Dopamine receptor D3
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- The correct title of this article is Dopamine receptor D3. It appears incorrectly here because of technical restrictions.
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Dopamine receptor D3
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| Identifiers | ||||||||||||||
| Symbol(s) | DRD3; D3DR; ETM1; FET1; MGC149204; MGC149205 | |||||||||||||
| External IDs | OMIM: 126451 MGI: 94925 HomoloGene: 623 | |||||||||||||
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| RNA expression pattern | ||||||||||||||
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| Orthologs | ||||||||||||||
| Human | Mouse | |||||||||||||
| Entrez | 1814 | 13490 | ||||||||||||
| Ensembl | ENSG00000151577 | ENSMUSG00000022705 | ||||||||||||
| Uniprot | P35462 | Q0VEC4 | ||||||||||||
| Refseq | NM_000796 (mRNA) NP_000787 (protein) |
NM_007877 (mRNA) NP_031903 (protein) |
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| Location | Chr 3: 115.33 - 115.38 Mb | Chr 16: 43.68 - 43.74 Mb | ||||||||||||
| Pubmed search | [1] | [2] | ||||||||||||
Dopamine receptor D3, also known as DRD3, is a human gene.[1]
This gene encodes the D3 subtype of the dopamine receptor. The D3 subtype inhibits adenylyl cyclase through inhibitory G-proteins. This receptor is expressed in phylogenetically older regions of the brain, suggesting that this receptor plays a role in cognitive and emotional functions. It is a target for drugs which treat schizophrenia, drug addiction, and Parkinson disease. Alternative splicing of this gene results in multiple transcript variants that would encode different isoforms, although some variants may be subject to nonsense-mediated decay (NMD).[1]
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[edit] Ligands
Numerous non-selective prescription drugs also bind to D3, but lack the strong receptor type and subtype selectivity that some of the following research compounds afford:
- (R)-3-(4-propylmorpholin-2-yl)phenol, an arylmorpholine, agonist, >1000-fold functional (efficiacy) selectivity over D2[2]
- 3-(4-chlorophenyl)-N-(4-(4-(2-fluorophenyl)piperazin-1-yl)butyl)acryl amide, full agonist, significant binding selectivity over D2[3]
- trans-N-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]cyclohexyl}-3-methoxybenzamide, full agonist, > 200-fold binding selectivity over D4, D2, 5-HT1A, and α1-receptors[4][5]
- (-)-7-{[2-(4-Phenylpiperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol[6]
- FAUC 346, partial agonist, subtype selective[7]
- FAUC 365, silent antagonist, subtype selective[7]
[edit] See also
[edit] References
- ^ a b Entrez Gene: DRD3 dopamine receptor D3.
- ^ Blagg J, Allerton CM, Batchelor DV, Baxter AD, Burring DJ, Carr CL, Cook AS, Nichols CL, Phipps J, Sanderson VG, Verrier H, Wong S (2007). "Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route". Bioorg. Med. Chem. Lett. 17 (24): 6691–6. doi:. PMID 17976986.
- ^ Saur O, Hackling AE, Perachon S, Schwartz JC, Sokoloff P, Stark H (2007). "N-(4-(4-(2-Halogenophenyl)piperazin-1-yl)butyl) substituted cinnamoyl amide derivatives as dopamine D2 and D3 receptor ligands". Arch. Pharm. (Weinheim) 340 (4): 178–84. doi:. PMID 17405129.
- ^ Leopoldo M, Lacivita E, Colabufo NA, Berardi F, Perrone R (2006). "Synthesis and binding profile of constrained analogues of N-[4-(4-arylpiperazin-1-yl)butyl]-3-methoxybenzamides, a class of potent dopamine D3 receptor ligands". J. Pharm. Pharmacol. 58 (2): 209–18. doi:. PMID 16451749.
- ^ van Vliet LA, Rodenhuis N, Dijkstra D, Wikström H, Pugsley TA, Serpa KA, Meltzer LT, Heffner TG, Wise LD, Lajiness ME, Huff RM, Svensson K, Sundell S, Lundmark M (2000). "Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-Tetrahydro-4-n-propyl-2H,5H-[1]benzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907)". J. Med. Chem. 43 (15): 2871–82. doi:. PMID 10956195.
- ^ Biswas S, Zhang S, Fernandez F, Ghosh B, Zhen J, Kuzhikandathil E, Reith ME, Dutta AK (2008). "Further structure-activity relationships study of hybrid 7-{[2-(4-phenylpiperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol analogues: identification of a high-affinity D3-preferring agonist with potent in vivo activity with long duration of action". J. Med. Chem. 51 (1): 101–17. doi:. PMID 18072730.
