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5-HT1A partial agonist

• Offsets EPS caused by antipsychotics by releasing DA in side-effect pathways (similar downstream effect as blocking 5-HT2A)
• May counter SRI-induced sexual dysfunction
• Possibly neuroprotective
• Seemingly all good things

Drugs with this mechanism (20)

• 1-PP — Buspirone metabolite; alpha-2 antagonism that adds noradrenergic activation the parent does not have.
• Aripiprazole — D2 partial agonist; weight-favorable, activating, low prolactin; can cause akathisia.
• Aripiprazole lauroxil LAI — Long-acting aripiprazole prodrug injection for schizophrenia; requires a loading strategy.
• Aripiprazole lauroxil LAI — Rapid-start aripiprazole lauroxil injection used only to initiate Aristada treatment.
• Aripiprazole monohydrate LAI — Extended-interval aripiprazole LAI for schizophrenia and bipolar maintenance.
• Aripiprazole monohydrate LAI — Long-acting aripiprazole for schizophrenia and bipolar maintenance; akathisia remains prominent.
• Brexpiprazole — D2 partial agonist similar to aripiprazole but less activating.
• Buspirone — Non-sedating 5-HT1A partial agonist anxiolytic; no dependence, slow onset.
• Cariprazine — D3-preferring dopamine partial agonist for schizophrenia, bipolar disorder, and adjunctive depression.
• Dehydro­ aripiprazole — Aripiprazole's long-lived active metabolite, with the same D2 partial agonism and a large share of steady-state exposure.
• Desmethyl­ cariprazine — Cariprazine metabolite with the same D3-preferring partial agonism as the parent.
• Gepirone — Selective 5-HT1A partial-agonist antidepressant; minimal sexual dysfunction but modest efficacy.
• Lurasidone — Weight-favorable atypical; must be taken with a 350-kcal meal.
• mCPP — Trazodone and nefazodone metabolite; a 5-HT2C agonist that causes anxiety and dysphoria, and accumulates when CYP2D6 is inhibited.
• Norquetiapine — Quetiapine's active metabolite, and the source of the norepinephrine reuptake block and muscarinic blockade the parent lacks.
• Ulotaront — Investigational TAAR1/5-HT1A agonist for schizophrenia without D2 blockade; phase 3 efficacy findings have been disappointing.
• Vilazodone — SSRI plus 5-HT1A partial agonist; take with food for absorption.
• Vortioxetine — Multimodal serotonergic antidepressant; cognitive benefits and less sexual dysfunction, but dose-related nausea.
• Ziprasidone — Weight-neutral atypical requiring food for absorption; QT prolongation limits use.
• Ziprasidone IM — Rapid IM antipsychotic for acute agitation; low metabolic burden but substantial QT liability.

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