Synthesis and evaluation of racemic [(11)C]NS2456 and enantiomers as selective serotonin reuptake radiotracers for PET.

  title={Synthesis and evaluation of racemic [(11)C]NS2456 and enantiomers as selective serotonin reuptake radiotracers for PET.},
  author={D. F. Smith and Dirk Bender and Katalin Marthi and Paul Cumming and S{\o}ren Baarsgaard Hansen and D. A. Peters and Elsebet {\O}stergaard Nielsen and J{\o}rgen Scheel-Kr{\"u}ger and Albert Gjedde},
  journal={Nuclear medicine and biology},
  volume={28 3},
[11C]‐NS 4194 versus [11C]‐DASB for PET imaging of serotonin transporters in living porcine brain
Pretreatment of pigs with citalopram did not reduce the uptake of either tracer in cerebellum, validating the use of that tissue as a nonbinding reference tissue for kinetic analysis of specific binding, and in several respects superior to [11C]‐NS 4194 for the detection of serotonin uptake sites by PET.
Synthesis of the serotonin transporter ligand (±)‐10‐methyl 3‐[6‐nitro‐(2‐quinolinyl)]‐3,10‐diazabicyclo‐[4.3.1]‐decane ([11C‐methyl]NS 2495) and first in vivo results
The serotonin transporter ligand (±)-10-[11C]-methyl 3-[6-nitro-(2-quinolinyl)]-3,10-diazabicyclo-[4.3.1]-decane ([11C-methyl]NS 2495) was synthesized via a methylation reaction with [11C]methyl iodide, and the specific radioactivity was found to be 1.8 GBq/μmol.
Synthesis of (±) 3‐(6‐nitro‐2‐quinolinyl)‐[9‐methyl‐11C]‐3,9‐diazabicyclo‐[4.2.1]‐nonane ([11C‐methyl]NS 4194)
(±) 3-(6-Nitro-2-quinolinyl)-[9-methyl-11C]-3,9-diazabicyclo-[4.2.1]-nonane ([11C-methyl]NS 4194), a selective serotonin reuptake inhibitor (SSRI), was synthesised within 35 min after end of
Determination of lipophilicity and its use as a predictor of blood-brain barrier penetration of molecular imaging agents.
  • R. Waterhouse
  • Biology, Chemistry
    Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging
  • 2003
PET Neuroimaging in Pigs
Ten-years of PET findings on neuromolecular processes in the living porcine brain are reviewed and, whenever possible, PET findings in pigs are related to those obtained in humans.
Stereoselective neuroimaging in vivo
The use of pigs in neuroscience: Modeling brain disorders


Uptake and distribution of a new SSRI, NS2381, studied by PET in living porcine brain
Radioligands for the study of the 5-HT transporter in vivo.
Among the various specific 5-HT uptake inhibitors only [(123)I]iodo-nitroquipazine for single photon emission computed tomography (SPECT) and [11C]-McN5652 for PET appear to meet the criteria of a useful radioligand.
Kinetics of the uptake of [3H]paroxetine in the rat brain
Binding was nearly absent from cerebellum and was highest in the dorsal raphé, superior colliculus, dorsal hypothalamus, and entorhinal cortex, but did not reach equilibrium in four hours of tracer circulation.
Graphical Analysis of Reversible Radioligand Binding from Time—Activity Measurements Applied to [N-11C-Methyl]-(−)-Cocaine PET Studies in Human Subjects
  • J. Logan, J. Fowler, D. Christman
  • Biology
    Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism
  • 1990
It can be shown that, for many systems, linearity is effectively reached some time before this, and this method provides an easy, rapid method for comparison of the reproducibility of repeated measures in a single subject, for longitudinal or drug intervention protocols, or for comparing experimental results between subjects.
Stereochemistry in the analysis of drug‐action. Part II