Open Access. Powered by Scholars. Published by Universities.®
Articles 1 - 8 of 8
Full-Text Articles in Medicine and Health Sciences
Key Structural Determinants In The Agonist Binding Loops Of Human Β2 And Β4 Nicotinic Acetylcholine Receptor Subunits Contribute To Α3Β4 Subtype Selectivity Of Α-Conotoxins, Hartmut Cuny, Shiva N. Kompella, Han Shen Tae, Rilei Yu, David J. Adams
Key Structural Determinants In The Agonist Binding Loops Of Human Β2 And Β4 Nicotinic Acetylcholine Receptor Subunits Contribute To Α3Β4 Subtype Selectivity Of Α-Conotoxins, Hartmut Cuny, Shiva N. Kompella, Han Shen Tae, Rilei Yu, David J. Adams
Illawarra Health and Medical Research Institute
α-Conotoxins represent a large group of pharmacologically active peptides that antagonize nicotinic acetylcholine receptors (nAChRs). The α3β4 nAChR, a predominant subtype in the peripheral nervous system, has been implicated in various pathophysiological conditions. As many α-conotoxins have multiple pharmacological targets, compounds specifically targeting individual nAChR subtypes are needed. In this study, we performed mutational analyses to evaluate the key structural components of human β2 and β4 nAChR subunits that determine α-conotoxin selectivity for α3β4 nAChR. α-Conotoxin RegIIA was used to evaluate the impact of non-conserved human β2 and β4 residues on peptide affinity. Two mutations, α3β2[T59K] and α3β2[S113R], strongly enhanced …
Dha Prevents Altered 5-Ht1a, 5-Ht2a, Cb1 And Gabaa Receptor Binding Densities In The Brain Of Male Rats Fed A High-Saturated-Fat Diet, Yinghua Yu, Yizhen Wu, Craig Patch, Zhixiang Wu, Alexander Szabo, Duo Li, Xu-Feng Huang
Dha Prevents Altered 5-Ht1a, 5-Ht2a, Cb1 And Gabaa Receptor Binding Densities In The Brain Of Male Rats Fed A High-Saturated-Fat Diet, Yinghua Yu, Yizhen Wu, Craig Patch, Zhixiang Wu, Alexander Szabo, Duo Li, Xu-Feng Huang
Illawarra Health and Medical Research Institute
Low levels of docosahexaenoic acid (DHA) have been linked to a number of mental illnesses such as memory loss, depression and schizophrenia. While supplementation of DHA is beneficial in improving memory and cognition, the influence of dietary fats on the neurotransmitters and receptors involved in cognitive function is still not known. The aim of this study was to investigate serotonin receptor (5-HT1A and 5-HT2A), cannabinoid receptor (CB1) and gamma-aminobutyric acid type A (GABAA) receptor binding densities in the brain of male rats fed a high-saturated-fat (HF) diet, as well as the effect of DHA supplementation …
Effects Of Olanzapine And Betahistine Co-Treatment On Serotonin Transporter, 5-Ht2a And Dopamine D2 Receptor Binding Density, Jiamei Lian, Xu-Feng Huang, Nagesh Pai, Chao Deng
Effects Of Olanzapine And Betahistine Co-Treatment On Serotonin Transporter, 5-Ht2a And Dopamine D2 Receptor Binding Density, Jiamei Lian, Xu-Feng Huang, Nagesh Pai, Chao Deng
Illawarra Health and Medical Research Institute
Olanzapine is widely used in treating multiple domains of schizophrenia symptoms but induces serious metabolic side-effects. Recent evidence has showed that co-treatment of betahistine (a histaminergic H1 receptor agonist and H3 receptor antagonist) is effective for preventing olanzapine-induced weight gain/obesity, however it is not clear whether this co-treatment affects on the primary therapeutic receptor binding sites of olanzapine such as serotonergic 5-HT2A receptors (5-HT2AR) and dopaminergic D2 receptors (D2R). Therefore, this study investigated the effects of this co-treatment on 5-HT2AR, 5-HT transporter (5-HTT) and D2R bindings in various brain regions involved in antipsychotic efficacy. Female Sprague Dawley rats were administered …
Reduction Of Histamine H1 Receptor Binding Induced By High-Fat Diet Can Be Prevented By Dha And Dietary Fiber In Specific Brain Areas Of Male Rats, Zhixiang Wu, Yinghua Yu, Yizhen Wu, Craig S. Patch, Alexander Szabo, Xu-Feng Huang
Reduction Of Histamine H1 Receptor Binding Induced By High-Fat Diet Can Be Prevented By Dha And Dietary Fiber In Specific Brain Areas Of Male Rats, Zhixiang Wu, Yinghua Yu, Yizhen Wu, Craig S. Patch, Alexander Szabo, Xu-Feng Huang
Illawarra Health and Medical Research Institute
High-fat (HF) diet and obesity are risk factors for a number of mental health problems including depression, cognitive dysfunction, dementia, and neurodegenerative diseases. Histamine H1 receptors (H1Rs) are involved in many of these conditions. This study examined H1R receptor binding density in the brain of male rats fed a high-saturated fat (HF) diet, as well as the effect of docosahexaenoic acid (DHA), galacto-oligosaccharide (GOS) and resistant starch (RS) supplementation of HF diet. Alterations of H1R expression in the post-mortem rat brain were detected by [ 3H]-pyrilamine binding autoradiography. We found that HF diet significantly decreased H1R binding densities in the …
Proteogenomic Analyses Of Lingo-1 And The Nogo Receptor In Schizophrenia, J Andrews, K Newell, F Fernandez
Proteogenomic Analyses Of Lingo-1 And The Nogo Receptor In Schizophrenia, J Andrews, K Newell, F Fernandez
Illawarra Health and Medical Research Institute
No abstract provided.
