TABLE 3.

Calculated RO for proposed targets of interest by unbound brain concentration (C_max,brain,u)

Target	System	K i (nM)	RO
			30 mg IR, s.d. (Cmax,brain,u = 145 nM/54.1 ng/ml)	30 mg IR, q.d. (Cmax,brain,u = 178 nM/66.3 ng/ml)	300 mg OAD, q.d. (Cmax,brain,u = 583 nM/217 ng/ml)
5‐HT2A	Serotonergic	14	0.912	0.927	0.977
α1B	Adrenergic	15	0.906	0.922	0.975
5‐HT1D	Serotonergic	26	0.848	0.873	0.957
α1D	Adrenergic	27	0.843	0.868	0.956
5‐HT2B	Serotonergic	48	0.752	0.788	0.924
5‐HT1A	Serotonergic	82	0.640	0.685	0.877
α1A	Adrenergic	98	0.597	0.645	0.856
H1	Histaminergic	190	0.433	0.484	0.754
α2C	Adrenergic	240	0.377	0.426	0.708
SERT	Serotonergic	280	0.342	0.389	0.675
5‐HT2C	Serotonergic	307	0.321	0.367	0.655
5‐HT7	Serotonergic	406	0.264	0.305	0.589
α2A	Adrenergic	430	0.253	0.293	0.575
α2B	Adrenergic	460	0.240	0.279	0.559
D3	Dopaminergic	490	0.229	0.267	0.543
D2	Dopaminergic	560	0.206	0.241	0.510
5‐HT1B	Serotonergic	814	0.152	0.180	0.417
D1	Dopaminergic	929	0.135	0.161	0.385
D5	Dopaminergic	1200	0.108	0.129	0.327
5‐HT5A	Serotonergic	2340	0.058	0.071	0.199
NK‐1	Tachykinin	3300	0.042	0.051	0.150
σ1	Sigma	3980	0.035	0.043	0.128
β2	Adrenergic	6000	0.024	0.029	0.089
5‐HT4	Serotonergic	10,000	0.014	0.018	0.055
MOP	Opiate	15,436	0.009	0.011	0.036
M4	Cholinergic	30,000	0.005	0.006	0.019
M2	Cholinergic	34,127	0.004	0.005	0.017

For normalization from molar to ng/ml the molecular weight of the trazodone free‐base was considered.

Values in bold indicate RO greater than or equal to 50%.

Abbreviations: C_max,brain,u, unbound brain concentration; IR, immediate release; RO, receptor occupancy.