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The correct title of this article is 5-HT1 receptor. It appears incorrectly here because of technical restrictions.

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[edit | edit source]

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

Subtypes[edit | edit source]

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.

5-HT1A[edit | edit source]

Main article: 5-HT1A receptor
Gene Agonists Antagonists

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

5-HT1B[edit | edit source]

Main article: 5-HT1B receptor
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.

5-HT1D[edit | edit source]

Main article: 5-HT1D receptor
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.

5-HT1E[edit | edit source]

Main article: 5-HT1E receptor
Gene Agonists Antagonists

5-HT1F[edit | edit source]

Main article: 5-HT1F receptor
Gene Agonists Antagonists

References[edit | edit source]

  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.
  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.

External links[edit | edit source]

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