Brexpiprazole

2022-04-23: Drugs reference: https://en.wikipedia.org/wiki/Brexpiprazole comprehensive Ki list.

Brexpiprazole #

Atypical antipsychotic. Mainly:

• 5-HT1A and 5-HT2C partial agonist; antagonizes just about everything else.
• SERT and DAT blocker.
• A1 blocker - improves memory in Alzheimer’s (like prazosin)
• α1, α2, β2 Adrenergic Receptor antagonist.
• D2/D3 partial agonist

  Site	Ki (nM)	Action
  5-HT1A	0.12	Partial agonist
  5-HT2A	0.47	Antagonist
  5-HT2B	1.9	Antagonist
  5-HT2C	12–34	Partial agonist
  5-HT7	3.7	Antagonist
  D2L	0.30	Partial agonist
  D3	1.1	Partial agonist
  α1A	3.8	Antagonist
  α1B	0.17	Antagonist
  α1D	2.6	Antagonist
  α2A	15	Antagonist
  α2B	17	Antagonist
  α2C	0.59	Antagonist
  H1 19	Antagonist
  SERT	65% at 10 μM	Blocker
  NET	0% at 10 μM	Blocker
  DAT	90% at 10 μM	Blocker