Dopaminski receptor D₅

Dopaminski receptor D5
Dopaminski receptor D5
Identifikatori
Simboli	DRD5; DBDR; DRD1B; DRD1L2
Vanjski ID	OMIM: 126453 MGI: 94927 HomoloGene: 20216 IUPHAR: D5 GeneCards: DRD5 Gene
Ontologija gena
Molekularna funkcija	• aktivnost dopaminskog receptora, Gs spregnutog; • vezivanje G-protein alfa podjedinice; • aktivnost transfera signala; • receptorska aktivnost; • aktivnost G-protein spregnutog receptora; • aktivnost dopaminskog receptora; • vezivanje leka; • vezivanje dopamina;
Celularna komponenta	• ćelijska membrana; • integralno sa ćelijskom membranom;
Biološki proces	• sinaptička transmisija, dopaminergička; • respons na amftamin; • regulacija sistemskog arterijskog krvnog pritiska vazopresinom; • norepinefrin-epinefrin vazokonstrikcija; • negativna regulacija aktivnosti proteinske kinaze; • homeostaza ćelijskih jona kalcijuma; • aktivacija adenilat ciklaze aktivnošću G-protein signalnog puta; • aktivacija adenilat ciklazne aktivnosti; • aktivacija adenilat ciklazne aktivnosti signalnim putem dopaminskog receptora; • sinaptička transmisija; • ponašanje parenja;
Pregled RNK izražavanja
	podaci
Ortolozi
Vrsta	Čovek
Entrez	1816
Ensembl	ENSG00000169676
UniProt	P21918
RefSeq (mRNA)	NM_000798.4
RefSeq (protein)	NP_000789.1
Lokacija (UCSC)	Chr 4:; 9.78 - 9.79 Mb
PubMed pretraga	[1]

D(1B) dopaminski receptor je protein koji je kod ljudi kodiran DRD5 genom.^[1]^[2]^[3]

Dopaminski D₅ podtip je G protein spregnuti receptor koji stimuliše adenilil ciklazu.^[4] Ovaj receptor je izražen u neuronima limbičkog regiona mozga. On ima 10-puta veći afinitet za dopamin nego D₁ podtip. Pseudogeni srodni sa ovim genom se nalaze na hromozomu 1 i hromozomu 2.^[2]

Ligandi уреди

D₁ i D₅ receptori su u znatnoj meri strukturno homologni i mali broj selektivnih liganda je dostupan. Postoje brojni ligandi koji su selektivni za D_1/5 u odnosu na druge dopaminske receptore. Nedavni razvoj selektivnog D₅ antagonista je omogućio ispitivanje D₁-posredovanog odgovora u odsustvu D₅ komponente. Selektivni D₅ agonisti trenutno nisu dostupni.

Agonist уреди

Dihidreksidin

Antagonist уреди

4-Hloro-7-metil-5,6,7,8,9,14-heksahidrodibenz[d,g]azecin-3-ol: antagonist, umerena selektivnost vezivanja u odnosu na D₁^[5]

Hemijska struktura D₅ selektivnog liganda 4-hloro-7-metil-5,6,7,8,9,14-heksahidrodibenz[d,g]azecin-3-ol.^[5]

Interakcije уреди

Za dopaminski receptor D5 je pokazano da interaguje sa GABRG2.^[6]

Reference уреди

^ Polymeropoulos MH, Xiao H, Merril CR (1992). „The human D5 dopamine receptor (DRD5) maps on chromosome 4”. Genomics. 11 (3): 777—778. PMID 1774076. doi:10.1016/0888-7543(91)90091-R.
^ ^а ^б „Entrez Gene: DRD5 dopamine receptor D5”.
^ Polymeropoulos MH, Xiao H, Merril CR (1991). „The human D₅ dopamine receptor (DRD5) maps on chromosome 4”. Genomics. 11 (3): 777—778. PMID 1774076. doi:10.1016/0888-7543(91)90091-R.
^ 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. PMID 9588624. doi:10.1007/BF02740640.
^ ^а ^б 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. PMID 16539400. doi:10.1021/jm051237e.
^ Liu, F; Wan Q; et al. (2000). „Direct protein-protein coupling enables cross-talk between dopamine D5 and gamma-aminobutyric acid A receptors”. Nature. England. 403 (6767): 274—280. ISSN 0028-0836. PMID 10659839. doi:10.1038/35002014.

Literatura уреди

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. PMID 1387108. doi:10.1016/0888-7543(92)90009-H.
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. PMID 1532789. doi:10.1016/0888-7543(92)90442-U.
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. PMID 1826762. doi:10.1038/350614a0.
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. PMC 52326  . PMID 1831904. doi:10.1073/pnas.88.17.7491.
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. PMC 52675  . PMID 1833775. doi:10.1073/pnas.88.20.9175.
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. PMID 7633397. doi:10.1093/hmg/4.4.507.
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. PMID 7727453. doi:10.1021/bi00017a025.
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. PMID 8288248. doi:10.1006/geno.1993.1489.
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. PMID 9603210. doi:10.1046/j.1471-4159.1998.70062459.x.
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. PMID 10391209. doi:10.1038/10290.
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. PMID 10659839. doi:10.1038/35002014.
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. PMC 139241  . PMID 12477932. doi:10.1073/pnas.242603899.
Hemby SE, Trojanowski JQ, Ginsberg SD (2003). „Neuron-specific age-related decreases in dopamine receptor subtype mRNAs”. J. Comp. Neurol. 456 (2): 176—183. PMID 12509874. doi:10.1002/cne.10525.
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. PMID 12623966. doi:10.1161/01.HYP.0000057422.75590.D7.

Vidi još уреди

Dopaminski receptor

Spoljašnje veze уреди

„Dopamine Receptors: D₁”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Архивирано из оригинала 31. 12. 2014. г.
DRD5+protein,+human на US National Library of Medicine Medical Subject Headings (MeSH)

[pmid1774076-1] Polymeropoulos MH, Xiao H, Merril CR (1992). „The human D5 dopamine receptor (DRD5) maps on chromosome 4”. Genomics. 11 (3): 777—778. PMID 1774076. doi:10.1016/0888-7543(91)90091-R.

[entrez-2] а ^б „Entrez Gene: DRD5 dopamine receptor D5”.

[autogenerated1-3] Polymeropoulos MH, Xiao H, Merril CR (1991). „The human D₅ dopamine receptor (DRD5) maps on chromosome 4”. Genomics. 11 (3): 777—778. PMID 1774076. doi:10.1016/0888-7543(91)90091-R.

[pmid9588624-4] 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. PMID 9588624. doi:10.1007/BF02740640.

[pmid16539400-5] а ^б 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. PMID 16539400. doi:10.1021/jm051237e.

[pmid10659839-6] Liu, F; Wan Q; et al. (2000). „Direct protein-protein coupling enables cross-talk between dopamine D5 and gamma-aminobutyric acid A receptors”. Nature. England. 403 (6767): 274—280. ISSN 0028-0836. PMID 10659839. doi:10.1038/35002014.

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Dopaminski receptor D5