Functional Expression Of The Damage-Associated Molecular Pattern Receptor P2x7 On Canine Kidney Epithelial Cells, Iman Jalilian, Mari Spildrejorde, Aine Seavers, Belinda L. Curtis, Jason D. Mcarthur, Ronald Sluyter
Functional Expression Of The Damage-Associated Molecular Pattern Receptor P2x7 On Canine Kidney Epithelial Cells, Iman Jalilian, Mari Spildrejorde, Aine Seavers, Belinda L. Curtis, Jason D. Mcarthur, Ronald Sluyter
Illawarra Health and Medical Research Institute
Epithelial cells are important in inflammation and immunity. In this study, we examined if Madin-Darby canine kidney (MDCK) epithelial cells express functional P2X7 receptors, which bind the damage-associated molecular pattern extracellular adenosine 5'-triphosphate (ATP). Reverse transcription (RT)-PCR and immunoblotting revealed the expression of P2X7 in MDCK cells. A flow cytometric assay demonstrated that ATP or 2'(3')-O-(4-benzoylbenzoyl)ATP induced ethidium(+) uptake into MDCK cells, and that this process was impaired by the P2X7 antagonists KN-62 and A438079. RT-PCR also demonstrated the presence of Toll-like receptor 4, NALP3, caspase-1, interleukin-1β and interleukin-18 in MDCK cells, as well as in positive control LPS-primed canine …
Small Molecule Antagonists Of The Urokinase (Upa): Urokinase Receptor (Upar) Interaction With High Reported Potencies Show Only Weak Effects In Cell-Based Competition Assays Employing The Native Upar Ligand, Melissa De Souza, Hayden Matthews, Jodi A. Lee, Marie Ranson, Michael J. Kelso
Small Molecule Antagonists Of The Urokinase (Upa): Urokinase Receptor (Upar) Interaction With High Reported Potencies Show Only Weak Effects In Cell-Based Competition Assays Employing The Native Upar Ligand, Melissa De Souza, Hayden Matthews, Jodi A. Lee, Marie Ranson, Michael J. Kelso
Illawarra Health and Medical Research Institute
Binding of the urokinase-type plasminogen activator (uPA) to its cell-surface-bound receptor uPAR and upregulation of the plasminogen activation system (PAS) correlates with increased metastasis and poor prognosis in several tumour types. Disruptors of the uPA:uPAR interaction represent promising anti-tumour/metastasis agents and several approaches have been explored for this purpose, including the use of small molecule antagonists. Two highly potent non-peptidic antagonists 1 and 2 (IC50 1 = 0.8 nM, IC50 2 = 33 nM) from the patent literature were reportedly identified using competition assays employing radiolabelled uPAR-binding uPA fragments and appeared as useful pharmacological tools for studying the PAS. Before …
Peroxisome Proliferator-Activated Receptor Alpha Target Genes, Maryam Rakhshandehroo, Bianca Knoch, Michael Muller, Sander Kersten
Peroxisome Proliferator-Activated Receptor Alpha Target Genes, Maryam Rakhshandehroo, Bianca Knoch, Michael Muller, Sander Kersten
Illawarra Health and Medical Research Institute
The peroxisome proliferator-activated receptor alpha (PPARα) is a ligand-activated transcription factor involved in the regulation of a variety of processes, ranging from inflammation and immunity to nutrientmetabolism and energy homeostasis. PPARα serves as amolecular target for hypolipidemic fibrates drugs which bind the receptor with high affinity. Furthermore, PPARα binds and is activated by numerous fatty acids and fatty acid-derived compounds. PPARα governs biological processes by altering the expression of a large number of target genes. Accordingly, the specific role of PPARα is directly related to the biological function of its target genes. Here, we present an overview of the involvement …