5-HT7 antagonist
5-HT7 serotonin receptor antagonist
- Receptors in cortex, thalamus and the circadian clock
- May enhance antidepressant/cognitive signaling
- May advance circadian phase
- Little is proven
- Possible early waking due to phase-advance
- Possible constipation
- Possible mitigation of antipsychotic-induced metabolic syndrome
- Possible ↑ neurogenesis & synaptic plasticity
- Potentially ↓ tau hyperphosphorylation and ↓ β-amyloid–induced toxicity
- Vortioxetine (Trintellix) is a neutral antagonist that does not block constitutive activity at 5-HT7 receptors—possible cognitive benefit but not theorized to prevent Alzheimer’s
Drugs with this mechanism (22)
- 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.
- Asenapine — Sublingual/transdermal atypical; oral tablets are ineffective if swallowed.
- Asenapine transdermal — Once-daily asenapine patch - the only transdermal antipsychotic.
- Dehydroaripiprazole — Long-lived active aripiprazole metabolite; same D2 partial agonism, large share of steady-state exposure.
- Lurasidone — Weight-favorable atypical; requires a 350-kcal meal.
- Paliperidone — Active metabolite of risperidone; extended-release oral and long-acting injectables.
- Paliperidone palmitate LAI — Long-acting paliperidone palmitate injection for schizophrenia-spectrum maintenance.
- Paliperidone palmitate LAI — Longest-interval paliperidone depot; requires prior stability on a shorter formulation.
- Paliperidone palmitate LAI — Long-acting paliperidone injection for schizophrenia and schizoaffective disorder.
- Paliperidone palmitate LAI — Extended-interval paliperidone LAI for schizophrenia; prior stabilization on a shorter formulation is required.
- Risperidone — Widely used atypical; dose-related EPS and the class's greatest prolactin burden.
- Risperidone LAI — Microsphere antipsychotic depot; delayed release requires oral overlap and relatively frequent injections.
- Risperidone LAI — Subcutaneous long-acting risperidone for schizophrenia; no oral supplementation after injection.
- Risperidone LAI — Long-acting risperidone depot for schizophrenia; formulated without a prolonged oral bridge.
- Risperidone LAI — Long-acting risperidone microsphere injection for schizophrenia and bipolar I maintenance.
- Risperidone LAI — Subcutaneous extended-release risperidone; no loading dose or oral overlap after initiation.
- Trifluoperazine — High-potency first-generation antipsychotic; low metabolic burden but high movement risk.
- Vortioxetine — Multimodal serotonergic antidepressant; cognitive benefits and less sexual dysfunction, but dose-related nausea.
Self-check
- What sleep change may follow the circadian phase advance from 5-HT7 blockade?
Early waking. - Does vortioxetine block constitutive 5-HT7 activity?
No; it is a neutral antagonist.
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