In vivo estimation of imidazoline(2) binding site turnover.
Turnover of imidazoline(2) (I(2)) binding sites in the mouse and rat brain has been measured following an acute intravenous dose of BU99006. This ligand selectively and irreversibly knocks out I(2) sites, as defined by [(3)H]2BFI binding. Recovery was measured using radioligand binding and autoradiography to determine global and regional changes in I(2) density. The density of I(2) sites in brain recovered from BU99006 treatment with a half-life of 2.1 hours in mice and 4.3 hours in rats. Monoamine oxidase (MAO) activity and MAO binding density were unaltered in the brains of BU99006-treated animals. These data suggest that the I(2) site that reacts with BU99006 recovers rapidly and is independent of MAO.
Paterson
L M
LM
Psychopharmacology Unit, School of Medical Sciences, University of Bristol, Bristol BS8 1TD, UK.
Robinson
E S J
ES
Nutt
D J
DJ
Hudson
A L
AL
D000818:Animals; D001572:Benzofurans / Q000008:administration & dosage / Q000378:metabolism; D001665:Binding Sites; D001921:Brain / Q000166:cytology / Q000378:metabolism; D002462:Cell Membrane / Q000378:metabolism; D007093:Imidazoles / Q000008:administration & dosage / Q000378:metabolism; D054755:Imidazoline Receptors; D008297:Male; D051379:Mice; D008808:Mice, Inbred CBA; D008995:Monoamine Oxidase / Q000378:metabolism; D009419:Nerve Tissue Proteins / Q000378:metabolism; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D011955:Receptors, Drug / Q000378:metabolism*
C468012:BU 99006; D001572:Benzofurans; D007093:Imidazoles; D054755:Imidazoline Receptors; D009419:Nerve Tissue Proteins; D011955:Receptors, Drug; C103723:2-(2-benzofuranyl)-2-imidazoline; D008995:Monoamine Oxidase