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

P A Coates; P Grundt; E S Robinson; D J Nutt; R Tyacke; A L Hudson; J W Lewis; S M Husbands

doi:10.1016/s0960-894x(00)00062-7

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

Bioorg Med Chem Lett. 2000 Mar 20;10(6):605-7. doi: 10.1016/s0960-894x(00)00062-7.

Authors

P A Coates¹, P Grundt, E S Robinson, D J Nutt, R Tyacke, A L Hudson, J W Lewis, S M Husbands

Affiliation

¹ School of Chemistry, University of Bristol, UK.

PMID: 10741563
DOI: 10.1016/s0960-894x(00)00062-7

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Binding, Competitive / drug effects
Brain Chemistry / drug effects
Imidazoline Receptors
In Vitro Techniques
Kidney / drug effects
Kidney / metabolism
Ligands
Photoaffinity Labels
Rats
Receptors, Adrenergic, alpha-2 / drug effects
Receptors, Drug / drug effects*

Substances

Imidazoline Receptors
Ligands
Photoaffinity Labels
Receptors, Adrenergic, alpha-2
Receptors, Drug