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Copper-Mediated Late-Stage Iodination and 123I-Labelling of Triazole-benzimidazole Bioactives
Investigations have generated two highly promising 123 I-labelled radiotracer candidates that retain high affinities for the GnRH-receptor.
An acylation‐Finkelstein approach to radioiodination of bioactives: The role of amide group anchimeric assistance
A straightforward sequential acylation-Finkelstein approach to achieve iodination of amine containing bioactives and discloses a number of fundamental aspects of amide group anchimeric assistance in substitution reactions.
Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor† †Electronic supplementary information (ESI) available: Detailed experimental procedures and…
- Richard Fjellaksel, Marc Boomgaren, R. Sundset, I. Haraldsen, J. Hansen, P. Riss
- Biology, ChemistryMedChemComm
- 14 September 2017
The synthesis and characterization of a library of small molecule antagonists of the human gonadotropin releasing hormone receptor based upon the 2-(4-tert-butylphenyl)-4-piperazinyl-benzimidazole scaffold via Cu-catalysed azide alkyne cycloaddition is reported.
Evaluation by metabolic profiling and in vitro autoradiography of two promising GnRH-receptor ligands for brain SPECT imaging.
- Richard Fjellaksel, Angel Moldes Anaya, R. Sundset
- Biology, ChemistryJournal of labelled compounds…
- 8 December 2019
A preclinical evaluation of the compound properties was performed to evaluate their potential as Single Photon Emission Computed Tomography (SPECT) radiotracers for imaging the GnRH-receptor and found that compounds 3 and 4 binds to rat Gn RH-R in different rat brain regions.
Discovery of a Lead Brain‐Penetrating Gonadotropin‐Releasing Hormone Receptor Antagonist with Saturable Binding in Brain
Positron emission tomography imaging in rat under baseline conditions in comparison to pretreatment with a receptor‐saturating dose of GnRH antagonist revealed saturable uptake into the brain.
Ny diagnostikk for Alzheimers i Nytt Senter
Stability evaluation of [18F]FDG: literature study, stability studies from two different PET centres and future recommendations
- J. G. Holler, Børge Renmælmo, Richard Fjellaksel
- MedicineEJNMMI Radiopharmacy and Chemistry
- 24 February 2022
Recommendations for determining the shelf life based on the available stability literature and the own two-centre stability studies are made, especially the choice of synthesis, photostability, the environment, temperature and storage.
Catalytic Intermolecular Functionalization of Benzimidazoles
- Jørn H. Hansen, Richard Fjellaksel
- Chemistry, BiologyChemistry and Applications of Benzimidazole and…
- 25 June 2019
This chapter describes contemporary strategies for selective catalytic intermolecular functionalization of the benzimidazole scaffold using copper, palladium, rhodium, nickel, and cobalt catalysis to ensure selectivity.
Development and evaluation of gonadotropin releasing hormone antagonists as SPECT radiotracers
- Richard Fjellaksel
- 24 May 2018