5-HT2B agonist
5-HT2B serotonin receptor agonist
- Activates cardiac valvular fibroblast signaling → valvular fibrosis
- May induce fibrotic changes in multiple organs
- Also associated with pulmonary vascular remodeling/hypertension
- Vasoconstriction → pulmonary hypertension risk
- An off-target liability, never a therapeutic goal
- The forbidden mechanism: new drug development is halted for drugs found to activate 5-HT2B
Drugs with this mechanism (5)
- Cabergoline — Long-acting dopamine agonist for prolactinomas; valvulopathy at high dose.
- Dihydroergotamine — Injectable or intranasal ergot for refractory migraine; never combine closely with a triptan.
- Ergotamine — Ergot alkaloid for migraine; vasoconstrictive, largely supplanted by triptans.
- Fenfluramine — Serotonin releaser once in "fen-phen"; now for Dravet seizures, valvulopathy risk.
- Serotonin — The endogenous ligand at fourteen receptor subtypes; the home of serotonicity — synaptic serotonin elevation.
Self-check
- What cardiac injury is linked to 5-HT2B activation?
Valvular fibrosis. - What pulmonary vascular complication is associated with 5-HT2B activation?
Pulmonary hypertension.
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