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

@article{Sby2002Lu2L,
  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},
  journal={Neuropharmacology},
  year={2002},
  volume={43},
  pages={95-100}
}
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Discovery and development of brain-penetrant 18F-labeled radioligands for neuroimaging of the sigma-2 receptors
Synthesis and in vitro evaluation of tetrahydroisoquinolines with pendent aromatics as sigma-2 (σ2) selective ligands.
TLDR
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.
Synthesis and pharmacological evaluation of ¹¹C-labeled piperazine derivative as a PET probe for sigma-2 receptor imaging.
Design, Radiosynthesis and Preliminary Biological Evaluation in Mice of a Brain-Penetrant 18F-Labelled σ2 Receptor Ligand
TLDR
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
TLDR
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.
Development of 3,4-dihydroisoquinolin-1(2H)-one derivatives for the Positron Emission Tomography (PET) imaging of σ₂ receptors.
Characterization of pulmonary sigma receptors by radioligand binding.
Sigma-2 receptor binding is decreased in female, but not male, APP/PS1 mice.
Imaging the Sigma-2 Receptor for Diagnosis and Prediction of Therapeutic Response
TLDR
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.
TLDR
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.
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References

SHOWING 1-10 OF 18 REFERENCES
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.
TLDR
The object of the study was to determine the structural factors governing sigma 1/sigma 2 affinity and selectivity within this class of compounds.
Trishomocubanes: novel σ-receptor ligands modulate amphetamine-stimulated [3H]dopamine release
Further characterization of [3H]ifenprodil binding to σ receptors in rat brain
A sigma-like binding site in rat pheochromocytoma (PC12) cells: decreased affinity for (+)-benzomorphans and lower molecular weight suggest a different sigma receptor form from that of guinea pig brain
Rat liver and kidney contain high densities of σ1 and σ2 receptors: characterization by ligand binding and photoaffinity labeling
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
TLDR
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.
[3H]1,3-di(2-tolyl)guanidine and [3H](+)pentazocine binding sites in the rat brain: Autoradiographic visualization of the putative sigma1 and sigma2 receptor subtypes
Autoradiographic distribution of [3H](+)-pentazocine and [3H]1,3-di-o-tolylguanidine (DTG) binding sites in guinea pig brain: a comparative study
Regional variation in the ratio of σ1 to σ2 binding in rat brain
Pharmacological identification of SM-21, the novel σ2 antagonist
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