Development of Small Molecule Inhibitors of Neuronal Calcium Ion Channels Relevant to the Treatment of Neuropathic Pain

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.