The D3 Dopamine Receptor: Neurobiology and Potential Clinical Relevance
Pharmacological ReviewsPublished 1 September 1997
Beth Levant
Citations388
SJR quartileQ1
SJR score6.60
SNIP4.90
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TL;DR
Receptors for this catecholamine are of considerable interest, as they are the principal target of drugs employed in the treatment of neuropsychiatric disorders such as schizophrenia and Parkinson’s disease.
Abstract
Dopamine is a major neurotransmitter in the central nervous system. Receptors for this catecholamine are of considerable interest, as they are the principal target of drugs employed in the treatment of neuropsychiatric disorders such as schizophrenia and Parkinson’s disease. Before 1990, the
Keywords
MedicineNeuroscience
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860 Citations1991Marie-Louise Bouthenet, Evelyne Souil +4 more
D2 and D3 receptor mRNAs were also detected at the level of the substantia nigra, suggesting that these receptors function as both autoreceptor and postsynaptic receptors, the latter being most abundant in dopaminergic areas known to be associated with cognitive and emotional functions.
NatureAlternative splicing directs the expression of two D2 dopamine receptor isoforms
686 Citations1989Bruno Giros, Pierre Sokoloff +4 more
It is shown that the gene for the D2 receptor produces two receptor isoforms by alternative messenger RNA splicing, providing a route to receptor diversity in this family of receptors.
Proceedings of the National Academy of SciencesIdentification, characterization, and localization of the dopamine D3 receptor in rat brain using 7-[3H]hydroxy-N,N-di-n-propyl-2-aminotetralin.
679 Citations1992Daniel Lévesque, Jorge Díaz +8 more
Native D3 receptors in brain are characterized by an unusually high nanomolar affinity for dopamine and a low modulatory influence of guanyl nucleotides on agonist binding, which suggest that D3 receptor are involved in a peculiar mode of neurotransmission in a restricted subpopulation of dopamine neurons.
NatureMolecular cloning and expression of the gene for a human D1 dopamine receptor
675 Citations1990Alien Dearry, Jay A. Gingrich +4 more
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NatureDopamine D4 receptors elevated in schizophrenia
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The EMBO JournalThe dopamine D2 receptor: two molecular forms generated by alternative splicing.
605 Citations1989Roberto Dal Toso, Bernd Sommer +6 more
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NatureCloning and expression of human and rat Dt dopamine receptors
564 Citations1990Qun-Yong Zhou, David K. Grandy +8 more
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Proceedings of the National Academy of SciencesA targeted mutation of the D3 dopamine receptor gene is associated with hyperactivity in mice.
466 Citations1996Domenico Accili, C. Simone Fishburn +11 more
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Proceedings of the National Academy of SciencesMolecular cloning and expression of a D1 dopamine receptor linked to adenylyl cyclase activation.
457 Citations1990Frederick J. Monsma, L C Mahan +3 more
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ScienceModulation of Cocaine Self-Administration in the Rat Through D-3 Dopamine Receptors
455 Citations1993S. Barak Caine, George F. Koob
Three dopamine receptor agonists had affinities for binding to the D-3 receptor that correlated highly with their relative potencies in decreasing cocaine self-administration in the rat at doses that were not by themselves reinforcing.
NeuroscienceAnatomical and affinity state comparisons between dopamine D1 and D2 receptors in the rat central nervous system
448 Citations1989Eric K. Richfield, John B. Penney +1 more
The anatomical distributions and affinity states of dopamine D1 and D2 receptors were compared in the rat central nervous system using quantitative autoradiography to provide an anatomical framework for evaluating behavioral and electrophysiological evidence of an interaction between the two dopamine receptor subtypes.
European Journal of Pharmacology Molecular PharmacologyPharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor
404 Citations1992Pierre Sokoloff, M Andrieux +5 more
Several agonists and antagonists, previously regarded as autoreceptor-selective, displayed higher affinities at D3 than at D2 receptors, suggesting that they realize differential dopamine receptor subtype occupancy during treatments and that this might be reflected in their clinical profile.
NeurosciencePhenotypical characterization of neurons expressing the dopamine D3 receptor in the rat brain
349 Citations1995Jorge Díaz, Daniel Lévesque +5 more
The occurrence of D3 receptor gene expression in some brain areas receiving low dopamine innervation supports the hypothesis that this receptor may mediate non-synaptic actions of dopamine.
