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Related Experiment Video

Updated: Nov 25, 2025

Dopamine Release at Individual Presynaptic Terminals Visualized with FFNs
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Fluorescent ligands for dopamine D2/D3 receptors.

Anni Allikalt1, Nirupam Purkayastha1, Khajidmaa Flad1

  • 1Department of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, 91058, Erlangen, Germany.

Scientific Reports
|December 15, 2020
PubMed
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Researchers developed novel fluorescent ligands targeting dopamine D2-like receptors for neurological and psychiatric disorders. These ligands show high affinity and enable visualization of receptors on living cells, aiding drug discovery.

Area of Science:

  • Medicinal Chemistry
  • Neuroscience
  • Biophysics

Background:

  • G protein-coupled receptors (GPCRs) are crucial drug targets.
  • Dopamine D2-like receptors (D2R, D3R) are implicated in Parkinson's disease and schizophrenia.
  • Fluorescent ligands are valuable tools for studying receptor dynamics and interactions.

Purpose of the Study:

  • To design and synthesize novel fluorescent ligands for dopamine D2-like receptors.
  • To evaluate the binding affinities and functional properties of these ligands.
  • To demonstrate their utility in cellular imaging and biochemical assays.

Main Methods:

  • Synthesis of fluorescent ligands based on phenylpiperazine and indanylamine scaffolds.
  • Radioligand binding assays to determine receptor affinity.

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Last Updated: Nov 25, 2025

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  • Cellular imaging using total internal reflection fluorescence microscopy (TIR-FM).
  • NanoBRET binding assays for receptor interaction studies.
  • Main Results:

    • Developed dansyl-labeled ligands with high affinity (sub-nanomolar) for D2R and D3R.
    • Xanthene and cyanine dye-labeled ligands maintained excellent binding properties and acted as agonists.
    • Cy3B-labeled ligand visualized D2R and D3R on living cells.
    • Rhodamine-labeled ligand demonstrated efficacy in NanoBRET assays for D3R.

    Conclusions:

    • Novel fluorescent ligands targeting dopamine D2-like receptors were successfully synthesized.
    • These ligands exhibit high affinity and agonist activity, suitable for D2R and D3R research.
    • The developed probes are effective tools for cellular imaging and biochemical assays, advancing GPCR research and drug discovery.