ArticleBritish journal of pharmacology2003
Functional coupling of the human dopamine D2 receptor with G alpha i1, G alpha i2, G alpha i3 and G alpha o G proteins: evidence for agonist regulation of G protein selectivity.
Article in British journal of pharmacology, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
31 citing papers in PubMed, 95 citations in OpenAlex.
- Dopaminergic Input Regulates the Sensitivity of Indirect Pathway Striatal Spiny Neurons to Brain-Derived Neurotrophic Factor.Biology · 2023Article
- Generation of Gαi knock-out HEK293 cells illuminates Gαi-coupling diversity of GPCRs.Communications biology · 2023Article
- Contribution of G-Protein α-Subunits to Analgesia, Hyperalgesia, and Hyperalgesic Priming Induced by Subanalgesic and Analgesic Doses of Fentanyl and Morphine.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2022Article
- Article
- In Parkinson's patient-derived dopamine neurons, the triplication of α-synuclein locus induces distinctive firing pattern by impeding D2 receptor autoinhibition.Acta neuropathologica communications · 2021Article
- Signaling-Biased and Constitutively Active Dopamine D2 Receptor Variant.ACS chemical neuroscience · 2021Article
- Epidermal growth factor receptor as a molecular determinant of glioblastoma response to dopamine receptor D2 inhibitors.Neuro-oncology · 2021Article
- Review
- Arrestin recruitment to dopamine D2 receptor mediates locomotion but not incentive motivation.Molecular psychiatry · 2020Article
- A dynamic and screening-compatible nanoluciferase-based complementation assay enables profiling of individual GPCR-G protein interactions.The Journal of biological chemistry · 2019Article
- Mouse models of GNAO1-associated movement disorder: Allele- and sex-specific differences in phenotypes.PloS one · 2019Article
- Regional Heterogeneity of D2-Receptor Signaling in the Dorsal Striatum and Nucleus Accumbens.Neuron · 2018Article
- G protein-coupled receptor kinases as regulators of dopamine receptor functions.Pharmacological research · 2016Review
- Dopamine D3 autoreceptor inhibition enhances cocaine potency at the dopamine transporter.Journal of neurochemistry · 2016Article
- The role of kinetic context in apparent biased agonism at GPCRs.Nature communications · 2016Article
- The brain gene expression profile of dopamine D2/D3 receptors and associated signaling proteins following amphetamine self-administration.Neuroscience · 2015Article
- UTP is not a biased agonist at human P2Y(11) receptors.Purinergic signalling · 2014Article
- Article
- Noradrenaline stimulates cell proliferation by suppressing potassium channels via G(i/o) -protein-coupled α(1B) -adrenoceptors in human osteoblasts.British journal of pharmacology · 2013Article
- Active-state models of ternary GPCR complexes: determinants of selective receptor-G-protein coupling.PloS one · 2013Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
(1) The human dopamine D(2long) (D(2L)) receptor was expressed with four different G proteins in Sf9 cells using the baculovirus expression system. When co-expressed with G(i)/G(o) G proteins (G(i1)alpha, G(i2)alpha, G(i3)alpha, or G(o)alpha, plus Gbeta(1) and Ggamma(2)), the receptor displayed a high-affinity binding site for the agonists (dopamine and NPA), which was sensitive to GTP (100 micro M), demonstrating interaction between the receptor and the different G proteins. (2) The receptor to G protein ratio (R : G ratio) was evaluated using [(3)H]-spiperone saturation binding (R) and [(35)S]-GTPgammaS saturation binding (G). R : G ratios of 1 : 12, 1 : 3, 1 : 14 and 1 : 5 were found for G(i1), G(i2), G(i3), and G(o) preparations, respectively. However, when R : G ratios of 1 : 2 and 1 : 12 were compared for G(i2) and G(o), no difference was found for the stimulation of [(35)S]-GTPgammaS binding. (3) Several agonists were tested for their ability to stimulate [(35)S]-GTPgammaS binding to membranes co-expressing the receptor and various G proteins. All the compounds tested showed agonist activity in preparations expressing G(i3) and G(o). However, for G(i2) and G(i1) preparations, compounds such as S-(-)-3-PPP and p-tyramine were unable to stimulate [(35)S]-GTPgammaS binding. (4) Most of the compounds showed higher relative efficacies (compared to dopamine) and higher potencies in the preparation expressing G(o). Comparison of the effects of different agonists in the different preparations showed that each agonist differentially activates the four G proteins. (5) We conclude that the degree of selectivity of G protein activation by the D(2L) receptor can depend on the conformation of the receptor stabilised by an agonist.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.