Proceedings of the National Academy of SciencesLocalization of dopamine D3 receptors to mesolimbic and D2 receptors to mesostriatal regions of human forebrain.
327 Citations1994Anne M. Murray, H. Ryoo +2 more
Binding of [125I]epidepride to D3-like receptors was negligible in the dorsal striatum but was concentrated in islands of dense binding in the nucleus accumbens and ventral putamen that aligned with acetylcholinesterase-poor striosomes.
Trends in Pharmacological SciencesMechanisms of signal transduction at the dopamine D2 receptor
313 Citations1989Lucia Vallar, Jacopo Meldolesi
A spectrum of intracellular signals is analyzed which might be sufficient to sustain inhibition of secretion in pituitary lactotroph cells and possibly the other effects of D2 receptors in other cell systems.
Journal of NeuroscienceAdaptive Increase in D<sub>3</sub>Dopamine Receptors in the Brain Reward Circuits of Human Cocaine Fatalities
312 Citations1996Julie K. Staley, Deborah C. Mash
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Journal of Medical GeneticsAssociation between schizophrenia and homozygosity at the dopamine D3 receptor gene.
281 Citations1992M.A. Crocq, R. Mant +8 more
Data is reported from two independent studies of a BalI polymorphism in the dopamine D3 receptor gene in patients with schizophrenia that more patients than controls were homozygous, and this difference was highly significant.
Journal of Neural TransmissionThe dopamine D3-receptor: A postsynaptic receptor inhibitory on rat locomotor activity
256 Citations1993Nicholas Waters, Kjell Svensson +3 more
It is suggested that U 99194 A can antagonise a population of postsynaptic dopamine receptors involved in the suppression of some aspects of psychomotor activity that belong to the D 3 receptor subtype.
European Journal of Pharmacology Molecular PharmacologyPramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors
254 Citations1995Joachim Mierau, Franz J. Schneider +4 more
The dopamine D3 receptor selectivity of pramipexole may explain the previously described properties of this drug, including its potent autoreceptor preference, while quinpirole and bromocriptine are non-selective or more D2/D4 receptor selective.
International review of neurobiologyMolecular Neurobiology of Dopaminergic Receptors
254 Citations1993David R. Sibley, Frederick J. Monsma +1 more
There is extensive evidence that "D1-like" dopamine receptors exist which are linked to the activation of phospholipase C, phosphatidylinositol turnover, and Ca2+ mobilization and might define a third distinct subfamily of dopamine receptors.
Molecular PharmacologyActivation of heterologously expressed D3 dopamine receptors: comparison with D2 dopamine receptors.
253 Citations1994Chris L. Chio, Mary E. Lajiness +1 more
Comparison of the potencies at the two receptors reveals that none of the agonists is as selective for D3 receptors as was previously thought based on radioligand binding data.
Neurochemistry InternationalDopamine receptors in brain and periphery
250 Citations1987Philip Seeman, Dimitri E. Grigoriadis
It is currently necessary to postulate only two receptors D(1) and D(2) to account for the majority of available data, and some of this information is reviewed.
Psychiatric GeneticsAmino acid substitution in the dopamine D3 receptor as a useful polymorphism for investigating psychiatric disorders
238 Citations1992L. Lannfelt, Pierre Sokoloff +6 more
A point mutation in the gene that creates a Ball restriction enzyme site and leads to a substitution of a Serine by a Glycine residue in the 5′ part of the receptor gene is detected.
Biochemical and Biophysical Research CommunicationsProposed Schizophrenia-Related Gene Polymorphism: Expression of the Ser9Gly Mutant Human Dopamine D3Receptor with the Semliki Forest Virus System
231 Citations1996Kenneth Lundström, Michael P. Turpin
Journal of Pharmacology and Experimental TherapeuticsExpression and pharmacological characterization of the human D3 dopamine receptor.
224 Citations1994Stephen B. Freedman, Shil Patel +5 more
The finding that a wide range of structurally diverse human dopamine D2 (hD2) receptor agonists have an apparent hD3 selectivity may imply that the hD 3 receptor exists predominantly in a high affinity state.
