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 |