5-HT1 receptor

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In the field of neurochemistry, 5-HT1 receptors are a subfamily of 5-HT receptors which bind the neurotransmitter and peripheral signal mediator serotonin, also known as 5-hydroxytryptamine (5-HT).[1]

Mode of action

5-HT1 receptors are G protein coupled receptors that Gi/Go-coupled. This causes a cellular decrease of cAMP.


Although working basically through the same mechanism, there are several 5-HT1 receptor subtypes (denoted A-F), each encoded by a separate gene. Furthermore each subtype has a somewhat different tissue distribution and binding preference for synthetic 5-HT1 agonist and antagonist ligands.


Gene Agonists Antagonists

5-HT1A acts on the CNS, where it induces neuronal inhibition and controls behaviour, such as sleep, feeding, thermoregulation, aggression, anxiety.


Gene Agonists Antagonists
  • ergotamine (vasoconstrictor in migraine)
  • sumatriptan (vasoconstrictor in migraine)
  • 5-carboxamidotryptamine (5-CT)

5-HT1B acts on the CNS, where it induces presynaptic inhibition and behavioural effects. It also has vascular effects, such as pulmonary vasoconstriction.


Gene Agonists Antagonists

5-HT1D acts on the CNS, and affects locomotion and anxiety. It also induces vascular vasoconstriction in the brain. Ergotamine works primarily through the 5-HT1B receptor, since the effect through the 5-HT1D receptor is contrary to the mode of action of ergotamine, i.e. vasoconstriction.


Gene Agonists Antagonists


Gene Agonists Antagonists


  1. Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, Saxena PR, Humphrey PP (1994). "International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin)". Pharmacol. Rev. 46 (2): 157–203. PMID 7938165.
  2. Glennon RA, Hong SS, Dukat M, Teitler M, Davis K (1994). "5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist". J. Med. Chem. 37 (18): 2828–30. doi:10.1021/jm00044a001. PMID 8071931.

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