Paterson L M, Robinson E S J, Nutt D J, Hudson A L
Psychopharmacology Unit, School of Medical Sciences, University of Bristol, Bristol BS8 1TD, UK.
Ann N Y Acad Sci. 2003 Dec;1009:367-70. doi: 10.1196/annals.1304.049.
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.
在给小鼠和大鼠静脉注射一剂急性剂量的BU99006后，已对小鼠和大鼠脑中咪唑啉（2）（I（2））结合位点的周转率进行了测量。如通过[³H]2BFI结合所定义的，该配体选择性且不可逆地消除I（2）位点。使用放射性配体结合和放射自显影术测量恢复情况，以确定I（2）密度的整体和区域变化。用BU99006处理后，脑中I（2）位点的密度恢复，在小鼠中的半衰期为2.1小时，在大鼠中为4.3小时。在接受BU99006处理的动物脑中，单胺氧化酶（MAO）活性和MAO结合密度未发生改变。这些数据表明，与BU99006反应的I（2）位点恢复迅速且独立于MAO。
