Publications by authors named "Michel R Gillard"
Research on the therapeutic applications of the histamine H3 receptor (H3R) has traditionally focused on antagonists/inverse agonists. In contrast, H3R agonists have received less attention despite their potential use in several disease areas. The lower availability of H3R agonists not only hampers their full therapeutic exploration, it also prevents an unequivocal understanding of the structural requirements for H3R activation.
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- Levetiracetam (Keppra) is a new medication approved for treating hard-to-control partial onset seizures in adults, showing good efficacy and tolerance due to its specific binding site in the brain.
- Researchers aimed to discover new drugs targeting the levetiracetam binding site (LBS) by modifying the structure of the original compound, finding that certain modifications improved the drug's potency against seizures.
- A promising drug candidate named ucb 34714 emerged from these modifications, showing to be ten times more effective than levetiracetam in mice and is set to enter phase II clinical trials.