[3H]nisoxetine: a new radioligand for norepinephrine uptake sites in brain.
[3H]Nisoxetine binds with high affinity (Kd = 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 Kd 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.
Tejani-Butt
S M
SM
Department of Psychiatry, University of Pennsylvania School of Medicine, Philadelphia.
Brunswick
D J
DJ
Frazer
A
A
D000818:Animals; D001596:Benzylamines / Q000494:pharmacology; D002540:Cerebral Cortex / Q000378:metabolism*; D005473:Fluoxetine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D008297:Male; D009638:Norepinephrine / Q000378:metabolism*; D011292:Premedication; D011869:Radioligand Assay; D051381:Rats; D011919:Rats, Inbred Strains
D001596:Benzylamines; D005473:Fluoxetine; C011386:nisoxetine; C012102:DSP 4; D009638:Norepinephrine