Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 34 for “"radioligand binding"”.
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Characterization of TSPO expression and radioligand-binding in the central nervous system and peripheral blood in neuroinflammatory disease
… the comparison of TSPO expression and PET radioligand signal in inflammatory conditions has been limited by the lack of suitable unfixed pathological samples for concurrent measurement of protein expression and radioligand-binding. In this thesis, I seek to characterize patterns of TSPO …
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Chiral alkaloid derivatives: Synthesis and medicinal chemistry applications
… opioid species generated were analysed for their binding affinity to the mu opioid receptor through radioligand binding techniques. Binding affinities of a variety of the opioid species to a selection of metals were also assessed by metal picrate extraction studies.
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5-HT1A receptor expression : Studies in postmortem tissue and characterisation of a model system.
… mRNA levels were quantified using real-time PCR. Radioligand binding was used to determine B[max] and Kd quantifying 5-HT[1A] receptor density. The SHSY-5Y neuroblastoma cell line is a well characterised cell line model used in neurotransmitter studies when differentiated. The 5-HT[1A] receptor …
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Optimisation of the Investigation of Antibody-Mediated Dysglycaemia
… diagnosed with IAS. IAs were measured using radioligand-binding assay and enzyme-linked immunosorbent assay (ELISA). Method comparison showed results to differ in rank order and relative magnitude. For one patient whose screening IA result was not grossly elevated using either IA assay …
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Molecular Characterization of the Opioid Receptors: Design, Development, and Preclinical Evaluation of Salvinorin A-Based Molecular Probes.
… models include: opioid receptor competitive radioligand binding affinity and functional [35S]GTP[γS] binding activity assays; while our in vivo models include: antinociceptive, antidepressant, and anxiolytic related assays. This resulted in three analogues exhibiting EC50 sub-200 nM …
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Design and synthesis of new potential anticancer agents and high-selective A2B antagonists
… were synthesized. Some of them were tested in a radioligand binding assay to evaluate the affinity and selectivity toward A2BR subtype, further confirming the high potential of these compounds as A2B antagonists.
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Aging and Sympathetic Neurotransmission in Two Strains of Rats that Differ in Longevity and Immune Profiles
… using HPLC, fluorescence histochemistry, β-AR radioligand binding, and enzyme-linked immunoassay (EIA), respectively. We evaluated β-AR expression by β-AR radioligand binding assay. Rilmenidine reduced circulating NE without a change in epinephrine (EPI), and reduced SNA as assessed by reduced …
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Expression of sigma receptors in human cancer cell lines and effects of novel sigma-2 ligands on their proliferation
… the sigma-1 receptor and an uncharacterised binding site, named the sigma-2 binding site. The presence of the sigma-2 binding site shows high correlation with proliferation of cells and is associated with cancer. I have categorized sigma-1 and sigma-2 binding sites in 11 human tumour cell …
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A structure-function analysis of the marine toxin neodysiherbaine and its synthetic analogs on kainate receptors
… pharmacological profile at kainate receptors. In radioligand binding assays, 2,4-epi-neoDH showed micromolar binding affinity to GluR5(Q)-2a and GluR6a subunits. Electrophysiology recordings revealed it acted as an antagonist at these receptors, without detectable activity at AMPA receptors. This …
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Fungi-derived natural products with binding affinities for human opioid or cannabinoid receptors
… which act on opioid or cannabinoid receptors. Radioligand binding assays for opioid and cannabinoid receptors have been a useful tool for the discovery of novel agents. With the use of this assay, four fungi species were selected and subjected to bioassay-guided fractionation affording a total …
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The synthesis and pharmacology of gamma-aminobutyric acid receptor mimetics
… at the GABA-benzodiazepine receptor complex. The binding of 3H-Isoguvacine to frozen-thawed, rat brain synaptosomal membranes has been investigated and found to be saturable, specific and stereospecific. The pharmacology of this 3H-Isoguvacine binding site was seen to be consistent with an …
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Engineering the angiotensin II type 1 receptor for structural studies
… cells and mammalian expression in HEK293 cells. Radioligand binding assays showed that only the mammalian system produced sufficient quantities of active AT1R for structural studies. Expression in the mammalian system was further optimised to approximately 6 mg/L. An AT1R-GFP fusion was created …
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EFFECTS OF CHRONIC METHYLPHENIDATE ON DOPAMINE/SEROTONIN INTERACTIONS IN THE MESOLIMBIC DOPAMINE SYSTEM OF THE MOUSE
… single and dual probe in vivo microdialysis, radioligand binding, and behavioral tests for depressive like behaviors to examine the effects of chronic MPH. Our studies showed that chronic MPH alters DA/5-HT system interactions in the mesolimbic DA system. The alterations are such that …
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Moderate Ethanol Consumption by the Pregnant Guinea Pig Increases Ethanol Preference in Offspring
… for the measurement of nAChR population by radioligand binding. Moderate maternal consumption of the aqueous ethanol produced growth restriction in postnatal offspring of both sexes, and increased spontaneous locomotor activity in male offspring only. These postnatal outcomes are similar to …
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Molecular Regulation of Opioid Receptor Signaling
… which are implicated in MOR desensitization; radioligand binding studies demonstrating that norBNI does not change the drug binding site of KOR in vivo; and development of lentiviral vectors expressing KOR which were used to show that KOR expression in the dorsal raphe is sufficient for …
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DESIGN, SYNTHESES, AND BIOLOGICAL EVALUATION OF 14-N-SUBSTITUTED NALTREXONE DERIVATIVES AS OPIOID RECEPTOR LIGANDS
… derivatives were determined in a competitive radioligand binding assay. Interestingly, the 14-N-substituted naltrexone derivatives did not maintain the high selectivity of the 14-O-substituted series. It was hypothesized that the conformational constraint introduced by the amide linker was …
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Searching for structural determinants of agonist selectivity in nicotinic acetylcholine receptors
… of the highly conserved nature of the agonist binding site in the nAChR family. This thesis focuses on identifying elements in nAChR subtypes to aid the design of novel smoking cessation drugs. Functional and radioligand binding assays showed that novel C(10) cytisine (Cyt) derivatives maintain …
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Computational Ligand-Based CNS Therapeutic Design: The Search for Novel-Scaffold Norepinephrine Transporter Inhibitors
… is unclear as to which of two MAT protein ligand binding sites these drugs bind, hindering knowledge of the specific binding modes of MAT ligands. In this study an in silico pharmacophore model was created using a ligand-based method aimed at drug screening for the ability to specifically inhibit …
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