Table 2.
Aripiprazole affinity for human receptors
| Types | Affinity | Affinity | Ki (nmol/L) | Biological action | Pharmacological action |
|---|---|---|---|---|---|
| Dopamine receptors | |||||
| D2 | + + + + | Very high | 0.34# | Partial agonist | Yes |
| D3 | + + + + | Very high | 0.8# | Unknown | |
| D4 | + | Moderate | 44# | Unknown | |
| Serotonin receptors | |||||
| 5-HT2B | + + + + | Very high | 0.36## | Inverse agonist | Unknown |
| 5-HT1A | + + + | High | 1.7# | Partial agonist | Unknown |
| 5-HT2A | + + | Moderate | 3.4# | Antagonist/partial agonist | Yes |
| 5-HT2C | + | Limited | 15# | Partial agonist | Unknown |
| 5-HT7 | + + + | High | 39# (10##) | Partial agonist | Unknown |
| 5-HT1D | + + | Moderate | 68## | Antagonist | Unknown |
| 5-HT6 | + | Limited | 570## | Antagonist | Unknown |
| 5-HT1B | + | Limited | 830## | Antagonist | Unknown |
| Noradrenaline receptors | |||||
| α1A | + + | Moderate | 57# (26##) | Antagonist | No |
| α1B | + + | Moderate | 35## | Antagonist | No |
| α2C | + + | Moderate | 38## | Antagonist | No |
| α2A | + + | Moderate | 74## | Antagonist | No |
| α2B | + | Limited | 103## | Antagonist | No |
| Histamine receptors | |||||
| H1 | + + | Moderate | 61# (25##) | Antagonist | No |
Ki the binding affinities were assessed in vitro
#Abilify Maintena prescribing information [ABILIFY MAINTENA—Accessdata.fda.gov]
##SHAPIRO et al. 2003 [121]