Dopamine receptor D5

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Dopamine receptor D5
Identifiers
Symbols DRD5 ; DBDR; DRD1B; DRD1L2
External IDs OMIM126453 MGI94927 HomoloGene20216 IUPHAR: D5 ChEMBL: 1850 GeneCards: DRD5 Gene
RNA expression pattern
PBB GE DRD5 208486 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 1816 13492
Ensembl ENSG00000169676 ENSMUSG00000039358
UniProt P21918 Q8BLD9
RefSeq (mRNA) NM_000798 NM_013503
RefSeq (protein) NP_000789 NP_038531
Location (UCSC) Chr 4:
9.78 – 9.79 Mb
Chr 5:
38.32 – 38.32 Mb
PubMed search [1] [2]

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[edit]

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[edit]

Dihydrexidine

Antagonists[edit]

  • 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[edit]

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

See also[edit]

References[edit]

  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. doi:10.1016/0888-7543(91)90091-R. PMID 1774076. 
  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. doi:10.1007/BF02740640. PMID 9588624. 
  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. doi:10.1021/jm051237e. PMID 16539400. 
  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. doi:10.1038/35002014. PMID 10659839. 

Further reading[edit]

External links[edit]

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