Blar i forfatter "Haraldsen, Ira Hebold"

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    • Discovery of a lead brain-penetrating gonadotropin-releasing hormone receptor antagonist with saturable binding in brain 

      Bekker, Roberto Bartholomeus Wilhelmus; Fjellaksel, Richard; Hjornevik, Trine; Nuruddin, Syed; Rafique, Waqas; Hansen, Jørn H; Sundset, Rune; Haraldsen, Ira Hebold; Riss, Patrick (Journal article; Tidsskriftartikkel; Peer reviewed, 2020-07-16)
      We report the synthesis, radiosynthesis and biological characterisation of two gonadotropin‐releasing hormone receptor (GnRH−R) antagonists with nanomolar binding affinity. A small library of GnRH−R antagonists was synthesised in 20–67 % overall yield with the aim of identifying a high‐affinity antagonist capable of crossing the blood–brain barrier. Binding affinity to rat GnRH−R was determined by ...

    • Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor 

      Fjellaksel, Richard; Boomgaren, Marc; Sundset, Rune; Haraldsen, Ira Hebold; Hansen, Jørn H; Riss, Patrick (Journal article; Tidsskriftartikkel; Peer reviewed, 2017-08-14)
      In this communication, we report the synthesis and characterization of a library of small molecule antagonists of the human gonadotropin releasing hormone receptor based upon the 2-(4-<i>tert</i>-butylphenyl)-4-piperazinyl-benzimidazole scaffold <i>via</i> Cu-catalysed azide alkyne cycloaddition. Our main purpose was to find a more soluble compound based on the WAY207024 lead with nanomolar potency ...