Dopamine receptor D5

Dopamine receptor D5
Identifiers
Symbols	DRD5; DBDR; DRD1B; DRD1L2; MGC10601
External IDs	OMIM: 126453 MGI: 94927 HomoloGene: 20216 IUPHAR: D5 GeneCards: DRD5 Gene
Gene Ontology Molecular function • dopamine receptor activity, coupled via Gs • dopamine D5 receptor activity • G-protein alpha-subunit binding • receptor activity • G-protein coupled receptor activity • dopamine receptor activity • drug binding • dopamine binding Cellular component • plasma membrane • plasma membrane • plasma membrane • integral to plasma membrane • integral to plasma membrane • brush border membrane Biological process • synaptic transmission, dopaminergic • response to amphetamine • regulation of systemic arterial blood pressure by vasopressin • norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressure • negative regulation of protein kinase activity • cellular calcium ion homeostasis • activation of adenylate cyclase activity by G-protein signaling pathway • activation of adenylate cyclase activity • activation of adenylate cyclase activity by dopamine receptor signaling pathway • synaptic transmission • mating behavior • visual learning • negative regulation of cell migration • positive regulation of cAMP biosynthetic process • negative regulation of NAD(P)H oxidase activity • wound healing • response to cocaine • positive regulation of adenylate cyclase activity • positive regulation of adenylate cyclase activity • negative regulation of blood pressure • regulation of female receptivity • sensitization • regulation of long-term neuronal synaptic plasticity • activation of phospholipase C activity by dopamine receptor signaling pathway • long term synaptic depression • reactive oxygen species metabolic process Sources: Amigo / QuickGO
RNA expression pattern
More reference expression data
Orthologs
Species	Human	Mouse
Entrez	1816	13492
Ensembl	ENSG00000169676	ENSMUSG00000039358
UniProt	P21918	Q8BLD9
RefSeq (mRNA)	NM_000798	NM_013503.2
RefSeq (protein)	NP_000789	NP_038531.1
Location (UCSC)	Chr 4: 9.78 – 9.79 Mb	Chr 5: 38.71 – 38.71 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

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 D_1/5 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

• Dopamine receptor

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. doi:10.1016/0888-7543(91)90091-R. PMID 1774076. 
2. ^ ^{a b} "Entrez Gene: DRD5 dopamine receptor D5". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=1816. 
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 Z B, Yu X M, Wang Y T, Niznik H B (Jan. 2000). "Direct protein-protein coupling enables cross-talk between dopamine D5 and gamma-aminobutyric acid A receptors". Nature (ENGLAND) 403 (6767): 274–280. doi:10.1038/35002014. ISSN 0028-0836. PMID 10659839. 

Further reading

• Missale C, Nash SR, Robinson SW et al. (1998). "Dopamine receptors: from structure to function". Physiol. Rev. 78 (1): 189–225. PMID 9457173. 
• Grandy DK, Allen LJ, Zhang Y et al. (1992). "Chromosomal localization of three human D5 dopamine receptor genes". Genomics 13 (4): 968–973. doi:10.1016/0888-7543(92)90009-H. PMID 1387108. 
• Eubanks JH, Altherr M, Wagner-McPherson C et al. (1992). "Localization of the D5 dopamine receptor gene to human chromosome 4p15.1-p15.3, centromeric to the Huntington's disease locus". Genomics 12 (3): 510–516. doi:10.1016/0888-7543(92)90442-U. PMID 1532789. 
• Sunahara RK, Guan HC, O'Dowd BF et al. (1991). "Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1". Nature 350 (6319): 614–619. doi:10.1038/350614a0. PMID 1826762. 
• Tiberi M, Jarvie KR, Silvia C et al. (1991). "Cloning, molecular characterization, and chromosomal assignment of a gene encoding a second D1 dopamine receptor subtype: differential expression pattern in rat brain compared with the D1A receptor". Proc. Natl. Acad. Sci. U.S.A. 88 (17): 7491–7495. doi:10.1073/pnas.88.17.7491. PMC 52326. PMID 1831904. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=52326. 
• Grandy DK, Zhang YA, Bouvier C et al. (1991). "Multiple human D5 dopamine receptor genes: a functional receptor and two pseudogenes". Proc. Natl. Acad. Sci. U.S.A. 88 (20): 9175–9179. doi:10.1073/pnas.88.20.9175. PMC 52675. PMID 1833775. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=52675. 
• Weinshank RL, Adham N, Macchi M et al. (1991). "Molecular cloning and characterization of a high affinity dopamine receptor (D1 beta) and its pseudogene". J. Biol. Chem. 266 (33): 22427–35. PMID 1834671. 
• Sobell JL, Lind TJ, Sigurdson DC et al. (1995). "The D5 dopamine receptor gene in schizophrenia: identification of a nonsense change and multiple missense changes but lack of association with disease". Hum. Mol. Genet. 4 (4): 507–514. doi:10.1093/hmg/4.4.507. PMID 7633397. 
• Beischlag TV, Marchese A, Meador-Woodruff JH et al. (1995). "The human dopamine D5 receptor gene: cloning and characterization of the 5'-flanking and promoter region". Biochemistry 34 (17): 5960–5970. doi:10.1021/bi00017a025. PMID 7727453. 
• Sherrington R, Mankoo B, Attwood J et al. (1994). "Cloning of the human dopamine D5 receptor gene and identification of a highly polymorphic microsatellite for the DRD5 locus that shows tight linkage to the chromosome 4p reference marker RAF1P1". Genomics 18 (2): 423–425. doi:10.1006/geno.1993.1489. PMID 8288248. 
• Sidhu A, Kimura K, Uh M et al. (1998). "Multiple coupling of human D5 dopamine receptors to guanine nucleotide binding proteins Gs and Gz". J. Neurochem. 70 (6): 2459–2467. doi:10.1046/j.1471-4159.1998.70062459.x. PMID 9603210. 
• Cargill M, Altshuler D, Ireland J et al. (1999). "Characterization of single-nucleotide polymorphisms in coding regions of human genes". Nat. Genet. 22 (3): 231–238. doi:10.1038/10290. PMID 10391209. 
• Liu F, Wan Q, Pristupa ZB et al. (2000). "Direct protein-protein coupling enables cross-talk between dopamine D5 and gamma-aminobutyric acid A receptors". Nature 403 (6767): 274–280. doi:10.1038/35002014. PMID 10659839. 
• Misbahuddin A, Placzek MR, Chaudhuri KR et al. (2004). "A polymorphism in the dopamine receptor DRD5 is associated with blepharospasm". Neurology 58 (1): 124–6. PMID 11781417. 
• Kabbani N, Negyessy L, Lin R et al. (2002). "Interaction with neuronal calcium sensor NCS-1 mediates desensitization of the D2 dopamine receptor". J. Neurosci. 22 (19): 8476–86. PMID 12351722. 
• Strausberg RL, Feingold EA, Grouse LH et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–16903. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=139241. 
• Hemby SE, Trojanowski JQ, Ginsberg SD (2003). "Neuron-specific age-related decreases in dopamine receptor subtype mRNAs". J. Comp. Neurol. 456 (2): 176–183. doi:10.1002/cne.10525. PMID 12509874. 
• Zheng S, Yu P, Zeng C et al. (2003). "Galpha12- and Galpha13-protein subunit linkage of D5 dopamine receptors in the nephron". Hypertension 41 (3): 604–610. doi:10.1161/01.HYP.0000057422.75590.D7. PMID 12623966. 

External links

• "Dopamine Receptors: D₁". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2260. 
• MeSH DRD5+protein,+human

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

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