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ID: ALA1156026
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of pyridazinone-based 5-HT(2C) agonists.
Authors: Allerton CM, Andrews MD, Blagg J, Ellis D, Evrard E, Green MP, Liu KK, McMurray G, Ralph M, Sanderson V, Ward R, Watson L.
Abstract: The SAR of a series of pyridazinone derived 5-HT(2C) agonists has been explored and resulted in identification of a compound with excellent levels of 5-HT(2C) functional agonism and selectivity over 5-HT(2A) and 5-HT(2B). This compound displayed good in vivo efficacy in pre-clinical models of stress urinary incontinence, despite having physiochemical properties commensurate with impaired CNS penetration.
CiteXplore: 19716297