et al. 1997; Rothman et al. 2000; Sánchez and Hyttel 1999), as cited by from the NIMH Psychoactive Drug Screening Program (PDSP) Database