Quantitative autoradiography of serotonin uptake sites in rat brain using [3H]cyanoimipramine.
The binding of [3H]cyanoimipramine to serotonin uptake sites in rat brain slices was studied using quantitative autoradiography. Binding was of high affinity and was to a single class of binding site. This is in contrast to results previously obtained by others with [3H]imipramine where two binding sites were observed. The sites labeled by [3H]cyanoimipramine had properties consistent with this ligand labeling serotonin uptake sites, as: (1) binding is displaced by drugs which are potent inhibitors of serotonin uptake but not by drugs which are weak inhibitors of uptake; (2) binding is dependent on the presence of sodium ions as is the uptake of serotonin; (3) binding is almost completely eliminated in the brains of rats lesioned by the serotonin neurotoxin 5,7-dihydroxytryptamine; (4) the distribution of binding sites throughout the rat brain is highly correlated with that found previously for [3H]indalpine, a potent serotonin uptake inhibitor, and for [3H]imipramine. The properties of binding of [3H]cyanoimipramine make it an ideal ligand for the quantitative autoradiography of serotonin uptake sites.
Kovachich
G B
GB
Neuropsychopharmacology Unit, Veterans Administration Medical Center, Philadelphia, PA 19104.
Aronson
C E
CE
Brunswick
D J
DJ
Frazer
A
A
D015057:1-Naphthylamine / Q000031:analogs & derivatives / Q000378:metabolism; D000818:Animals; D001345:Autoradiography; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D005473:Fluoxetine / Q000378:metabolism; D007099:Imipramine / Q000031:analogs & derivatives* / Q000378:metabolism; D007700:Kinetics; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000378:metabolism*; D020280:Sertraline; D015031:Zimeldine / Q000031:analogs & derivatives / Q000378:metabolism
D011985:Receptors, Serotonin; D005473:Fluoxetine; C024316:cianopramine; D015031:Zimeldine; C017578:norzimelidine; D015057:1-Naphthylamine; D007099:Imipramine; D020280:Sertraline