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. Author manuscript; available in PMC: 2011 Aug 1.
Published in final edited form as: Expert Opin Pharmacother. 2010 Aug;11(12):2107–2115. doi: 10.1517/14656566.2010.506188

Table 1.

Equilibrium dissociation constants for various atypical antipsychotics including asenapine (Asen, aka Org 5222), clozapine (Cloz), olanzapine (Olanz), risperidone (Risp), and sertindole (Sert). Efficacy at dopamine D2 receptors is shaded given that clinical efficacy of antipsychotics require ~70% D2 occupancy. Muscarinic effects are boxed given that efficacy at muscarinic receptors have been linked to weight gain/cognitive dysfunction side effects. The typical antipsychotic haloperidol (Halo) is added for comparative purposes.

Equilibrium dissociation constants for antipsychotics at human brain receptors
Asen 5HT2C
0.27
5HT2A
0.77
α1
1.1
D2
2
H1
9.3
5HT1D
10.2
5HT1A
15
α2
16
M
7000
Cloz 5HT2A
2.59
H1
3.1
5HT2C
4.8
α1
6.8
M
9
α2
15
5HT1D
130
5HT1A
160
D2
210
Olanz H1
0.087
5HT2A
1.48
5HT2C
4.1
D2
20
M
36
α1
44
5HT1D
150
α2
280
5HT1A
610
Risp 5HT2A
0.15
α1
2.7
D2
3.77
5HT1D
3.9
H1
5.2
α2
8
5HT2C
32
5HT1A
190
M
34000
Sert 5HT2A
0.14
D2
2.7
α1
3.9
5HT2C
6
5HT1D
20
α2
190
H1
320
5HT1A
1050
M
5000
Halo D2
2.6
α1
17
5HT1D
40
5HT2A
61
H1
260
α2
600
5HT1A
1800
5HT2C
4700
M
>10000