Drug inhibition indicates a single-site model of the 5-HT uptake site/antidepressant binding site in rat and human brain.
Drug inhibition against [3H]paroxetine binding to rat cortex and human putamen was investigated in saturation experiments. The addition of 5-HT, imipramine, citalopram and clomipramine all produced changes in apparent binding affinity (Kd) without changes in the number of binding sites (Bmax). These data suggest that there is no heterogeneity of specific [3H]paroxetine binding, supporting a single site model of the 5-HT uptake site and antidepressant binding site.
Marcusson
J O
JO
Department of Geriatric Medicine, University of Umea, Sweden.
Andersson
A
A
Bäckström
I
I
D000368:Aged; D000818:Animals; D000928:Antidepressive Agents / Q000378:metabolism*; D001665:Binding Sites; D001921:Brain / Q000378:metabolism*; D015283:Citalopram / Q000494:pharmacology; D002997:Clomipramine / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D008875:Middle Aged; D017374:Paroxetine; D010880:Piperidines / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D012701:Serotonin / Q000378:metabolism*
D000928:Antidepressive Agents; D010880:Piperidines; D015283:Citalopram; D012701:Serotonin; D017374:Paroxetine; D002997:Clomipramine