Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand.
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.
Coates
P A
PA
School of Chemistry, University of Bristol, UK.
Grundt
P
P
Robinson
E S
ES
Nutt
D J
DJ
Tyacke
R
R
Hudson
A L
AL
Lewis
J W
JW
Husbands
S M
SM
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects; D054755:Imidazoline Receptors; D066298:In Vitro Techniques; D007668:Kidney / Q000187:drug effects / Q000378:metabolism; D008024:Ligands; D019920:Photoaffinity Labels; D051381:Rats; D018341:Receptors, Adrenergic, alpha-2 / Q000187:drug effects; D011955:Receptors, Drug / Q000187:drug effects*
D054755:Imidazoline Receptors; D008024:Ligands; D019920:Photoaffinity Labels; D018341:Receptors, Adrenergic, alpha-2; D011955:Receptors, Drug