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Journal of Neural TransmissionAutoradiographic localization of dopamine D1 and D2 receptors in the brain of several mammalian species
212 Citations1990Montserrat Camps, Peter H. Kelly +1 more
The results indicate that dopamine receptor distribution is well preserved in the basal ganglia during evolution, although differences among species exist in their distribution outside the basal Ganglia and their absolute amount.
Molecular PharmacologyUnique binding characteristics of antipsychotic agents interacting with human dopamine D2A, D2B, and D3 receptors.
212 Citations1993Åsa Malmberg, D M Jackson +2 more
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Journal of Pharmacology and Experimental TherapeuticsNeurochemical and functional characterization of the preferentially selective dopamine D3 agonist PD 128907.
201 Citations1995Thomas A. Pugsley, M. Duff Davis +8 more
Findings indicating that PD 128907 shows a preference for DA D3 over D2L and D4.2 receptors indicates that its action at low doses may be due to interaction with D3 receptors and at higher doses, with both D2 and D 3 receptors.
Journal of Pharmacology and Experimental TherapeuticsPharmacological and functional characterization of D2, D3 and D4 dopamine receptors in fibroblast and dopaminergic cell lines.
200 Citations1994Lei‐Han Tang, R.D. Todd +2 more
Data imply that the D2 receptor couples to the G alpha i2 subtype in both cell lines, whereas D4 does not.(ABSTRACT TRUNCATED AT 250 WORDS)
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Findings provide further support for the hypothesis that the direction of modulatory action of DA is determined by the specific subtype of EAA receptor activated.
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189 Citations1993G. Bernhard Landwehrmeyer, Guadalupe Mengod +1 more
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NeuropharmacologyBehavioural effects of the putative D-3 dopamine receptor agonist 7-OH-DPAT in relation to other “D-2-like” agonists
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Proceedings of the National Academy of SciencesA paradoxical regulation of the dopamine D3 receptor expression suggests the involvement of an anterograde factor from dopamine neurons.
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It is proposed that an anterograde factor present in mesolimbic dopaminergic neurons, but distinct from dopamine and known peptide cotransmitters, plays a positive role on transcription of the D3 receptor gene.
American Journal of Medical GeneticsRelationship between homozygosity at the dopamine D3 receptor gene and schizophrenia
181 Citations1994R. Mant, Julie Williams +4 more
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European Journal of NeuroscienceDifferential Visualization of Dopamine D2 and D3 Receptor Sites in Rat Brain. A Comparative Study Using <i>In Situ</i> Hybridization Histochemistry and Ligand Binding Autoradiography
177 Citations1993G. Bernhard Landwehrmeyer, Guadalupe Mengod +1 more
The expression of D3 binding sites in the rat brain is demonstrated and a procedure to differentiate D2 and D3 receptor populations in binding studies is provided.
Proceedings of the National Academy of SciencesSelective loss of dopamine D3-type receptor mRNA expression in parietal and motor cortices of patients with chronic schizophrenia.
165 Citations1993Claudia Schmauss, Vahram Haroutunian +2 more
Many variables associated with either the course and/or the therapeutic management of the disease may account for the selective loss of D3 mRNA in the motor, somatoensory, and somatosensory association areas of schizophrenic brains.
Journal of Pharmacology and Experimental TherapeuticsNafadotride, a potent preferential dopamine D3 receptor antagonist, activates locomotion in rodents.
164 Citations1995François Sautel, Nathalie Griffon +8 more
These studies establish nafadotride as a pure, extremely potent, competitive and preferential dopamine D3 receptor antagonist in vitro.
NeuropsychopharmacologyDopamine Receptor Gene Expression in the Human Medial Temporal Lobe
159 Citations1994James H. Meador‐Woodruff, David K. Grandy +5 more
The results provide a description of the distribution of these receptor mRNAs in normal humans and suggest multiple levels of complexity as well as regulation of the medial temporal lobe dopamine projection.
The Journal of Comparative NeurologyDopamine receptor mRNA expression patterns by opioid peptide cells in the nucleus accumbens of the rat: A double in situ hybridization study
151 Citations1995Eileen Curran, Stanley J. Watson
Colocalization of proenkephalin and prodynorphin mRNAs with each other as well as with D1, D2, and D3 dopamine receptor m RNAs was analyzed in the nucleus accumbens of the rat.
