Dopamine receptor: Difference between revisions
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<StructureSection load=' | <StructureSection load='' size='350' side='right' scene='47/475982/Cv/1' caption='Structure of the human dopamine D3 receptor in complex with the antagonist eticlopride and maltose, [[3pbl]]'> | ||
==Introduction== | ==Introduction== | ||
'''Dopamine receptors''' are a class of metabotropic G protein-coupled receptors that are important in the central nervous system. Dopamine receptors are involved in many neurological processes that comprise motivation, pleasure, cognition, memory, learning, and fine motor skills. There are five subtype dopamine receptors, D1, D2, D3, D4, and D5. The D3 receptor is a part of the D2-like family.<ref>PMID:15148138</ref> | '''Dopamine receptors''' are a class of metabotropic G protein-coupled receptors that are important in the central nervous system. Dopamine receptors are involved in many neurological processes that comprise motivation, pleasure, cognition, memory, learning, and fine motor skills. There are five subtype dopamine receptors, D1, D2, D3, D4, and D5.<br /> | ||
* '''dopamine receptor D1''' influences renal sodium transport and vascular hemodynamics<ref>PMID: 1916765</ref>.<br /> | |||
* '''dopamine receptor D2''' reduces the activation of dopamine receptor 1 on neurons<ref>PMID: 16055058</ref>.<br /> | |||
* '''dopamine receptor D3''' plays a role in endocytic sorting. <ref>PMID: 22802617</ref>. The D3 receptor is a part of the D2-like family.<ref>PMID:15148138</ref><br /> | |||
* '''dopamine receptor D4''' mediates the effects of dopamine<ref>PMID: 31149768</ref>.<br /> | |||
For additional details see [[Dopamine Receptors]]. | |||
See also: | |||
* [[G protein-coupled receptor]] | |||
*[[Receptor]] | |||
*[[Transmembrane (cell surface) receptors]] | |||
*[[Aripiprazole]] | |||
==Function== | ==Function== | ||
Human dopamine D3 receptor is a protein that is encoded by the dopamine receptor gene (DRD3).<ref>PMID: 1916765</ref> The DRD3 gene codes for the D3 dopamine receptor that inhibits adenylyl cyclase through inhibitory G-proteins. G-protein coupled receptors are a family of transmembrane proteins that transmit chemical signals from outside the cell to cause changes inside of the cell. Adenylate cyclase is part of the G-protein receptor's signaling and catalyze the conversion of ATP to cyclic AMP (cAMP).<ref>Reece, Jane; Campbell, Neil (2002). Biology. San Francisco: Benjamin Cummings. ISBN 0-8053-6624-5.</ref> The D3 receptor is located in the brain, suggesting that it plays a role in cognitive and emotional functions.<ref>National Center for Biotechnology Information, U.S. National Library of Medicine. DRD3 dopamine receptor D3 [Homo sapiens]. 19 November 2011.</ref> The human dopamine D3 receptor is membrane-bound and scattered in the cytoplasm. Receptor stimulation causes internalization of the receptors at the perinuclear areas. This is followed by the spreading of the receptors to the membrane. DRD3 is also contained in lipid rafts of renal proximal tubule cells.<ref>PMID: 19520868</ref> | Human dopamine D3 receptor is a protein that is encoded by the dopamine receptor gene (DRD3).<ref>PMID: 1916765</ref> The DRD3 gene codes for the D3 dopamine receptor that inhibits adenylyl cyclase through inhibitory G-proteins. G-protein coupled receptors are a family of transmembrane proteins that transmit chemical signals from outside the cell to cause changes inside of the cell. Adenylate cyclase is part of the G-protein receptor's signaling and catalyze the conversion of ATP to cyclic AMP (cAMP).<ref>Reece, Jane; Campbell, Neil (2002). Biology. San Francisco: Benjamin Cummings. ISBN 0-8053-6624-5.</ref> The D3 receptor is located in the brain, suggesting that it plays a role in cognitive and emotional functions.<ref>National Center for Biotechnology Information, U.S. National Library of Medicine. DRD3 dopamine receptor D3 [Homo sapiens]. 19 November 2011.</ref> The human dopamine D3 receptor is membrane-bound and scattered in the cytoplasm. Receptor stimulation causes internalization of the receptors at the perinuclear areas. This is followed by the spreading of the receptors to the membrane. DRD3 is also contained in lipid rafts of renal proximal tubule cells.<ref>PMID: 19520868</ref> | ||
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*Clebopride<ref>Cuena Boy R, Maciá Martínez MA (1998). "[Extrapyramidal toxicity caused by metoclopramide and clebopride: study of voluntary notifications of adverse effects to the Spanish Drug Surveillance System]" (in Spanish). Atencion Primaria 21 (5): 289–95. PMID 9608114. Free full text</ref> | *Clebopride<ref>Cuena Boy R, Maciá Martínez MA (1998). "[Extrapyramidal toxicity caused by metoclopramide and clebopride: study of voluntary notifications of adverse effects to the Spanish Drug Surveillance System]" (in Spanish). Atencion Primaria 21 (5): 289–95. PMID 9608114. Free full text</ref> | ||
*Nafadotride<ref>Pilla M, Perachon S, Sautel F, Garrido F, Mann A, Wermuth CG, Schwartz JC, Everitt BJ, Sokoloff P. Selective inhibition of cocaine-seeking behaviour by a partial dopamine D3 agonist. Nature. 1999;400:371–375.</ref> | *Nafadotride<ref>Pilla M, Perachon S, Sautel F, Garrido F, Mann A, Wermuth CG, Schwartz JC, Everitt BJ, Sokoloff P. Selective inhibition of cocaine-seeking behaviour by a partial dopamine D3 agonist. Nature. 1999;400:371–375.</ref> | ||
Two ligands that are associated with the dopamine D3 receptor are 3-chloro-5-ethyl-N{[(2S)-1-ethylpyrrolidin-2-yl]methyl}-6-hydroxyl-2-methyloxybenzamide <scene name='47/475982/Cv/ | Two ligands that are associated with the dopamine D3 receptor are 3-chloro-5-ethyl-N{[(2S)-1-ethylpyrrolidin-2-yl]methyl}-6-hydroxyl-2-methyloxybenzamide <scene name='47/475982/Cv/5'>(eticlopride, ETQ)</scene> and <scene name='47/475982/Cv/6'>maltose</scene> (MAL). ETQ binds to dopamine D3 receptor by Asp 110 and Phe346. MAL binds by Asp 1020, Glu 1022, Glu1011, and Leu1032. Of note, this structure ([[3pbl]]) is chimeric between dopamine D3 receptor and Lysozyme, MAL binds only to Lysozyme part of this chimera. <ref name="structure" /> <scene name='47/475982/Cv/7'>So, MAL cannot be the real ligand of dopamine D3 receptor</scene>. | ||
==Diseases== | ==Diseases== | ||
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ETM1 is the most common movement disorder involving postural tremor of the arms, head, legs, body core, voice, jaw, and other facial muscles. | ETM1 is the most common movement disorder involving postural tremor of the arms, head, legs, body core, voice, jaw, and other facial muscles. | ||
This condition can be provoked by emotions, hunger, fatigue, and temperature extremes.<ref name="disease" /> | This condition can be provoked by emotions, hunger, fatigue, and temperature extremes.<ref name="disease" /> | ||
==3D structures of dopamine receptor== | ==3D structures of dopamine receptor== | ||
[[ | [[Dopamine receptor 3D structures]] | ||
==References== | ==References== | ||
<references /> | <references /> | ||
[[Category:Topic Page]] | |||