Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I 2 ligand

PA Coates, P Grundt, ESJ Robinson, DJ Nutt…

Index: Coates, Philippa A.; Grundt, Peter; Robinson, Emma S.J.; Nutt, David J.; Tyacke, Robin; Hudson, Alan L.; Lewis, John W.; Husbands, Stephen M. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 6 p. 605 - 607

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Citation Number: 18

Abstract

An irreversible ligand (7) has been prepared based on the selective I2 ligand 2-BFI. Compound 7 displayed high affinity and selectivity for I2-sites and has been shown to irreversibly bind to these sites in rat brain. Compound 7 should, therefore, prove an invaluable tool for the further elucidation of I2-site function.