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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

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

Subtypes

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

Main article: 5-HT1A receptor
Gene Agonists Antagonists
HTR1A

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

5-HT1B

Main article: 5-HT1B receptor
Gene Agonists Antagonists
HTR1B
  • 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

Main article: 5-HT1D receptor
Gene Agonists Antagonists
HTR1D

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

Main article: 5-HT1E receptor
Gene Agonists Antagonists
HTR1E

5-HT1F

Main article: 5-HT1F receptor
Gene Agonists Antagonists
HTR1F

References

  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.

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