Potential of [11C]DASB for measuring endogenous serotonin with PET: binding studies.
The serotonin transporter radioligand [11C]-3-amino-4-(2-dimethylaminomethylphenylsulfanyl)-benzonitrile, or [11C]DASB, was examined in order to assess its potential for measuring fluctuations in endogenous serotonin concentrations with positron emission tomography. Binding characteristics of [11C]DASB and the propensity for serotonin to displace the tracer were explored in rat brain homogenates. Experiments showed that serotonin displaced [11C]DASB in vitro. Ex vivo experiments performed after tranylcypromine injection (3 or 15 mg/kg) showed a dose-dependent trend in radioactivity uptake and suggested that serotonin may compete with [11C]DASB for transporter binding.
Lundquist
Pinelopi
P
Division of Pharmacokinetics and Drug Therapy, Department of Pharmaceutical Biosciences, Uppsala University, SE-751 24 Uppsala, Sweden. pinelopi.lundquist@farmbio.uu.se
Wilking
Helena
H
Höglund
A Urban
AU
Sandell
Johan
J
Bergström
Mats
M
Hartvig
Per
P
Långström
Bengt
B
D000814:Aniline Compounds / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D005240:Feasibility Studies; D008297:Male; D008657:Metabolic Clearance Rate; D018377:Neurotransmitter Agents / Q000378:metabolism; D009928:Organ Specificity; D049268:Positron-Emission Tomography / Q000379:methods*; D011485:Protein Binding; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D012701:Serotonin / Q000378:metabolism*; D013440:Sulfides / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D014018:Tissue Distribution
C412822:3-amino-4-(2-dimethylaminomethylphenylsulfanyl)benzonitrile; D000814:Aniline Compounds; D018377:Neurotransmitter Agents; D019275:Radiopharmaceuticals; D013440:Sulfides; D012701:Serotonin