ArticleJournal of neural transmission (Vienna, Austria : 1996)1996
Antipsychotics with inverse agonist activity at the dopamine D3 receptor.
Article in Journal of neural transmission (Vienna, Austria : 1996), 1996. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
What it found
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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
11 citing papers in PubMed, 52 citations in OpenAlex.
- Discovery, Characterization, and Optimization of a Novel Positive Allosteric Modulator-Antagonist of the DJournal of medicinal chemistry · 2025Article
- ESG-1-60 and ESG-1-61: Novel dopamine DBritish journal of pharmacology · 2025Article
- Role of dopamine DPsychopharmacology · 2019Article
- Discovery of CNS-Like D3R-Selective Antagonists Using 3D Pharmacophore Guided Virtual Screening.Molecules (Basel, Switzerland) · 2018Article
- Inverse agonism and its therapeutic significance.Indian journal of pharmacology · 2011Article
- Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist.Science (New York, N.Y.) · 2010Article
- A review of the discovery, pharmacological characterization, and behavioral effects of the dopamine D2-like receptor antagonist eticlopride.CNS neuroscience & therapeutics · 2008Review
- Histamine H3-receptor-mediated [35S]GTP gamma[S] binding: evidence for constitutive activity of the recombinant and native rat and human H3 receptors.British journal of pharmacology · 2002Article
- Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery.British journal of pharmacology · 2000Review
- Review: amino acid domains involved in constitutive activation of G-protein-coupled receptors.Molecular neurobiology · 1998Review
- Selective expression of dopamine D3 receptor mRNA in proliferative zones during embryonic development of the rat brain.The Journal of neuroscience : the official journal of the Society for Neuroscience · 1997Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In NG 108-15 cells expressing the recombinant human D3 receptor, dopamine agonists enhance [3H]thymidine incorporation and decrease cAMP accumulation. In these cells, but not in wild type cells, haloperidol, fluphenazine, and various other antipsychotics inhibited basal [3H]thymidine incorporation in a concentration-dependent manner. In contrast, other dopamine antagonists such as nafadotride or (+)AJ 76, two D3-preferring antagonists, were without effect. The concentration-response curve of haloperidol was shifted to the right in presence of nafadotride, with a potency compatible with its nanomolar apparent affinity as neutral antagonist. Pertussis toxin treatment abolished or markedly reduced the responses to haloperidol or fluphenazine. In contrast, no significant enhancement of cAMP accumulation could be observed, under the influence of haloperidol or eticlopride. These data indicate that some dopamine antagonists behave as inverse agonists, and thus appear to inhibit an agonist-independent activity of the D3 receptor on [3H]thymidine incorporation pathway, but not on the cAMP pathway.
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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.