Chemical Name: 2-(Phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl-3-pyridinecarboxamide
Biological ActivityPotent and selective P2X7 antagonist (pIC50 values are 8.3, 7.5 and 7.2 for human, mouse and rat receptors respectively). Selective over a panel of 50 other receptors, ion channels and transporters. Reduces BzATP-induced IL-1β release from monocytes in vitro and from rat brain in vivo. Attenuates amphetamine-induced hyperactivity in rats. Brain penetrant.
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Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567.
Bhattacharya et al.
Synthesis and pharmacological characterization of two novel, brain penetrating P2X7 antagonists.
Letavic et al.
ACS Med.Chem.Lett., 2013;12:419
Citation for JNJ 47965567
The citations listed below are publications that use Tocris products. Selected citations for JNJ 47965567 include:
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Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage.
Authors: Uderhardt Et al.
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Average Rating: 4.3 (Based on 3 Reviews)
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DMSO dilution 100 μM
I have used this product emulsified in 30% sulphoxymethylester, and injected them sub-cutaneously to study IL-1beta release mechanism in the hippocampus of the brain. I am currently working on its effect on hippocampal neurons in culture.
Used to block a potentially P2X7-dependent process, but no effect was observed. No positive control so unsure if the drug actually blocked its target. More experiments needed.