Journal of Pharmacology and Experimental TherapeuticsDopamine D2 and D3 receptors inhibit dopamine release.
147 Citations1994Lei Tang, R.D. Todd +1 more
This is the first report of a functional role for D3 receptors and establishes these cell lines as a convenient in vitro model system to study signal transduction mechanisms associated with autoreceptor function.
Human GeneticsAllelic association between a Ser-9-Gly polymorphism in the dopamine D3 receptor gene and schizophrenia
145 Citations1996Saleem Shaikh, Dami A. Collier +7 more
The results suggest that the Ser-9 allele, or a nearby polymorphism in linkage disequilibrium, results in a small increase in susceptibility to schizophrenia.
NeurologyDecrease of the D3 dopamine receptor mRNA expression in lymphocytes from patients with Parkinson's disease
145 Citations1996Yoshitaka Nagai, S. Ueno +4 more
There was a statistically significant decrease of the D3 dopamine receptor (D3R) mRNA expression in PD patients compared with that in controls and the decrease correlated with the degree of clinical severity inPD patients.
European Journal of PharmacologyBehavioral and neurochemical data suggest functional differences between dopamine D2 and D3 receptors
140 Citations1994Kjell Svensson, Arvid Carlsson +3 more
The hypothesis that the functional dopamine D3 receptor is a postsynaptic receptor inhibitory on rat locomotion is supported and the present data support the hypothesis.
Journal of NeurochemistryComplete Conversion of Brain D<sub>2</sub> Dopamine Receptors from the High‐ to the Low‐Affinity State for Dopamine Agonists, Using Sodium Ions and Guanine Nucleotide
140 Citations1985Dimitri E. Grigoriadis, Philip Seeman
It is concluded that it is possible to convert brain D2 dopamine receptors completely into their low‐affinity state, in the presence of NaCl and a guanine nucleotide, providing that appropriate allowance is made for the serotonergic component of [3H]spiperone binding.
Brain ResearchDopamine receptor distribution in the rat CNS: elucidation using anti-peptide antisera directed against D1A and D3 subtypes
135 Citations1994Marjorie A. Ariano, David R. Sibley
Results localizing cellular D2-like receptor expression patterns in this projection system of the rat neostriatum implies that all three of these dopamine receptor subtypes may be co-expressed in this efferent system.
Biochemical and Biophysical Research CommunicationsShorter variants of the D3 dopamine receptor produced through various patterns of alternative splicing
135 Citations1991Bruno Giros, Marie‐Pascale Martres +3 more
Using Polymerase Chain Reaction amplification of mRNAs from several areas of rat brain, the occurrence of two shorter transcripts of the dopamine D3 receptor gene are shown, in addition to that corresponding to the D3 receptors, to result from different processes of alternative splicing.
European Journal of PharmacologyPharmacological aspects of R-( + )-7-OH-DPAT, a putative dopamine D3 receptor ligand
135 Citations1993G. Damsma, Tjibbe Bottema +7 more
In rats R-(+)-7-OH-DPAT dose dependently decreased dopamine release and induced yawning, while sniffing behaviour occurred at the highest dose tested (1000 nmol/kg), suggesting the possibility that the inhibition of dopamineRelease and the elicitation of yawning are mediated by dopamine D3 receptors.
Journal of Neural TransmissionLocomotor inhibition by the D3 ligand R-(+)-7-OH-DPAT is independent of changes in dopamine release
132 Citations1994Kjell Svensson, Arvid Carlsson +1 more
The hypothesis that the dopamine D3 receptor is a postsynaptic receptor with an inhibitory influence on rat locomotor activity is supported.
Journal of Pharmacology and Experimental TherapeuticsFunctional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: 1. Activation of postsynaptic D3 receptors mediates hypothermia, whereas blockade of D2 receptors elicits prolactin secretion and catalepsy.
126 Citations1995M J Millan, J.‐L. PEGLION +8 more
Data demonstrate that the novel naphthofurane, (+)-S 14297, is a selective ligand (antagonist) at dopamine D3 receptors and suggest that their activation mediates hypothermia in the rat.
