5-HT 1A receptor

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5-HT 1A receptor
5-HT1A receptor
Scheme of the transmembrane domains in the HT1AR
Properties of human protein
Mass / length primary structure 422 amino acids
Identifier
Gene name HTR1A
External IDs
Occurrence
Parent taxon Vertebrates

The 5-HT 1A receptor (abbr. 5-HT1A ) is a protein in the cell membrane of vertebrate cells, mainly in the brain , but also in peripheral nerve cells and in fetal lymphoid tissue . The receptor is mainly pre- and postsynaptic and serves as a serotonin sensor in the synaptic gap. Agonists to 5-HT1A have potential anti-anxiety effects. The receptor belongs to the family of serotonin receptors . The associated gene is called HTR1A and is located on chromosome 5 in humans.

distribution

The 5-HT 1A receptor is the most widely used serotonin receptor. It is found in the cerebral cortex , hippocampus , amygdala and raphe nuclei .

Medical importance

The 5-HT 1A receptor is the point of attack in the treatment of anxiety disorders , blood pressure problems , psychoses and aggressive behavior disorders .

Scientists from Peking University found that a C-1019G point mutation in the 5-HT 1A gene reduced the likelihood of being in a relationship from 50.4% to 39.0%. For the first time, a direct influence of genetic disposition on the development of relationships could be shown, although the mutation is only one of many factors.

Signal transduction

The receptor is linked to an inhibiting G protein (Gi / Go). The binding of serotonin leads to a reduction in the concentration of intracellular cyclic adenosine monophosphate (cAMP) and thus to the inhibition of protein kinase A , whereupon the probability of potassium channels being open increases. In addition, the L-type calcium channels are inhibited via the Go protein . These two mechanisms lead to a decreased release of serotonin.

Agonists

Substances that bind to the 5-HT 1A receptor are, for example: cannabidiol (CBD), ipsapirone , gepirone , buspirone , urapidil , tandospirone and 5-hydroxytryptamine (= serotonin, 5-HT).

Antagonists

Substances that block the 5-HT 1A receptor include: propranolol and dotarizine .

literature

  • H. Lüllmann among others: Pharmacology and Toxicology. Thieme-Verlag, 2006, ISBN 3-13-368516-3 , pp. 115f

Web link

Individual evidence

  1. Homologues at OMA
  2. Entry at InterPro
  3. ^ J. Liu, P. Gong, X. Zhou: The association between romantic relationship status and 5-HT1A gene in young adults. In: Scientific reports. Volume 4, 2014, ISSN  2045-2322 , p. 7049, doi : 10.1038 / srep07049 . PMID 25412229 , PMC 4238299 (free full text).