ArticleACS chemical neuroscience2011
Cross-receptor interactions between dopamine D2L and neurotensin NTS1 receptors modulate binding affinities of dopaminergics.
Article in ACS chemical neuroscience, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed.
- Review
- Mechanistic and therapeutic insights into class A GPCR dimers in neuropsychiatric disorders.npj drug discovery · 2026Review
- A neurotensin receptor type 1-derived pepducin acts as a biased allosteric modulator to regulate target receptor function.Acta pharmaceutica Sinica. B · 2026Article
- GPCR Heterodimers: Implications for Biased Signaling.Handbook of experimental pharmacology · 2026Review
- Modulation of Neuron and Astrocyte Dopamine Receptors via Receptor-Receptor Interactions.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Optical Control of Dopamine D2-like Receptors with Cell-Specific Fast-Relaxing Photoswitches.Journal of the American Chemical Society · 2023Article
- Class A and C GPCR Dimers in Neurodegenerative Diseases.Current neuropharmacology · 2022Review
- Visualization of real-time receptor endocytosis in dopamine neurons enabled by NTSR1-Venus knock-in mice.Frontiers in cellular neuroscience · 2022Article
- Bivalent ligands promote endosomal trafficking of the dopamine D3 receptor-neurotensin receptor 1 heterodimer.Communications biology · 2021Article
- Structure-Guided Design of G-Protein-Coupled Receptor Polypharmacology.Angewandte Chemie (International ed. in English) · 2021Article
- Dopamine D2 autoreceptor interactome: Targeting the receptor complex as a strategy for treatment of substance use disorder.Pharmacology & therapeutics · 2020Review
- Differential allosteric modulation within dopamine DScientific reports · 2019Article
- Brain Dopamine Transmission in Health and Parkinson's Disease: Modulation of Synaptic Transmission and Plasticity Through Volume Transmission and Dopamine Heteroreceptors.Frontiers in synaptic neuroscience · 2018Review
- Understanding the Role of GPCR Heteroreceptor Complexes in Modulating the Brain Networks in Health and Disease.Frontiers in cellular neuroscience · 2017Review
- Structure-guided development of heterodimer-selective GPCR ligands.Nature communications · 2016Article
- Neurotensin inhibits both dopamine- and GABA-mediated inhibition of ventral tegmental area dopamine neurons.Journal of neurophysiology · 2015Article
- Activation of neurotensin receptor type 1 attenuates locomotor activity.Neuropharmacology · 2014Article
- Gut-brain peptides in corticostriatal-limbic circuitry and alcohol use disorders.Frontiers in neuroscience · 2014Review
- Diversity and Bias through Receptor-Receptor Interactions in GPCR Heteroreceptor Complexes. Focus on Examples from Dopamine D2 Receptor Heteromerization.Frontiers in endocrinology · 2014Review
- Disease-specific heteromerization of G-protein-coupled receptors that target drugs of abuse.Progress in molecular biology and translational science · 2013Review
Corrections and comments
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Authors and funding
3 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Dopaminergic systems have been described to functionally interact with the neuromodulatory peptide neurotensin. Employing fluorescence detected coimmunoprecipitation and radioligand binding experiments, we herein demonstrate that coexpression of dopamine D(2L) receptor and the neurotensin receptor subtype NTS(1) leads to physical interaction and the formation of heteromers in transfected human embryonic kidney 293 cells. In this in vitro system, a trans-inhibitory effect on the agonist binding affinity of D(2) was observed in presence of neurotensin. To correlate between the functional properties of dopaminergic agents and the magnitude of neurotensin-induced modulation of D(2L) binding affinities in cells coexpressing D(2L) and NTS(1), a structurally diverse set of dopamine receptor agonists, partial agonists, and antagonists was tested. Ligand specific profiles indicating substantial bias between ligand efficacy and transmodulation were discovered, suggesting a heteromerization-based functional selectivity. In the presence of neurotensin, the novel D(2) agonist FAUC 326 displayed a 34-fold decrease of binding affinity in cells coexpressing D(2L) and NTS(1).
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Registered trials
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