- ^ a b Bettinetti L, Schlotter K, Hübner H, Gmeiner P (2002). "Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists". J. Med. Chem. 45 (21): 4594–7. doi:. PMID 12361386.
[edit] 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.
- Sidhu A, Niznik HB (2000). "Coupling of dopamine receptor subtypes to multiple and diverse G proteins.". Int. J. Dev. Neurosci. 18 (7): 669–77. PMID 10978845.
- Le Coniat M, Sokoloff P, Hillion J, et al. (1991). "Chromosomal localization of the human D3 dopamine receptor gene.". Hum. Genet. 87 (5): 618–20. PMID 1916765.
- Sokoloff P, Giros B, Martres MP, et al. (1990). "Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.". Nature 347 (6289): 146–51. doi:. PMID 1975644.
- Giros B, Martres MP, Sokoloff P, Schwartz JC (1991). "[Gene cloning of human dopaminergic D3 receptor and identification of its chromosome]". C. R. Acad. Sci. III, Sci. Vie 311 (13): 501–8. PMID 2129115.
- Liu K, Bergson C, Levenson R, Schmauss C (1994). "On the origin of mRNA encoding the truncated dopamine D3-type receptor D3nf and detection of D3nf-like immunoreactivity in human brain.". J. Biol. Chem. 269 (46): 29220–6. PMID 7961889.
- Schmauss C, Haroutunian V, Davis KL, Davidson M (1993). "Selective loss of dopamine D3-type receptor mRNA expression in parietal and motor cortices of patients with chronic schizophrenia.". Proc. Natl. Acad. Sci. U.S.A. 90 (19): 8942–6. PMID 8415635.
- Griffon N, Crocq MA, Pilon C, et al. (1996). "Dopamine D3 receptor gene: organization, transcript variants, and polymorphism associated with schizophrenia.". Am. J. Med. Genet. 67 (1): 63–70. doi:. PMID 8678117.
- Staley JK, Mash DC (1996). "Adaptive increase in D3 dopamine receptors in the brain reward circuits of human cocaine fatalities.". J. Neurosci. 16 (19): 6100–6. PMID 8815892.
- Chen CH, Liu MY, Wei FC, et al. (1997). "Further evidence of no association between Ser9Gly polymorphism of dopamine D3 receptor gene and schizophrenia.". Am. J. Med. Genet. 74 (1): 40–3. PMID 9034004.
- Gulcher JR, Jónsson P, Kong A, et al. (1997). "Mapping of a familial essential tremor gene, FET1, to chromosome 3q13.". Nat. Genet. 17 (1): 84–7. doi:. PMID 9288103.
- Oldenhof J, Vickery R, Anafi M, et al. (1998). "SH3 binding domains in the dopamine D4 receptor.". Biochemistry 37 (45): 15726–36. doi:. PMID 9843378.
- Cargill M, Altshuler D, Ireland J, et al. (1999). "Characterization of single-nucleotide polymorphisms in coding regions of human genes.". Nat. Genet. 22 (3): 231–8. doi:. PMID 10391209.
- Pilla M, Perachon S, Sautel F, et al. (1999). "Selective inhibition of cocaine-seeking behaviour by a partial dopamine D3 receptor agonist.". Nature 400 (6742): 371–5. doi:. PMID 10432116.
- Ilani T, Ben-Shachar D, Strous RD, et al. (2001). "A peripheral marker for schizophrenia: Increased levels of D3 dopamine receptor mRNA in blood lymphocytes.". Proc. Natl. Acad. Sci. U.S.A. 98 (2): 625–8. doi:. PMID 11149951.
- Lin R, Karpa K, Kabbani N, et al. (2001). "Dopamine D2 and D3 receptors are linked to the actin cytoskeleton via interaction with filamin A.". Proc. Natl. Acad. Sci. U.S.A. 98 (9): 5258–63. doi:. PMID 11320256.
- Oldenhof J, Ray A, Vickery R, Van Tol HH (2001). "SH3 ligands in the dopamine D3 receptor.". Cell. Signal. 13 (6): 411–6. PMID 11384839.
- Soma M, Nakayama K, Rahmutula D, et al. (2002). "Ser9Gly polymorphism in the dopamine D3 receptor gene is not associated with essential hypertension in the Japanese.". Med. Sci. Monit. 8 (1): CR1–4. PMID 11796958.
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