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Munro, T.A., Berry, L.M., Van’t Veer, A., Beguin, C., Carrol Ivy, F., Zhao, Z., Carlezon, W.A. and Cohen, B.M. (2012) Long-Acting κ Opioid Antagonists Nor-BNI, GNTI and JDTic: Pharmacokinetics in Mice and Lipophilicity. BMC Pharmacology, 12, 5. http://dx.doi.org/10.1186/1471-2210-12-5

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• TITLE: Neuropeptide Receptors in Pain Circuitries: Useful Targets for CNS Imaging with Non-Peptide Ligands Suitable for PET?

  AUTHORS: Margit Pissarek

  KEYWORDS: Neuropeptide Receptors, PET, Brain, Pain, Spinal Cord

  JOURNAL NAME: World Journal of Neuroscience, Vol.4 No.4, August 14, 2014

  ABSTRACT: Neuropeptide receptors of the brain and spinal cord are parts of the pain circuits targeted by analgesic drugs. Some of these receptors have been found in the central nervous system as well as in intracranial vascular structures and achieved revival of attention because of their role in acute and chronic pain syndromes. A number of them are of high clinical relevance for e.g. migraine. Others participate in symptoms of rare diseases like amyotrophic lateral sclerosis. Here we will focus on five of the neuropeptide receptors and their non-peptide ligands potentially or already successfully used as PET probes. Opioid receptors and neurotensin receptors are known to mediate analgesic actions. Bradykinin and calcitonin gene-related peptide (CGRP) receptors are known to be involved in the regulation of vascular tone and inflammatory responses, and neurokinin receptors play a role in the occurrence of pain perception in a rather indirect manner. Most experiences as PET tracers have been gathered with opioid receptor ligands and neurokinin receptor ligands. The most innovative fields revealed by the studies summarized in this report are the ligands of κ opioid receptors and CGRP receptors for which a first PET tracer was presented recently.