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Piperazine-based P2X4 receptor antagonists.

Katharina Sophie Erlitz1,2, Alena I Siutkina3, Ann-Kathrin Prinz3

  • 1European Institute for Molecular Imaging (EIMI), University of Muenster, Muenster, Germany.

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|December 31, 2024
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Summary
This summary is machine-generated.

Researchers developed novel piperazine-based antagonists targeting the P2X4 receptor (P2X4R), a key player in neuroinflammation and pain. Some compounds showed superior P2X4R antagonism compared to paroxetine, indicating therapeutic potential.

Keywords:
Buchwald reactionCham‐Evans‐Lam couplingP2X4 receptorP2X4R antagonistligand‐gated ion channel

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Medicinal Chemistry

Background:

  • The P2X4 receptor (P2X4R) is implicated in neuroinflammation, chronic pain, and cancer.
  • P2X4R antagonism represents a potential therapeutic strategy for these conditions.
  • Paroxetine serves as a reference compound for P2X4R antagonist development.

Purpose of the Study:

  • To design and synthesize novel piperazine-based P2X4R antagonists.
  • To investigate the structure-activity relationships (SARs) of these compounds.
  • To identify lead compounds with improved P2X4R antagonistic potency.

Main Methods:

  • Synthesis of over 35 piperazine-based compounds.
  • Evaluation of P2X4R antagonistic activity using a Ca²⁺-flux assay.
  • Assessment of absorption, distribution, metabolism, and excretion (ADME) properties.

Main Results:

  • Several synthesized compounds demonstrated higher P2X4R antagonistic potency than paroxetine.
  • Increased lipophilicity correlated with high plasma protein binding and reduced metabolic stability.
  • Compounds featuring a naphthalene-2-yloxy group exhibited particular metabolic liabilities.

Conclusions:

  • Promising SARs were identified for piperazine-based P2X4R antagonists.
  • Further optimization is required to enhance potency and improve pharmacokinetic properties.
  • This study provides a foundation for developing P2X4R-targeted therapeutics.