PET evaluation of a tetracyclic, atypical antidepressant, [N-methyl-11C]mianserin, in the living porcine brain.
We synthesized [N-methyl-11C]mianserin by alkylation of N-desmethyl mianserin with [11C]methyl iodide followed by HPLC purification. We used PET for determining the regional cerebral pharmacokinetics of the radiotracer in anesthetized swine. [N-methyl-11C]Mianserin entered most brain regions readily (range of K1 values: 0.66-1.13), reaching highest levels in the basal ganglia and thalamus. The binding potential of [N-methyl-11C]mianserin was relatively low (range: 0.07-0.50), but regional differences were nonetheless observed, with highest values in the temporal cortex and lowest values in the brainstem. These PET findings, which are the first ones for a tetracyclic, antidepressant drug, show that [N-methyl-11C]mianserin has only a limited degree of regional specificity of binding in the living brain.
Marthi
K
K
PET Center, Aarhus University Hospital, Aarhus, Denmark. marthi@tki.aak.bme.hu
Bender
D
D
Watanabe
H
H
Smith
D F
DF
D000818:Animals; D018687:Antidepressive Agents, Second-Generation / Q000493:pharmacokinetics*; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D005260:Female; D007553:Isotope Labeling; D008803:Mianserin / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics*; D013552:Swine; D014055:Tomography, Emission-Computed
C465865:(N-methyl)mianserin; D018687:Antidepressive Agents, Second-Generation; D019275:Radiopharmaceuticals; D008803:Mianserin