Lu 28-179 labels a σ2-site in rat and human brain

  title={Lu 28-179 labels a $\sigma$2-site in rat and human brain},
  author={Karina Kr{\o}yer S{\o}by and Jens D Mikkelsen and Eddi Meier and Christian Thomsen},
Synthesis and in vitro evaluation of tetrahydroisoquinolines with pendent aromatics as sigma-2 (σ2) selective ligands.
The flexibility and length of the carbon linker and the carboxylic acid moiety are confirmed to be key to the exceptional binding affinity and selectivity for this active series of σ2 receptor ligands.
Design, Radiosynthesis and Preliminary Biological Evaluation in Mice of a Brain-Penetrant 18F-Labelled σ2 Receptor Ligand
Results indicate that the herein developed σ2 receptor ligand [18F]RM273 has potential to assess by non-invasive molecular imaging the correlation between the availability of ρ2 receptors and properties of brain tumors such as tumor proliferation or resistance towards particular therapies.
Sigma-1 Agonist Binding in the Aging Rat Brain: a MicroPET Study with [11C]SA4503
Some areas showed reductions of ligand binding with aging whereas binding in other areas (cortex) was not significantly affected, and changes of total distribution volume (VT) and binding potential (BPND) of the tracer.
Characterization of pulmonary sigma receptors by radioligand binding.
Imaging the Sigma-2 Receptor for Diagnosis and Prediction of Therapeutic Response
Two σ binding site subtypes were distinguished based on differences in their drug-binding profiles and molecular weight and suggest that σ1 receptors may modulate the activity of GABA and NMDA receptors in the CNS.
Development of molecular probes for imaging sigma-2 receptors in vitro and in vivo.
The development and use of sigma(2) receptor ligands are reviewed, and how these ligands have been used with a variety of in vitro and in vivo models to gain a greater understanding of the role this receptor plays in cancer.


Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.
The object of the study was to determine the structural factors governing sigma 1/sigma 2 affinity and selectivity within this class of compounds.
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
Potent anxiolytic activity in the black/white box exploration test in rats was found with the two most prominent sigma 2 ligands Lu 29-253 and Lu 28-179, and good penetration into the CNS was documented both after subcutaneous and peroral administration of Lu28-179 by ex vivo binding studies.
Pharmacological identification of SM-21, the novel σ2 antagonist