Cutamesine Overcomes REM Sleep Deprivation-Induced Memory Loss: Relationship to Sigma-1 Receptor Occupancy

@article{Ramakrishnan2014CutamesineOR,
  title={Cutamesine Overcomes REM Sleep Deprivation-Induced Memory Loss: Relationship to Sigma-1 Receptor Occupancy},
  author={Nisha Kuzhuppilly Ramakrishnan and Marianne Schepers and Gert Luurtsema and Csaba Nyakas and Philip H. Elsinga and Kiichi Ishiwata and Rudi A. Dierckx and Aren van Waarde},
  journal={Molecular Imaging and Biology},
  year={2014},
  volume={17},
  pages={364-372}
}
PurposeRapid eye movement (REM) sleep deprivation (SD) decreases cerebral sigma-1 receptor expression and causes cognitive deficits. Sigma-1 agonists are cognitive enhancers. Here, we investigate the effect of cutamesine treatment in the REM SD model.ProceduresSigma-1 receptor occupancy (RO) in the rat brain by cutamesine was determined using 1-[2-(3,4-dimethoxyphenethyl)]-4-(3-phenylpropyl)piperazine ([11C]SA4503) and positron emission tomography (PET), and tissue cutamesine levels were… 
University of Groningen Sigma-1 agonist binding in the aging rat brain : A microPET study with [ 11 C ] SA 4503
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 were reduced.
Assessment of sigma-1 receptor occupancy in mice with non-radiolabelled FTC-146 as a tracer
TLDR
Brain regional distribution and binding inhibition upon pretreatment were comparable with data reported with labeled [18F]FTC-146, and there was a dose-dependent decrease in brain regional FTC-146 binding in pretreated mice.
Revisiting the sigma-1 receptor as a biological target to treat affective and cognitive disorders
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TLDR
The Inhibition and Occupancy plots yielded the best fits to the data, according to the goodness of fit parameters, due primarily to the absent commingling of the dependent and independent variables tested with the Saturation ( original Lassen) plot.
In Vivo Receptor Visualization and Evaluation of Receptor Occupancy with Positron Emission Tomography.
TLDR
Work in this area is reviewed, focusing on the chemical structures of reported PET tracers, their Ki/Kd values, and the physical properties relevant to target receptor selectivity, focusing especially on LogD and LogP as important physical properties that can be easily compared across a range of studies.
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.

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