Probes for imidazoline binding sites: Synthesis and evaluation of a selective, irreversible I2 ligand

Philippa A. Coates; Peter Grundt; Emma S.J. Robinson; David J. Nutt; Robin Tyacke; Alan L. Hudson; John W. Lewis; Stephen M. Husbands

doi:10.1016/S0960-894X(00)00062-7

Probes for imidazoline binding sites: Synthesis and evaluation of a selective, irreversible I₂ ligand

Philippa A. Coates
, Peter Grundt
, Emma S.J. Robinson
, David J. Nutt
, Robin Tyacke
, Alan L. Hudson
, John W. Lewis
, Stephen M. Husbands

University of Bristol

Research output: Contribution to journal › Article › peer-review

17 Citations (SciVal)

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. (C) 2000 Elsevier Science Ltd. All rights reserved.

Original language	English
Pages (from-to)	605-607
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	10
Issue number	6
DOIs	https://doi.org/10.1016/S0960-894X(00)00062-7
Publication status	Published - 20 Mar 2000

Funding

The authors acknowledge the Medical Research Council (MRC) for their support.

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Access to Document

10.1016/S0960-894X(00)00062-7

Cite this

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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. (C) 2000 Elsevier Science Ltd. All rights reserved.",

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AU - Nutt, David J.

AU - Tyacke, Robin

AU - Hudson, Alan L.

AU - Lewis, John W.

AU - Husbands, Stephen M.

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