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Full-Text Articles in Social and Behavioral Sciences

Activation Of The Damage-Associated Molecular Pattern Receptor P2x7 Induces Interleukin-1b Release From Canine Monocytes, Iman Jalilian, Michelle Peranec, Belinda L. Curtis, Aine Seavers, Mari Spildrejorde, Vanessa Sluyter, Ronald Sluyter Jan 2012

Activation Of The Damage-Associated Molecular Pattern Receptor P2x7 Induces Interleukin-1b Release From Canine Monocytes, Iman Jalilian, Michelle Peranec, Belinda L. Curtis, Aine Seavers, Mari Spildrejorde, Vanessa Sluyter, Ronald Sluyter

Faculty of Science - Papers (Archive)

P2X7, a damage-associated molecular pattern receptor and adenosine 5'-triphosphate (ATP)-gated cation channel, plays an important role in the activation of the NALP3 inflammasome and subsequent release of interleukin (IL)-1β from human monocytes; however its role in monocytes from other species including the dog remains poorly defined. This study investigated the role of P2X7 in canine monocytes, including its role in IL-1β release. A fixed-time flow cytometric assay demonstrated that activation of P2X7 by extracellular ATP induces the uptake of the organic cation, YO-PRO-12+, into peripheral blood monocytes from various dog breeds, a process impaired by the specific P2X7 …


Metabolic Parameters And Emotionality Are Little Affected In G-Protein Coupled Receptor 12 (Gpr12) Mutant Mice, Elisabeth Frank, Yizhen Wu, Naomi Piyaratna, William James Body, P Snikeris, Timothy South, Anna-Karin Gerdin, Mikael Bjursell, Mohammad Bohlooly-Y, Leonard H. Storlien, Xu-Feng Huang Jan 2012

Metabolic Parameters And Emotionality Are Little Affected In G-Protein Coupled Receptor 12 (Gpr12) Mutant Mice, Elisabeth Frank, Yizhen Wu, Naomi Piyaratna, William James Body, P Snikeris, Timothy South, Anna-Karin Gerdin, Mikael Bjursell, Mohammad Bohlooly-Y, Leonard H. Storlien, Xu-Feng Huang

Faculty of Health and Behavioural Sciences - Papers (Archive)

Background: G-protein coupled receptors (GPR) bear the potential to serve as yet unidentified drug targets for psychiatric and metabolic disorders. GPR12 is of major interest given its putative role in metabolic function and its unique brain distribution, which suggests a role in emotionality and affect. We tested Gpr12 deficient mice in a series of metabolic and behavioural tests and subjected them to a well-established high-fat diet feeding protocol. Methodology/Principal Findings: Comparing the mutant mice with wild type littermates, no significant differences were seen in body weight, fatness or weight gain induced by a high-fat diet. The Gpr12 mutant mice displayed …


Novel Olanzapine Analogues Presenting A Reduced H1 Receptor Affinity And Retained 5ht2a/D2 Binding Affinity Ratio, Somayeh Jafari, Marc E. Bouillon, Xu-Feng Huang, Stephen G. Pyne, Francesca Fernandez-Enright Jan 2012

Novel Olanzapine Analogues Presenting A Reduced H1 Receptor Affinity And Retained 5ht2a/D2 Binding Affinity Ratio, Somayeh Jafari, Marc E. Bouillon, Xu-Feng Huang, Stephen G. Pyne, Francesca Fernandez-Enright

Faculty of Science, Medicine and Health - Papers: part A

Background Olanzapine is an atypical antipsychotic drug with high clinical efficacy, but which can cause severe weight gain and metabolic disorders in treated patients. Blockade of the histamine 1 (H1) receptors is believed to play a crucial role in olanzapine induced weight gain, whereas the therapeutic effects of this drug are mainly attributed to its favourable serotoninergic 2A and dopamine 2 (5HT2A/D2) receptor binding affinity ratios. Results We have synthesized novel olanzapine analogues 8a and 8b together with the already known derivative 8c and we have examined their respective in vitro affinities for the 5HT2A, D2, and H1 receptors. Conclusions …


P2x7 Receptor Activation Mediates Organic Cation Uptake Into Human Myeloid Leukaemic Kg-1 Cells, Safina Gadeock, Aleta Pupovac, Vanessa Sluyter, Mari Spildrejorde, Ronald Sluyter Jan 2012

P2x7 Receptor Activation Mediates Organic Cation Uptake Into Human Myeloid Leukaemic Kg-1 Cells, Safina Gadeock, Aleta Pupovac, Vanessa Sluyter, Mari Spildrejorde, Ronald Sluyter

Faculty of Science - Papers (Archive)

The P2X7 purinergic receptor is an ATP-gated cation channel with an emerging role in neoplasia. In this study we demonstrate that the human KG-1 cell line, a model of acute myelogenous leukaemia, expresses functional P2X7. RT-PCR and immunochemical techniques demonstrated the presence of P2X7 mRNA and protein respectively in KG-l cells, as well as in positive control multiple myeloma RPMI 8226 cells. Flow cytometric measurements demonstrated that ATP induced ethidium(+) uptake into KG-l cells suspended in sucrose medium (EC(50) of ∼3 μM), but not into cells in NaCl medium. In contrast, ATP induced ethidium(+) uptake into RPMI 8226 cells suspended …