Dopamine receptor D5

Dopamine receptor D5

Dopamine receptor D5
Identifiers
Symbols  ; DBDR; DRD1B; DRD1L2
External IDs IUPHAR: ChEMBL: GeneCards:
RNA expression pattern
Orthologs
Species Human Mouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)
RefSeq (protein)
Location (UCSC)
PubMed search

D(1B) dopamine receptor is a protein that in humans is encoded by the DRD5 gene.[1][2][1]

This gene encodes the D5 subtype of the dopamine receptor. The D5 subtype is a G-protein coupled receptor which stimulates adenylyl cyclase.[3] This receptor is expressed in neurons in the limbic regions of the brain. It has a 10-fold higher affinity for dopamine than the D1 subtype. Pseudogenes related to this gene reside on chromosome 1 and chromosome 2.[2]

Ligands

The D1 and D5 receptors have a high degree of structural homology and few ligands are available that can distinguish between them as yet, however there are a number of ligands that are selective for D1/5 over the other dopamine receptors. The recent development of a selective D5 antagonist has allowed the action of D1-mediated responses to be studied in the absence of a D5 component, but no selective D5 agonists are yet available.

Agonists

Dihydrexidine

Antagonists

  • 4-Chloro-7-methyl-5,6,7,8,9,14-hexahydrodibenz[d,g]azecin-3-ol: antagonist, moderate binding selectivity over D1[4]
Chemical structure of a D5-preferring ligand 4-chloro-7-methyl-5,6,7,8,9,14-hexahydrodibenz[d,g]azecin-3-ol.[4]


Interactions

Dopamine receptor D5 has been shown to interact with GABRG2.[5]

See also

References

  1. ^ a b Polymeropoulos MH, Xiao H, Merril CR (Mar 1992). "The human D5 dopamine receptor (DRD5) maps on chromosome 4". Genomics 11 (3): 777–778.  
  2. ^ a b "Entrez Gene: DRD5 dopamine receptor D5". 
  3. ^ Sidhu A (1998). "Coupling of D1 and D5 dopamine receptors to multiple G proteins: Implications for understanding the diversity in receptor-G protein coupling". Mol. Neurobiol. 16 (2): 125–134.  
  4. ^ a b Mohr P, Decker M, Enzensperger C, Lehmann J (2006). "Dopamine/serotonin receptor ligands. 12(1): SAR studies on hexahydro-dibenz[d,g]azecines lead to 4-chloro-7-methyl-5,6,7,8,9,14-hexahydrodibenz[d,g]azecin-3-ol, the first picomolar D5-selective dopamine-receptor antagonist". J. Med. Chem. 49 (6): 2110–2116.  
  5. ^ Liu F, Wan Q, Pristupa ZB, Yu XM, Wang YT, Niznik HB (2000). "Direct protein-protein coupling enables cross-talk between dopamine D5 and gamma-aminobutyric acid A receptors". Nature 403 (6767): 274–80.  

Further reading

External links

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