5-HT2A inverse agonist
5-HT2A serotonin receptor inverse agonist
- Suppresses constitutive 5-HT2A receptor activity, not merely agonist binding
- Antipsychotic effect independent of dopamine receptor blockade
- Pimavanserin for Parkinson disease psychosis
Drugs with this mechanism (2)
- Norclozapine — Active clozapine metabolite; M1 agonist implicated in some clozapine effects.
- Pimavanserin — Selective 5-HT2A inverse agonist; first drug for Parkinson psychosis, no D2 blockade.
Self-check
- What activity does 5-HT2A inverse agonism suppress beyond agonist binding?
Constitutive receptor activity. - Which psychosis is pimavanserin used for in this deck?
Parkinson disease psychosis.
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