Publications by authors named "Eleftheria N Finger"
Studies on human genetics have suggested that inhibitors of the Na1.7 voltage-gated sodium channel hold considerable promise as therapies for the treatment of chronic pain syndromes. Herein, we report novel, peripherally-restricted benzoxazolinone aryl sulfonamides as potent Na1.
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- * To streamline this process, researchers can start with a smaller subset of compounds and use virtual screening methods to prioritize which additional compounds to test, combining multiple screening techniques for better results.
- * A new method of combining these prioritizations was tested and showed to retrieve significantly more active compounds compared to using a single approach, improving the efficiency of drug discovery and guiding future screening strategies.
The voltage-gated sodium channel Na1.7 is a genetically validated target for the treatment of pain with gain-of-function mutations in man eliciting a variety of painful disorders and loss-of-function mutations affording insensitivity to pain. Unfortunately, drugs thought to garner efficacy via Na1 inhibition have undesirable side effect profiles due to their lack of selectivity over channel isoforms.
View Article and Find Full Text PDFThe EphA4 receptor and its ephrin ligands are involved in astrocytic gliosis following CNS injury. Therefore, a strategy aimed at the blockade of EphA4 signaling could have broad therapeutic interest in brain disorders. We have identified novel small molecule inhibitors of EphA4 kinase in specific enzymatic and cell-based assays.
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- The study investigates how repeated administration of a metabotropic glutamate receptor 5 positive allosteric modulator (CDPPB) affects anti-psychotic-like effects in a rat model of schizophrenia.
- CDPPB acutely reduces amphetamine-induced hyperlocomotion, but with repeated dosing over 7 days, the effects vary by brain region, showing tolerance in the frontal cortex but not in the striatum.
- These findings highlight that receptor desensitization is region-specific and may influence both sleep architecture and response to psychostimulants differently.