5-HT1A agonist
5-HT1A serotonin receptor agonist
- Presynaptic autoreceptor activation initially ↓ serotonin firing/release
- Prolonged activation desensitizes autoreceptors → serotonin transmission rises
- Serotonin toxicity, secondary to 5-HT2A
- Postsynaptic activation → anxiolytic and antidepressant effects
- ↓ serotonin release
- Prolonged activation of presynaptic 5-HT1A receptors (as seen with SRIs) can lead to their desensitization, eventually ↑ serotonergic transmission
- Possible contributor to serotonin toxicity (secondary to 5-HT2A)
Drugs with this mechanism (8)
- Flibanserin — Multifunctional serotonergic agent for low sexual desire; alcohol interaction.
- Gepirone — Selective 5-HT1A partial-agonist antidepressant; minimal sexual dysfunction but modest efficacy.
- Lysergic acid diethylamide — Classic serotonergic psychedelic; potent 5-HT2A agonist.
- Psilocin — The active dephosphorylated form of psilocybin; a 5-HT2A agonist.
- Serotonin — The endogenous ligand at fourteen receptor subtypes; the home of serotonicity — synaptic serotonin elevation.
- 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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