European Journal of Pharmacology Molecular PharmacologyFunctional coupling of the human dopamine D3 receptor in a transfected NG 108-15 neuroblastoma-glioma hybrid cell line
124 Citations1994Catherine Pilon, Daniel Lévesque +5 more
In transfected NG 108-15 cells, the dopamine D3 receptor is coupled to a pertussis toxin-sensitive G protein and mediates two possibly unrelated biological effects, through initial biochemical events that remain to be identified.
European Journal of Pharmacology Molecular PharmacologyCharacterization of the human dopamine D3 receptor expressed in transfected cell lines
119 Citations1994Robert G. MacKenzie, Donald VanLeeuwen +6 more
It is concluded that the signalling properties of the D3 receptor differ from those of its closest homolog, the D2 receptor.
Neurochemistry InternationalVisualization of dopamine D1, D2 and D3 receptor mRNA's in human and rat brain
117 Citations1992Guadalupe Mengod, Mercè Villaró +8 more
Using 32P-labelled oligonucleotides derived from the coding regions of dopamine D1, D2 and D3 receptor mRNAs, cells containing transcripts for these receptors in the human and rat brain were localized and a good agreement was found between the distribution of transcripts and binding sites.
Journal of Pharmacology and Experimental TherapeuticsFunctional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: II. Both D2 and "silent" D3 autoreceptors control synthesis and release in mesolimbic, mesocortical and nigrostriatal pathways.
109 Citations1995Alain P. Gobert, Jean‐Michel Rivet +6 more
The data suggest that D3 (auto)receptors control synthesis and release of DA in dopaminergic pathways innervating the limbic system, cortex and striatum and that D2/D3 receptor antagonist haloperidol modified DA turnover upon administration alone.
Molecular PharmacologyD2, D3, and D4 dopamine receptors couple to G protein-regulated potassium channels in Xenopus oocytes.
108 Citations1996P. Werner, Nicolas Hussy +3 more
All three D2-like dopamine receptors share the potential to activate inwardly rectifying potassium channels, and dopamine was ineffective in oocytes injected 2 hr previously with pertussis toxin.
Medical Entomology and ZoologyCNS Neurotransmitters and Neuromodulators: Dopamine
106 Citations1996Trevor W. Stone
NeuroreportD2-Family receptor distribution in human postmortem tissue
105 Citations1995Robert A. Lahti, Rosalinda C. Roberts +1 more
Based upon the ligands properties it is inferred that D2 distribution is highest in putamen, caudate and nucleus accumbens; D4 receptor in cortical areas and hippocampus; and D3 in the nucleus Accumbens.
Journal of Pharmacology and Experimental Therapeutics[3H]quinpirole binding to putative D2 and D3 dopamine receptors in rat brain and pituitary gland: a quantitative autoradiographic study.
105 Citations1993Beth Levant, D E Grigoriadis +1 more
The utility of [3H]quinpirole to label D3 as well as D2 dopamine receptors is shown, in concordance with the recently reported distribution of D3 receptor mRNA in these brain regions.
NeuropsychopharmacologyLack of Discrimination by Agonists for D2 and D3 Dopamine Receptors
104 Citations1995Kellie P. Burris
Putative D3 receptor-selective agonists also interact with a high-affinity, G protein-coupled state of D2 receptors, demonstrating that currently available agonists cannot be used to discriminate between behavioral effects mediated by D2 and D3 receptors.
Journal of Affective DisordersDopamine D2, D3 and D4 receptor and transporter gene polymorphisms and mood disorders
104 Citations1996Hiroshi Manki, Shigenobu Kanba +10 more
It is suggested that there is a significant association between the dopamine D4 receptor gene and mood disorders, especially major depression, but no association between any of the other polymorphisms and Mood disorders.
Journal of Biological ChemistryA novel short isoform of the D3 dopamine receptor generated by alternative splicing in the third cytoplasmic loop.
104 Citations1993C. Simone Fishburn, D. Belleli +3 more
expression studies show the novel short D3 isoform to bind dopaminergic ligands with a D3-like pharmacological profile and suggests that an internal acceptor site in the exon coding for the distal part of the third cytoplasmic loop directs alternative splicing of the D3 dopamine receptor.
European Journal of NeuroscienceOpposing Roles for Dopamine D<sub>2</sub> and D<sub>3</sub> Receptors on Neurotensin mRNA Expression in Nucleus Accumbens
101 Citations1994Jorge Díaz, Daniel Lévesque +5 more
Using in situ hybridization histochemistry in rat nucleus accumbens, it is shown that the dopamine D3 receptor mRNA is expressed in the ventromedial part of the shell subdivision, where its gross distribution matches that of neurotensin mRNA.
