Publications by authors named "Valentina O Badescu"

The α7 nicotinic acetylcholine receptor is a calcium permeable, ligand-gated ion channel that modulates synaptic transmission in the hippocampus, thalamus, and cerebral cortex. Previously disclosed work described PNU-120596 that acts as a powerful positive allosteric modulator of the α7 nicotinic acetylcholine receptor. The initial structure-activity relationships around PNU-120596 were gleaned from screening a large thiazole library.

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The objective of the described research effort was to identify a novel serotonin and norepinephrine reuptake inhibitor (SNRI) with improved norepinephrine transporter activity and acceptable metabolic stability and exhibiting minimal drug-drug interaction. We describe herein the discovery of a series of 3-substituted pyrrolidines, exemplified by compound 1. Compound 1 is a selective SNRI in vitro and in vivo, has favorable ADME properties, and retains inhibitory activity in the formalin model of pain behavior.

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Synopsis of recent research by authors named "Valentina O Badescu"

  • - Valentina O Badescu's research primarily focuses on the modulation of neurotransmitter receptors, particularly the α7 nicotinic acetylcholine receptor, aiming to improve understanding of its structure-activity relationships which are crucial for designing more effective therapeutic agents.
  • - Recent findings highlighted in her 2023 article reveal the significance of PNU-120596 as a positive allosteric modulator for the α7 receptor, providing insights into the potential effects of modulation on synaptic transmission in key brain areas.
  • - In addition to receptor modulation, Badescu's research also includes the development of dual serotonin and norepinephrine reuptake inhibitors, demonstrating successful identification of compounds that exhibit desirable pharmacological properties and potential applications in pain management.