Premium
In Vivo Estimation of Imidazoline 2 Binding Site Turnover
Author(s) -
PATERSON LM,
ROBINSON ESJ,
NUTT DJ,
HUDSON AL
Publication year - 2003
Publication title -
annals of the new york academy of sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.712
H-Index - 248
eISSN - 1749-6632
pISSN - 0077-8923
DOI - 10.1196/annals.1304.049
Subject(s) - imidazoline receptor , in vivo , binding site , radioligand , monoamine oxidase , ligand (biochemistry) , chemistry , radioligand assay , medicine , endocrinology , biochemistry , biology , receptor , enzyme , microbiology and biotechnology
A bstract : 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.