PubMedLinkage analysis of schizophrenia with five dopamine receptor genes in nine pedigrees.
98 Citations1993Hilary Coon, William Byerley +8 more
Testing for genetic linkage to schizophrenia in nine multigenerational families using a neurophysiological indicator variable, the P50 auditory evoked response, indicates that a defect at any of the actual receptor sites is unlikely to be a major contributor to schizophrenia.
Acta Psychiatrica ScandinavicaLack of association between schizophrenia and alleles in the dopamine D<sub>3</sub> receptor gene
97 Citations1993Erik G. Jönsson, L. Lannfelt +3 more
The present study does not provide evidence that the BalI polymorphism in the dopamine D3 receptor gene is involved in the pathophysiology of schizophrenia, but if not corrected for multiple testing, an association was found between homozygosity and positive response to neuroleptic drugs.
Brain ResearchAutoradiographic distribution of D3-type dopamine receptors in human brain using [3H]7-hydroxy-N,N-di-n-propyl-2-aminotetralin
97 Citations1994Luc Herroelen, J.-P. De Backer +4 more
The authors' data confirm a predilection of D3 receptors in brain areas involved in cognitive and emotional functions and suggest that they also play a role in the dopaminergic control of motor processes.
European Journal of PharmacologyThe dopamine receptor agonist 7-OH-DPAT modulates the acquisition and expression of morphine-induced place preference
96 Citations1995Fernando Rodrı́guez de Fonseca, Pilar Rubio +4 more
The pattern of effects seen with 7-OH-DPAT suggests that it may be useful for treating opiate dependence and craving, although involvement of dopamine D2 receptors cannot be excluded.
Journal of Pharmacology and Experimental TherapeuticsCharacterization of [3H]quinpirole binding to D2-like dopamine receptors in rat brain.
95 Citations1992Beth Levant, D E Grigoriadis +1 more
The in vitro binding properties of newly developed [3H]quinpirole in rat brain are described, with high affinity binding characteristics revealed by association-dissociation kinetics, and this pharmacological profile is similar, though-not identical, to that observed for spiperone-labeled D2 receptors.
Biological PsychiatryDopamine-related genes and their relationships to monoamine metabolites in CSF
94 Citations1996Erik G. Jönsson, Göran Sedvall +10 more
The results suggest that specific DRD2, DRD3, and TH genotypes participate in the regulation of monoamine turnover in the central nervous system.
PubMed[Gene cloning of human dopaminergic D3 receptor and identification of its chromosome].
92 Citations1990Bruno Giros, Martres Mp +2 more
The coding region of the human dopaminergic D3 receptor gene was cloned and sequenced and the deduced amino acid sequence displays a global homology with rat D3ceptor with a deletion of 46 residues within the third intracytoplasmic loop.
Proceedings of the National Academy of SciencesMorphogenic potentials of D2, D3, and D4 dopamine receptors revealed in transfected neuronal cell lines.
89 Citations1994Barbara C. Swarzenski, Lei‐Han Tang +3 more
To determine which D2-like receptors possess morphogenic potentials, a clonal mesencephalic cell line was transfected with D2, D3, or D4 receptor subtypes and treated with quinpirole and changes in morphological characteristics were quantitated.
Human GeneticsChromosomal localization of the human D3 dopamine receptor gene
88 Citations1991Maryvonne Le Coniat, Pierre Sokoloff +6 more
A novel dopamine D3 receptor gene that may be involved in psychiatric diseases has recently been characterized and has been assigned to chromosome 3 by hybridization with a D3 receptors probe to human sorted chromosomes.
European Journal of PharmacologyDopamine receptor agonist potencies for inhibition of cell firing correlate with dopamine D3 receptor binding affinities
87 Citations1995Deborah S. Kreiss, Debra A. Bergstrom +4 more
A functional role for the dopamine D3 receptor subtype in the autoreceptor-mediated regulation of dopamine cell activity is supported and the limitations of using currently available dopamine receptor agonists to delineate relative in vivo roles are demonstrated.
