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6 Hz Active Anticonvulsant Fluorinated N-Benzamide Enaminones and Their Inhibitory Neuronal Activity

Author

Listed:
  • Isis J. Amaye

    (Department of Pharmaceutical Sciences, School of Pharmacy and Health Professions, University of Maryland Eastern Shore, One Backbone Road, Princess Anne, MD 21853, USA)

  • Thomas Heinbockel

    (Department of Anatomy, College of Medicine, Howard University, 520 W Street, NW, Washington, DC 20059, USA)

  • Julia Woods

    (Department of Anatomy, College of Medicine, Howard University, 520 W Street, NW, Washington, DC 20059, USA)

  • Zejun Wang

    (Department of Anatomy, College of Medicine, Howard University, 520 W Street, NW, Washington, DC 20059, USA)

  • Miguel Martin-Caraballo

    (Department of Pharmaceutical Sciences, School of Pharmacy and Health Professions, University of Maryland Eastern Shore, One Backbone Road, Princess Anne, MD 21853, USA)

  • Patrice Jackson-Ayotunde

    (Department of Pharmaceutical Sciences, School of Pharmacy and Health Professions, University of Maryland Eastern Shore, One Backbone Road, Princess Anne, MD 21853, USA)

Abstract

A small library of novel fluorinated N-benzamide enaminones were synthesized and evaluated in a battery of acute preclinical seizure models. Three compounds (GSA 62, TTA 35, and WWB 67) were found to have good anticonvulsant activity in the 6-Hz ‘psychomotor’ 44-mA rodent model. The focus of this study was to elucidate the active analogs’ mode of action on seizure-related molecular targets. Electrophysiology studies were employed to evaluate the compounds’ ability to inhibit neuronal activity in central olfactory neurons, mitral cells, and sensory-like ND7/23 cells, which express an assortment of voltage and ligand-gated ion channels. We did not find any significant effects of the three compounds on action potential generation in mitral cells. The treatment of ND7/23 cells with 50 µM of GSA 62, TTA 35, and WWB 67 generated a significant reduction in the amplitude of whole-cell sodium currents. Similar treatment of ND7/23 cells with these compounds had no effect on T-type calcium currents, indicating that fluorinated N-benzamide enaminone analogs may have a selective effect on voltage-gated sodium channels, but not calcium channels.

Suggested Citation

  • Isis J. Amaye & Thomas Heinbockel & Julia Woods & Zejun Wang & Miguel Martin-Caraballo & Patrice Jackson-Ayotunde, 2018. "6 Hz Active Anticonvulsant Fluorinated N-Benzamide Enaminones and Their Inhibitory Neuronal Activity," IJERPH, MDPI, vol. 15(8), pages 1-13, August.
    • Handle: RePEc:gam:jijerp:v:15:y:2018:i:8:p:1784-:d:164625
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