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Non-peptide ligands in the characterization of peptide receptors at the interface between neuroendocrine and mental diseases

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Author(s): Margit Pissarek | Ulrich Disko

Journal: World Journal of Neuroscience
ISSN 2162-2000

Volume: 03;
Issue: 02;
Start page: 100;
Date: 2013;
Original page

Keywords: Feeding Receptor | Hypothalamus | Neuropeptide | Non-Peptide Antagonist | PET | SPECT

ABSTRACT
Hypothalamic receptors for neuropeptide Y, melaninconcentrating hormone, melanocortins and orexins/ hypocretins as well as for the downstream signaling corticotrophic factor have been discussed broadly for their influence on food intake and reward but also on several psychiatric disorders. For the development of non-peptide ligands for the in vivo detection of alterations in density and affinity of such G-protein coupled (GPCRs) peptide receptors the requirements to affinity and pharmacokinetics have been shifted to thresholds markedly distict from classical GPCRs to dissociation constants < 0.5 nM, partition coefficients log P < 3.5 and transcellular transport ratios, e.g. for the permeability glycoprotein transporter, below 3. Nevertheless, a multitude of compounds has been reported originally as potential therapeutics in the treatment of obesity among which some are suitable candidates for labeling as PET or SPECT-tracers providing receptor affinities even below 0.1 nM. These could be unique tools not only for better understanding of the mechanism of obesity but also for investigations of extrahypothalamic role of “feeding receptors” at the interface between neuroendocrine and mental diseases.
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