European Journal of PharmacologyBehavioral and biochemical effects of the dopamine D3 receptor-selective ligand, 7-OH-DPAT, in the normal and the reserpine-treated rat
87 Citations1994Sven Ahlénius, Peter Salmi
It appears that the dopamine D3 receptor-preferring ligand, 7-OH-DPAT, displays the profile of a dopamine D2 receptor agonist, pre- and postsynaptically.
Journal of NeuroscienceFunctional expression and characterization of human D2 and D3 dopamine receptors
86 Citations1994M N Potenza, GF Graminski +2 more
Functional characteristics of human D2 and D3 receptors (DRs) were examined using a new bioassay suited for the study of Gi-protein- coupled receptors (GiRs) and reveal functional similarities and differences between the D2R andD3R.
PsychopharmacologyBehavioural effects in the rat of the putative dopamine D3 receptor agonist 7-OH-DPAT: comparison with quinpirole and apomorphine
85 Citations1996Ronan Depoortère, Ghislaine Perrault +1 more
Together, the data suggest that the putative dopamine D3 agonist 7-OH-DPAT, at low doses, has depressant effects similar to those induced by low doses of the other two DA agonists.
European Journal of PharmacologyIn vivo evidence for preferential role of dopamine D3 receptor in the presynaptic regulation of dopamine release but not synthesis
81 Citations1996Raul R. Gainetdinov, Tatyana D. Sotnikova +2 more
The present results give further support to the hypothesis that the dopamine D3 autoreceptor is preferentially involved in the presynaptic regulation of dopamine release, while the D2 autore receptor controls dopamine synthesis.
Journal of Pharmacology and Experimental TherapeuticsInhibition of dopamine synthesis by dopamine D2 and D3 but not D4 receptors.
81 Citations1996Christina M. O'Hara, Ann Uhland‐Smith +2 more
Data confirm the hypothesis that dopamine D2 and D3 receptors can perform dual roles in autoreceptor regulation, and exclude cyclic AMP- and okadaic acid-sensitive phosphatase activity.
Biochemical and Biophysical Research CommunicationsExpression of the D3 Dopamine Receptor Gene and a Novel Variant Transcript Generated by Alternative Splicing in Human Peripheral Blood Lymphocytes
80 Citations1993Yoshitaka Nagai, Saneyoshi Ueno +3 more
The sequential reverse transcription and polymerase chain reaction amplified the mRNA coding for the D3 dopamine receptor (D3R) in human peripheral blood lymphocytes and there was a novel shorter variant transcript of the D2 dopamine receptor gene generated by alternative splicing in lymphocyte and brain.
Journal of Biological ChemistryRegulation of ligand binding to pituitary D-2 dopaminergic receptors. Effects of divalent cations and functional group modification.
78 Citations1983David R. Sibley, Ian Creese
The effects of divalent cations and protein-modifying reagents on the binding of agonist and antagonist ligands to D-2 dopaminergic receptors were studied and can be incorporated into a two-step, three-component ternary complex model in which the second binding reaction appears to be under equilibrium restraint.
PsychopharmacologyChanges in dopamine D1, D2 and D3 receptor mRNA levels in rat brain following antipsychotic treatment
77 Citations1992Paul R. Buckland, Michael O‘Donovan +1 more
The results indicate that the up-regulation of dopamine receptors may be associated with the occurrence of tardive dyskinesia but not the clinical mode of action of antipsychotics.
European Journal of Pharmacology[3H]7-OH-DPAT is capable of labeling dopamine D2 as well as D3 receptors
76 Citations1995Antonio Morilla González, David R. Sibley
The binding of [3H]7-OH-DPAT to the D2 receptor was sensitive to guanine nucleotides suggesting occupancy of a high affinity G protein-coupled state of the receptor.
American Journal of Medical GeneticsAssociation study of bipolar disorder with candidate genes involved in catecholamine neurotransmission: DRD2, DRD3, DAT1, and TH genes
76 Citations1996Daniel Souery, Olivier Lipp +5 more
Despite strong evidence for genetic involvement in the etiology of affective disorders, linkage and association methodologies are still exploring the nature of genetic factors in these diseases, including candidate genes involved in catecholamine neurotransmission.
