Tropisetron
5-HT3 antagonist antiemetic that is also an alpha-7 nicotinic partial agonist, studied for cognition and neuroprotection.
Pharmacology
Contents
WHAT IS TROPISETRON?
Detailed overview
Tropisetron is a prescription 5-HT3 receptor antagonist antiemetic (Navoban) developed to control chemotherapy- and surgery-related nausea, but it is also a partial agonist at the alpha-7 nicotinic acetylcholine receptor (α7 nAChR). This dual pharmacology is what makes it interesting for nootropic and neuroprotection research: α7 nAChR activation is involved in sensory gating, memory, and the cholinergic anti-inflammatory pathway. In a short-term human study it improved the P50 auditory gating and some cognitive deficits seen in schizophrenia, and in animal models it showed neuroprotective, anti-inflammatory and analgesic effects. Its cognitive use is currently experimental; the compound's primary approved indication remains antiemesis.
Mechanism
5-HT3 antagonist + α7 nicotinic partial agonist
Half-life
~6-8 h (longer in poor metabolizers)
Legal status
Rx antiemetic (EU; not FDA-approved)
Receptor profile
- Alpha-7 nicotinic acetylcholine receptor (α7 nAChR)Strong
- Serotonin 5-HT3 receptor (antagonist)Strong
- Beta-amyloid (experimental neuroprotection)Moderate
- Dopamine (dose-dependent)Weak
Safety
Side effects, stop signs, contraindications
Side effects · 5
- Headache, the most common antiemetic side effect
- Constipation and digestive discomfort
- Dizziness, drowsiness or fatigue
- QT prolongation and heart-rhythm changes, especially at high doses or with other QT-prolonging drugs
- Rarely abdominal pain, diarrhea or transient blood-pressure changes
Contraindications · 5
- Pregnancy and breastfeeding: safety not adequately established, avoid
- Congenital long QT syndrome, arrhythmia or concurrent use of other QT-prolonging drugs
- Known hypersensitivity to tropisetron or other 5-HT3 antagonists
- Poor CYP2D6 metabolizers: elevated plasma levels and prolonged exposure
- Prescription medicine, not recommended as a nootropic without medical supervision
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Short-term tropisetron treatment and cognitive and P50 auditory gating deficits in schizophrenia
A placebo-controlled study of tropisetron added to risperidone for the treatment of negative symptoms in chronic and stable schizophrenia
Tropisetron enhances recognition memory in rats chronically treated with risperidone or quetiapine
Activation of alpha-7 nicotinic acetylcholine receptor by tropisetron mitigates 3-nitropropionic acid-induced Huntington's disease in rats
Tropisetron attenuates neuroinflammation and chronic neuropathic pain via α7nAChR activation in the spinal cord in rats
Involvement of stimulation of α7 nicotinic acetylcholine receptors in the suppressive effect of tropisetron on dextran sulfate sodium-induced colitis in mice
FAQ
FAQ
5-HT3 antagonist antiemetic that is also an alpha-7 nicotinic partial agonist, studied for cognition and neuroprotection.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.