Evaluation of S-[11C]citalopram as a radioligand for in vivo labelling of 5-hydroxytryptamine uptake sites.
The biologically active S-enantiomer of [N-methyl-11C]citalopram was evaluated as a radioligand for in vivo labelling of the 5-hydroxytryptamine uptake site in brain, using ex vivo tissue counting in rats and positron emission tomography in man. In rats, the maximal signal for total versus non-specific binding was approx. 2 at 60-120 min after radioligand injection. Subsequent studies in man failed to identify a specific signal over a 90 min scanning period, due to prolonged retention of non-specific label.
Hume
S P
SP
MRC Cyclotron Unit, Hammersmith Hospital, London, England.
Lammertsma
A A
AA
Bench
C J
CJ
Pike
V W
VW
Pascali
C
C
Cremer
J E
JE
Dolan
R J
RJ
D000818:Animals; D001921:Brain / Q000378:metabolism; D002250:Carbon Radioisotopes; D015283:Citalopram / Q000378:metabolism*; D008297:Male; D011869:Radioligand Assay; D051381:Rats; D017207:Rats, Sprague-Dawley; D012701:Serotonin / Q000378:metabolism*; D013237:Stereoisomerism; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D015283:Citalopram; D012701:Serotonin