학술논문
In Vivo Estimation of Imidazoline2 Binding Site Turnover
Document Type
Academic Journal
Author
Source
Annals of the New York Academy of Sciences. Jan 01, 2003 1009:367-370
Subject
Language
English
ISSN
0077-8923
Abstract
Turnover of imidazoline2 (I2) 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 I2 sites, as defined by [H]2BFI binding. Recovery was measured using radioligand binding and autoradiography to determine global and regional changes in I2 density. The density of I2 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 I2 site that reacts with BU99006 recovers rapidly and is independent of MAO.