Development of Small Molecule Inhibitors of Neuronal Calcium Ion Channels Relevant to the Treatment of Neuropathic Pain
thesis
posted on 2022-08-23, 05:25authored byANJIE SHALIQUE BISPAT
Neuropathic pain is a debilitating condition affecting 7-8% of the population. Current treatment options, which include anticonvulsants, antidepressants and opioids, offer minimal relief. This project was focused on the development of analgesics, which act at the N- and T-type calcium channels involved in pain transmission. Sixty-three novel compounds were rationally designed, synthesised and tested for activity using a Fluorescence Image Plate Reader bioassay. The stability of the compounds in plasma and their cytotoxic properties were assessed. The sulfonamide derivatives were identified as drug leads due to their stability in plasma, low toxicity profile and high potency for both calcium channels.
History
Campus location
Australia
Principal supervisor
Kellie Tuck
Additional supervisor 1
Peter Duggan (CSIRO)
Year of Award
2022
Department, School or Centre
Chemistry
Additional Institution or Organisation
The Commonwealth Scientific and Industrial Research Organisation