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 19 of 19 for “"GABA receptor"”.
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Molecular pharmacology of an insect GABA receptor
Cys-loop receptors are ligand-gated ion channels that are involved in fast synaptic neurotransmission in the central and peripheral nervous system. The Cys-loop receptor RDL (‘resistant to dieldrin’) is a GABA-gated chloride channel from Drosophila melanogaster and is a major target site for …
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Molecular characterization of GABA receptor subunits from the parasitic nematode Haemonchus contortus
… channel genes, Hcounc- 49B and C that encode two GABA-gated chloride channel subunits. Electrophysiological analysis shows that the Hco-UNC-49B subunit forms a functional homomeric channel in Xenopus laevis oocytes that produces a robust response to GABA and is highly sensitive to picrotoxin. In …
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Investigation of two Interacting Neurosteroid Sites on a GABA Receptor by Mutagenesis and Mathematical Modeling
<p>Given the utility of GABA receptor ligands as anthelminthics and insecticides, further study of invertebrate GABA receptor modulation promises to help identify new drugs to combat emerging resistance. The C. elegans GABA receptor, UNC-49, is modulated by the neurosteroids pregnenolone sulfate …
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Examination of intramolecular interactions between residues of the cys-loop GABA receptor Hco-UNC-49 from Haemonchus contortus
… unique parasitic nematode γ-aminobutyric acid (GABA) gated chloride channel that may prove to be a novel drug target. The objective of this thesis was to characterize intramolecular interactions of Hco-UNC-49B. Two sets of oppositely charged residues were chosen based on their proximity to each …
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Investigation into the role of binding loop E on the function of the nematode cys-loop GABA receptor.
… the LGCC gated by γ- aminobutyric acid (GABA) within H. contortus. To meet this objective, each amino acid residue in binding loop E was changed to a cysteine and analyzed via electrophysiology and the substituted cysteine accessibility method. It was found that of the 18 loop E mutants …
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The synthesis and pharmacology of gamma-aminobutyric acid receptor mimetics
Gamma-aminobutyric acid (GABA) has been shown to be an important inhibitory neurotransmitter in mammalian central nervous system (CNS). GABA receptors have been previously characterized in mammalian brain using 3H-GABA itself, a potent GABA agonist, 3H-muscimol, and the GABA antagonist, …
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Characterisation of a Novel GABA Signalling System in the Human Cerebral Vasculature
γ-aminobutyric acid (GABA) is the primary inhibitory neurotransmitter in the mammalian brain, underlying diverse functions from the maintenance of consciousness and the formation of memories to the regulation of the processes underlying brain development and circadian rhythms. While GABAergic …
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In-vitro analysis of microfilariae phenotypic responses induced by small molecules and dsRNA targeting receptor pathways
… as dsRNA molecules targeting genes involved in receptor pathways essential for nematode function. Utilizing the video analysis software called the Worminator, we quantified changes in movement upon exposure to agonists and antagonists acting on various receptors. Distinct responses were observed …
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Investigation into potential Dirofilaria immitis drug targets through rational anthelmintic synthesis and design
… and examine their activity on the anthelmintic receptor targets of interest, ACC-2 which is an acetylcholine-gated chloride channel unique to nematodes and the UNC-49 GABA receptor. In total, 22 compounds, 12 of which are novel, were synthesized, including imidazole-4-acetic acid like compounds, …
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A molecular characterization of agonists that bind to Hco-UNC-49, a GABA-gated chloride channel from Haemonchus contortus
… into the efficacy of a range of classical GABA receptor agonists on Hco-UNC-49 expressed in Xenopus oocytes. The results of our electrophysiological recordings indicate that there is a size requirement for full agonism of the Hco-UNC-49 binding site. Furthermore, a number of molecules that …
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Molecular characterization of the binding site of nematode GABA-A receptors
… in large part by nematocidal drugs that target receptors of the parasitic nervous system. Hco-UNC-49 is a nematode GABA receptor that has a relatively low overall sequence homology to mammalian GABA receptors but is very similar to the UNC-49 receptor found in the free living nematode …
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IMPACT OF PESTICIDES ON THE NEURAL STRUCTURE OF THE HONEY BEE, APIS MELLIFERA
Fipronil, a commonly used pesticide, is a GABA receptor antagonist that induces hyperexcitability in the central nervous system of insects. Its use is controversial because it is a suspected contributor to the global decline of non-target pollinator populations. Sublethal doses of fipronil reduce …
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Evaluation of Seizure Threshold as an Early Behavioral Marker of Disease Progression in the Mouse Model of Mucopolysaccharidosis IIIA
… chemiconvulsant drug, pentylenetetrazol (PTZ), a GABA receptor inhibitor. The acute intravenous infusion with PTZ did not show threshold differences between the diseased and normal mice. However, chronic administration of a subconvulsive dose of PTZ, resulted in a difference in seizure …
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Genetics of Obesity In Starr County, Texas Mexican Americans
… and low frequency variants, in two adjacent GABA receptor subunit genes, <em>GABRB2 </em>and <em>GABRA6, </em>including a nonsynonymous variant in <em>GABRA6</em>. Additional associations include an association with a composite measure of adiposity that encompasses degree of adiposity and …
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The synthesis and biochemical and pharmacological evaluation of gamma-aminobutyric acid antagonists
… is concemed with the examination of a number of GABA antagonists in two in vitro assay systems. A series of cage-structured compounds including bicyolic phosphate esters (2,6,7,-Trioxa-l-phosphabicyclo (2,2,2,) octan-l-oxides with suitable 4-substituents) have been shown to be potent a GABA …
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Role of gamma-aminobutyric acid (GABA) in hypothalamic nuclear development
… (ARC). The VMN and PVN have a unique pattern of GABA expression in elements surrounding the nuclei, with a void of GABA within the region of the developing nuclei. The ARC, on the other hand, has dense GABAergic immunoreactive elements throughout the nucleus. Because of the expression pattern of …
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Mechanism of anaesthetic activation, combination and antagonism
The type A γ-aminobutyric acid receptors (GABAAR) – pentameric ligand gated ion channels (pLGICs) – are the main mediators of fast inhibitory neurotransmission in the human brain. Malfunctions in these receptors are a common cause for neurological disorders such as anxiety, epilepsy, schizophrenia …
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Genome-scale identification of cellular pathways required for cell surface recognition
… organisms. Interactions mediated by cell surface receptors can be challenging to detect in biochemical assays, because they are often highly transient, and membrane-embedded receptors are difficult to solubilise in their native conformation. The biochemical features of low-affinity extracellular …
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Investigation of the role of ARFGEF3 in breast to brain metastasis
… and grow in the brain express neurotransmitter receptors and form synaptic connections with neurons and these pseudo-synapses contribute to tumour proliferation and survival. In our study, Whole exon sequencing data of 26 breast to brain metastatic (BBM) tumours revealed genomic abnormalities in …