Pharmacodynamics +<unk>  Site Ki (nM) Action Ref 5-HT1A 0.12 Partial agonist 5-HT1B 32 5-HT2A 0.47 Antagonist 5-HT2B 1.9 Antagonist 5-HT2C 12–34 Partial agonist 5-HT5A 140 5-HT6 58 Antagonist 5-HT7 3.7 Antagonist D1 160 D2L 0.30 Partial agonist D3 1.1 Partial agonist D4 6.3 D5 α1A 3.8 Antagonist α1B 0.17 Antagonist α1D 2.6 Antagonist α2A 15 Antagonist α2B 17 Antagonist α2C 0.59 Antagonist β1 59 Antagonist β2 67 Antagonist β3 >10,000 H1 19 Antagonist H2 >10,000 H3 >10,000 52% at 10 μM M1 67% at 10 μM M2 >10,000 σ 96% at 10 μM 65% at 10 μM Blocker 0% at 10 μM Blocker 90% at 10 μM Blocker Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. Most or all data are for human cloned proteins.<unk>  acts as a partial agonist of the serotonin 5-HT1A receptor and the dopamine D2 and D3 receptors. Partial agonists have both blocking properties and stimulating properties at the receptor they bind to. The ratio of blocking activity to stimulating activity determines a portion of its clinical effects.<unk>  has more blocking and less stimulating activity at the dopamine receptors than its predecessor, aripiprazole, which may decrease its risk for agitation and restlessness. Specifically, where aripiprazole has an intrinsic activity or agonist effect at the D2 receptor of 60%+,<unk>  has an intrinsic activity at the same receptor of about 45%. For aripiprazole, this means more dopamine receptor activation at lower doses, with blockade being reached at higher doses, whereas<unk>  is the opposite. By contrast,<unk>  has a much higher affinity for the 5-HT1A receptor than aripiprazole as well as a much higher intrinsic activity. In vivo characterization of<unk>  shows that it may act as a near-full agonist of the 5-HT1A receptor. This may further underlie a lower potential than aripiprazole to cause treatment-emergent, movement-related disorders such as akathisia due to the downstream dopamine release that is triggered by 5-HT1A receptor agonism. It is also an antagonist of the serotonin 5-HT2A, 5-HT2B, and 5-HT7 receptors, which may contribute to antidepressant effect. It also binds to and blocks the α1A-, α1B-, α1D-, and α2C-adrenergic receptors. The drug has negligible affinity for the muscarinic acetylcholine receptors, and hence has no anticholinergic effects. Although<unk>  has less affinity for H1 compared to aripiprazole weight gain can occur.
Brexpiprazole
Lorpiprazole
Mepiprazole
Aripiprazole
Pirlindole
Risperidone
Electroconvulsive therapy
Edivoxetine