ArticleAnnals of neurosciences2012
Development of time-resolved fluorescent based [EU]-GTP binding assay for selection of human Histamine 3 receptor antagonists/inverse agonist: a potential target for Alzheimer's treatment.
Article in Annals of neurosciences, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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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.
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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.
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Who cites it
1 citing paper in PubMed, 3 citations in OpenAlex.
- Pharmacological Characterization of Human Histamine Receptors and Histamine Receptor Mutants in the Sf9 Cell Expression System.Handbook of experimental pharmacology · 2017Review
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Authors and funding
3 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundThe histamine H3 receptor is an attractive G protein-coupled receptor drug target that regulates neurotransmission in the central nervous system and plays a crucial role in cognitive and homeostatic functions. This receptor exhibits molecular, pharmacological, and functional heterogeneity that affects the preclinical development of effective antagonists. The range of assay technologies like radio isotope based [35S] GTPγS binding assay, luminescent based reporter gene assay (In-direct cAMP measurement) for binding and signaling have been developed in High Throughput Screening (HTS) laboratories for the identification of hit or lead compounds acting on H3 receptor. PURPOSE: The [35S] GTPγS binding assay still remains a useful and a simple technique to demonstrate receptor activation and is one of the few functional, cell-free assays that has set the standards in the field of research. However, its radioactive nature imposes clear limitations to its use in regular laboratory practice and in high-throughput experimentation.
methodsHerein, we have developed and optimized a membrane based non-radioactive assay using a europium-labeled GTP analogue in which europium-GTP binding can be assayed using time-resolved fluorescence technology.
resultsThe characterization of H3 agonist or antagonist with HTRF platform has revealed a rank order potency (pEC50 & P K B) comparable to that from isotopic functional studies measured by liquid scintillation counter (LSC). Lastly, the Eu-GTP binding assay has been found to be highly robust (Z' factor 0.84) with high percentage over basal counts.
conclusionThis assay can be utilized as a component of cascade for the screening of H3 receptor ligands.
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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.