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5-HT1 receptor

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.


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.


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.


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.


Main article: 5-HT1E receptor
Gene Agonists Antagonists


Main article: 5-HT1F receptor
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.
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "5-HT1_receptor". A list of authors is available in Wikipedia.
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