N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline, an irreversible receptor inactivator, as a tool for measurement of alpha 2-adrenoceptor occupancy in vivo.

In rats treatment with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) induces a dose-dependent decrease in the number of alpha 2-adrenoceptors. Prior injection of alpha-adrenergic agents such as yohimbine and clonidine protect alpha 2-adrenoceptors against the effects of EEDQ. The ED50 values for yohimbine and clonidine were 10.27 and 5.83 mumol/kg, respectively.