Discovery of a Lead Brain‐Penetrating Gonadotropin‐Releasing Hormone Receptor Antagonist with Saturable Binding in Brain

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 anta...

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Detalles Bibliográficos
Autores principales: Bekker, Roberto B. W., Fjellaksel, Richard, Hjornevik, Trine, Nuruddin, Syed, Rafique, Waqas, Hansen, Jørn H., Sundset, Rune, Haraldsen, Ira H., Riss, Patrick J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2020
Materias:
Communications
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7540054/
https://www.ncbi.nlm.nih.gov/pubmed/32677155
http://dx.doi.org/10.1002/cmdc.202000256

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7540054/
https://www.ncbi.nlm.nih.gov/pubmed/32677155
http://dx.doi.org/10.1002/cmdc.202000256

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