World Library  
Flag as Inappropriate
Email this Article

Dopamine D2 receptor

Article Id: WHEBN0022759606
Reproduction Date:

Title: Dopamine D2 receptor  
Author: World Heritage Encyclopedia
Language: English
Subject: Mania, Risperidone, Perphenazine, Thioridazine, Mirtazapine, Bromocriptine, Imipramine, Cabergoline, Doxepin, Spiperone
Collection:
Publisher: World Heritage Encyclopedia
Publication
Date:
 

Dopamine D2 receptor

Dopamine receptor D2
1I15.
Available structures
PDB Ortholog search: RCSB
Identifiers
DRD2 Gene
RNA expression pattern

Dopamine receptor D2, also known as D2R, is a protein that, in humans, is encoded by the DRD2 gene.

Function

This gene encodes the D2 subtype of the dopamine receptor. This G protein-coupled receptor inhibits adenylyl cyclase activity.

Alternative splicing of this gene results in two transcript variants encoding different isoforms. A third variant has been described, but it has not been determined whether this form is normal or due to aberrant splicing.[1]

In mice, regulation of D2R surface expression by the calcium sensor NCS-1 in the dentate gyrus controls exploration, synaptic plasticity and memory formation.[2]

Genetics

Allelic variants:

  • A-241G
  • C132T, G423A, T765C, C939T, C957T, and G1101A[3]
  • Cys311Ser
  • -141C insertion/deletion[4] The polymorphisms has been investigated with respect to association with schizophrenia.[5]

Some researchers have previously associated the polymorphism Taq 1A (rs1800497) to the DRD2 gene. However, the polymorphism resides in exon 8 of the ANKK1 gene.[6]

Ligands

Most of the older antipsychotic drugs such as chlorpromazine and haloperidol are antagonists for the dopamine D2 receptor, but are, in general, very unselective, at best selective only for the "D2-like family" receptors and so binding to D2, D3 and D4, and often also to many other receptors such as those for serotonin and histamine, resulting in a range of side-effects and making them poor agents for scientific research. In similar manner, older dopamine agonists used for Parkinson's disease such as bromocriptine and cabergoline are poorly selective for one dopamine receptor over another, and, although most of these agents do act as D2 agonists, they affect other subtypes as well. Several selective D2 ligands are, however, now available, and this number is likely to increase as further research progresses.

Agonists

Antagonists

D2Sh selective (presynaptic autoreceptors)

Allosteric modulators

  • PAOPA[11]
  • SB-269,652 - allosteric antagonist at dopamine D2 and D3 receptors[12]

Protein-protein interactions

The dopamine receptor D2 has been shown to interact with EPB41L1,[13] PPP1R9B[14] and NCS-1.[15]

Receptor oligomers

The D2 receptor forms heteromers with the following receptors: dopamine D1 (→ D1-D2),[16] D3,[17] 5-HT2A,[18] adenosine A2A,[19] CB1, mGlu5.

See also

References

Further reading

External links

  • Medical Subject Headings (MeSH)

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

This article was sourced from Creative Commons Attribution-ShareAlike License; additional terms may apply. World Heritage Encyclopedia content is assembled from numerous content providers, Open Access Publishing, and in compliance with The Fair Access to Science and Technology Research Act (FASTR), Wikimedia Foundation, Inc., Public Library of Science, The Encyclopedia of Life, Open Book Publishers (OBP), PubMed, U.S. National Library of Medicine, National Center for Biotechnology Information, U.S. National Library of Medicine, National Institutes of Health (NIH), U.S. Department of Health & Human Services, and USA.gov, which sources content from all federal, state, local, tribal, and territorial government publication portals (.gov, .mil, .edu). Funding for USA.gov and content contributors is made possible from the U.S. Congress, E-Government Act of 2002.
 
Crowd sourced content that is contributed to World Heritage Encyclopedia is peer reviewed and edited by our editorial staff to ensure quality scholarly research articles.
 
By using this site, you agree to the Terms of Use and Privacy Policy. World Heritage Encyclopedia™ is a registered trademark of the World Public Library Association, a non-profit organization.
 



Copyright © World Library Foundation. All rights reserved. eBooks from World eBook Library are sponsored by the World Library Foundation,
a 501c(4) Member's Support Non-Profit Organization, and is NOT affiliated with any governmental agency or department.