Abstract

[ 3H]Nisoxetine binds with high affinity (K d = 0.7 nM) and selectivity to a homogenous population of sites associated with the uptake of norepinephrine. Specific [ 3H]nisoxetine binding to rat cortical homogenates was saturable, sodium-dependent and averaged 90% of total binding at its K d concentration. Pretreatment with the neurotoxin DSP-4 resulted in 95% decrease in binding. [ 3H]Nisoxetine exhibits superior properties to radioligands previously used and appears to be the radioligand of choice for studies involving uptake sites for norepinephrine.

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