5-HT (Serotonin) Receptors
Serotonin Receptor Subtypes (5-HT₁–₇), Signalling & Distribution — Receptor-Selective Agonists & Antagonists: Triptans, Buspirone, Ondansetron, Prokinetics, Atypical Antipsychotics & Serotonin Syndrome
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Introduction
- 5-Hydroxytryptamine (5-HT, serotonin) is an indoleamine that acts as a CNS neurotransmitter and a peripheral signalling molecule; ~90–95% of body 5-HT lies in enterochromaffin (EC) cells of the gut, the remainder in platelets and brain, with CNS 5-HT confined to the brainstem raphe nuclei.
- Largest receptor family — Fourteen mammalian 5-HT receptor subtypes grouped into seven subfamilies (5-HT1–5-HT7), each a separate gene product, together form the largest known neurotransmitter/hormone receptor family.
- Why it matters — Receptor-selective serotonergic drugs cover several major therapeutic classes — triptans (5-HT1B/1D, migraine), buspirone (5-HT1A, anxiety), ondansetron (5-HT3, antiemesis), prokinetic benzamides (5-HT4, GI motility) and atypical antipsychotics/pimavanserin (5-HT2A) — and the receptor map explains the toxidrome serotonin syndrome.
- Historical — Erspamer isolated gut enteramine and Page isolated a platelet vasoconstrictor named serotonin in clotting blood; both proved to be 5-HT in the early 1950s. The related indoleamine melatonin (pineal) regulates circadian rhythm. 5-HT itself has no therapeutic use.
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Serotonin 5ht Receptors
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