Preclinical Evaluation and Nonhuman Primate Receptor Occupancy Study of
| Autor: | Hartmuth C, Kolb, Olivier, Barret, Anindya, Bhattacharya, Gang, Chen, Cristian, Constantinescu, Chaofeng, Huang, Michael, Letavic, Gilles, Tamagnan, Chunfang A, Xia, Wei, Zhang, Anna Katrin, Szardenings |
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| Rok vydání: | 2018 |
| Předmět: |
Inflammation
Male Mice Knockout Radiochemistry Brain In Vitro Techniques Ligands Macaca mulatta Permeability Rats Kinetics Pyrimidines Treatment Outcome Blood-Brain Barrier Positron-Emission Tomography Animals Humans Female Tissue Distribution Receptors Purinergic P2X7 Radiopharmaceuticals Peptides Protein Binding |
| Zdroj: | Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 60(8) |
| ISSN: | 1535-5667 |
| Popis: | The P2X7 receptor is an adenosine triphosphate-gated ion channel, which is abundantly expressed in glial cells within the central nervous system and in the periphery. P2X7 receptor activation leads to the release of the proinflammatory cytokine IL-1β in the brain, and antagonism of the P2X7 receptor is a novel therapeutic strategy to dampen adenosine triphosphate-dependent IL-1β signaling. PET ligands for the P2X7 receptor will not only be valuable to assess central target engagement of drug candidates but also hold promise as surrogate markers of central neuroinflammation. Herein we describe the in vitro and in vivo evaluation of |
| Databáze: | OpenAIRE |
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