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TPCNE—A novel SPET tracer for the sigma‐1 receptor: First human studies and in vivo haloperidol challenge by James M. Stone; Erik Årstad; Kjell Erlandsson; Rikki N. Waterhouse; Peter J. Ell; Lyn S. Pilowsky is a Neuroscience article available to read on EtoBox.
What is TPCNE—A novel SPET tracer for the sigma‐1 receptor: First human studies and in vivo haloperidol challenge about?
## Abstract [^123^I]TPCNE (1(__trans__‐[^123^I]iodopropen‐2‐yl)‐4‐[(4‐cyanophenoxy)methyl] piperidine; __K~i~__ = 0.67 nM; log __P__ = 3.36) is a novel sigma‐1 receptor SPET ligand. In this study, we developed an optimized labeling method for [^123^I]TPCNE and investigated the kinetics, binding characteristics, and whole‐body distribution of this tracer for the first time in humans. We also performed a challenge with the sigma‐1 receptor antagonist haloperidol against [^123^I]TPCNE. Seven healthy volunteers were recruited. Dynamic brain SPET scans were performed following i.v. administration of 185 MBq [^123^I]TPCNE in all seven subjects. Three of the subjects were given oral haloperidol (2.5 mg) ∼1 h before the scan. The dynamic data were analyzed with both reversible and irreversible compartmental models. [^123^I]TPCNE showed high uptake in brain and liver. All non‐haloperidol‐treated subjects showed a high whole‐brain uptake (average: 8.7% of injected activity). No significant clearance of the tracer was seen up to 30 h post injection. In the haloperidol‐treated subjects, the time–activity curves clearly demonstrated clearance of the tracer from the brain. Regional radioactivity
Who reads TPCNE—A novel SPET tracer for the sigma‐1 receptor: First human studies and in vivo haloperidol challenge?
It is typically read by researchers, students, and practitioners in Neuroscience.
- Author
- James M. Stone; Erik Årstad; Kjell Erlandsson; Rikki N. Waterhouse; Peter J. Ell; Lyn S. Pilowsky
- Publisher
- John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 0887-4476)
- Published
- 2006
- Language
- EN
- Field
- Neuroscience (Life Sciences)