Dopamine receptor D3: Difference between revisions
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Revision as of 14:19, 4 December 2008
Template:PBB 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's 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]
Ligands
Numerous non-selective prescription drugs bind to the D3 receptor, notably including some of the newer dopamine agonists used for Parkinson's disease such as pramipexole and ropinirole, but these also bind to D2 and lack the strong receptor type and subtype selectivity that some of the following research compounds afford:
Agonists
- (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]
Antagonists
- Nafadotride
- FAUC 365, silent antagonist, subtype selective[7]
- SB-277011-A, selective D3 antagonist, 80x selectivity over D2 with no partial agonist effects, used in drug addiction research as a potential therapy for addiction to several different drugs
See also
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:10.1016/j.bmcl.2007.10.059. PMID 17976986.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ 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:10.1002/ardp.200600196. PMID 17405129.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ 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:10.1211/jpp.58.2.0008. PMID 16451749.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ 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:10.1021/jm0000113. PMID 10956195.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ 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:10.1021/jm070860r. PMID 18072730.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ 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:10.1021/jm025558r. PMID 12361386.
{{cite journal}}: CS1 maint: multiple names: authors list (link)
Further reading
External links
- "Dopamine Receptors: D3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
{{cite web}}: Cite has empty unknown parameter:|coauthors=(help) - Receptors,+Dopamine+D3 at the U.S. National Library of Medicine Medical Subject Headings (MeSH)
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