Open Access. Powered by Scholars. Published by Universities.®
Articles 1 - 5 of 5
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 …
Impact Of 27-Hydroxycholesterol On Amyloid-Beta Peptide Production And Atp-Binding Cassette Transporter Expression In Primary Human Neurons, Kim W Scott, S L Chan, A F Hill, G J Guillemin, B Garner
Impact Of 27-Hydroxycholesterol On Amyloid-Beta Peptide Production And Atp-Binding Cassette Transporter Expression In Primary Human Neurons, Kim W Scott, S L Chan, A F Hill, G J Guillemin, B Garner
Illawarra Health and Medical Research Institute
Cholesterol is an integral component of neuronal membranes and recent evidence has shown that it regulates amyloid-β protein precursor processing to form amyloid-β peptides, which are a major constituent of cerebral amyloid plaques associated with Alzheimer's disease. 27-Hydroxycholesterol (27OHC) is synthesized from cholesterol via sterol 27-hydroxylase (CYP27A1) in the brain and, unlike cholesterol, can cross into the brain through the blood brain barrier from the circulation. Previous studies point toward a potential role for 27OHC in the regulation of neuronal amyloid-β peptide generation, however, this has not been investigated in primary human neurons. Here we show that 27OHC significantly reduced …