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.

Subject headings

MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)

MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)

Keyword

Aniline Compounds/*pharmacokinetics/*therapeutic use

Animals

Brain/*metabolism/*radionuclide imaging

Feasibility Studies

Male

Metabolic Clearance Rate

Neurotransmitter Agents/metabolism

Organ Specificity

Positron-Emission Tomography/*methods

Protein Binding

Radiopharmaceuticals/diagnostic use/pharmacokinetics

Rats

Rats; Sprague-Dawley

Research Support; Non-U.S. Gov't

Serotonin/*metabolism

Sulfides/*pharmacokinetics/*therapeutic use

Tissue Distribution

PHARMACY

FARMACI

Publication and Content Type

ref (subject category)

art (subject category)