American Journal of Medical GeneticsDopamine D3 receptor gene: Organization, transcript variants, and polymorphism associated with schizophrenia
76 Citations1996Nathalie Griffon, M.A. Crocq +11 more
The previously reported association between homozygosity at both alleles of the Bal I polymorphism and schizophrenia was presently maintained in an extended sample, comprising 119 DSM-III-R chronic schizophrenics and 85 controls.
European Journal of PharmacologyAutoradiographic localization of [3H]quinpirole binding to dopamine D2 and D3 receptors in rat brain
76 Citations1992Donald R. Gehlert, Susan L. Gackenheimer +2 more
Results indicate that [3H]quinpirole labels a high affinity agonist conformation of dopamine D2 receptors as well as dopamine D3 receptors in rat brain, and provides the first detection of the dopamine D 3 receptor protein in the brain.
American Journal of Medical GeneticsAssociation study of schizophrenia with dopamine D3 receptor gene polymorphisms: Probable effects of family history of schizophrenia?
73 Citations1993Vishwajit L. Nimgaonkar, X. R. Zhang +3 more
Using a case-control design, a reported association of schizophrenia with homozygosity at the dopamine D3 receptor gene locus was investigated in a group of patients, with schizophrenia, and psychiatrically normal controls, matched for ethnicity and area of residence.
NeuropsychopharmacologyEffects of D3/D2 Dopamine Receptor Agonists and Antagonists on Prepulse Inhibition of Acoustic Startle in the Rat
71 Citations1995S. Barak Caine, Mark A. Geyer +1 more
Pretreatment with haloperidol prevented the disruption of PPI produced by the highest dose of each agonist, consistent with previous studies suggesting that dopamine agonists may modulate PPI in the rat through the D2 subtype of dopamine receptors.
Neurobiology of AgingDopamine D2, D3, and D4 receptor mRNA levels in rat brain and pituitary during aging
70 Citations1994Alessandra Valerio, Marco Belloni +4 more
The data suggest that the molecular mechanisms responsible for regulating the pattern of expression of the various dopamine receptors are differentially regulated by aging.
PsychopharmacologyDose-dependent effects of the D3-preferring agonist 7-OH-DPAT on motor behaviors and place conditioning
70 Citations1995Taline V. Khroyan, David L. Baker +1 more
The results suggest that intermediate doses (0.01–0.1 mg/kg) that increase yawning, and decrease locomotion and sniffing, may preferentially occupy D3 receptors, and suggest that these putative D3-preferring doses have weak aversive effects.
American Journal of Medical GeneticsNo association between schizophrenia and homozygosity at the D<sub>3</sub> dopamine receptor gene
69 Citations1993Yang Liu, Tao Li +8 more
Further studies will be needed with larger samples of patients from Wales and Alsace as well as with samples of different racial groups to prove or disprove the initial positive association between schizophrenia and genotypes of the D3 dopamine receptor gene.
NeuropsychopharmacologyBinding of [3H]PD 128907, a Putatively Selective Ligand for the D3 Dopamine Receptor, in Rat Brain: A Receptor Binding and Quantitative Autoradiographic Study
69 Citations1998B. Josephine Bancroft
Observations indicate labeling of a dopaminergic site with characteristics consistent with the D3 receptor in rat brain using in vitro radioligand binding and autoradiographic methods.
Journal of Neural TransmissionDifferential effects of dopamine D2 and D3 receptor antagonists in regard to dopamine release, in vivo receptor displacement and behaviour
67 Citations1994Nicholas Waters, L. L�fberg +4 more
Support is given for the hypothesis that the dopamine D3 receptor is functionally relevant at the postsynaptic level and proposed to exert an inhibitory influence on psychomotor functions.
European Journal of PharmacologyAssessment of cocaine-like discriminative stimulus effects of dopamine D3 receptor ligands
66 Citations1995Jane B. Acri, Sean R. Carter +6 more
The results suggest that dopamine D3 receptors may be involved in the subjective effects of cocaine, and therefore may be a target for the discovery of treatments for cocaine dependence.
European Journal of PharmacologyActivation of dopamine D3 autoreceptors inhibits firing of ventral tegmental dopaminergic neurones in vivo
66 Citations1995Franćoise Lejeune, Mark J. Millan
Data suggest that inhibitory (dendritic) dopamine D3 (auto)receptors control the electrical activity of ventral tegmental area-localised dopaminergic neurones in anaesthetised rats.
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