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 96 for “"receptor agonists"”.
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Diverse Kappa Opioid Receptor Agonists: Relationships Between Signaling and Behavior
… system, comprised mainly of the three opioid receptors (kappa, mu and delta) and their endogenous neuropeptide ligands (dynorphin, endorphin and enkephalin, respectively), mediates mood and reward. Activation of the mu opioid receptor is associated with positive reward and euphoria, while …
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Functionally selective receptor signaling and endocytosis by dopamine D1 receptor agonists
The dopamine D1 receptor (D1R) is a G protein-coupled receptor that signals through Gs and Golf G proteins. D1R agonists increase cAMP production and recruit β-arrestin to the plasma membrane, which may lead to receptor desensitization and/or induce D1R endocytosis. In addition, the D1R is …
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EFFECTS OF SIGMA-1 RECEPTOR AGONISTS ON COMPULSIVE BEHAVIOR AND NEUROPLASTICITY
… (mTOR). Preclinical studies suggest that sigma-1 receptor agonists produce antidepressant-like drug effects and affect the mTOR pathway. Other mechanisms include serotonin neurotransmission and N-methyl-D-aspartate (NMDA) receptors. This study evaluated drugs acting as sigma-1 agonists, NMDA …
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Investigating toll-like receptor agonists as an immunotherapeutic for metastatic osteosarcoma
… to determine the plausibility of toll-like receptor agonists as an immunotherapeutic for canine osteosarcoma. From a comparative and translational perspective, the long-term goals of this research include not only the treatment of canine osteosarcoma, but also human osteosarcoma, as this …
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Studies in the synthesis and analysis of novel heterocyclic synthetic cannabinoid receptor agonists
Over the past decade, synthetic cannabinoid receptor agonists (SCRA) have come to represent a diverse category of new psychoactive substance (NPS). However, from a chemical perspective, little is known about the clandestine chemical syntheses of SCRAs. To contextualise the latter paucity of …
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Multiple Toll-Like Receptor Agonists Act as Potent Adjuvants in the Induction of Autoimmunity
… molecular patterns (PAMPs) activating Toll-like receptors (TLRs) on host cells. I investigated the role that PAMPs play in Experimental Autoimmune Encephalomyelitis (EAE), an animal model of MS. Both genetic and environmental influences contribute to the pathogenesis of MS. I used various PAMPs …
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The Identification and Pharmacological Characterisation of Novel Apelin Receptor Agonists In Vitro and In Vivo
… consisting of the G protein coupled apelin receptor and two endogenous peptide ligands, apelin and elabela. It is implicated as a potential therapeutic for a number of diseases; however, the endogenous peptides are limited by half-life and bioavailability. This study aims to identify and …
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The Influence of Alpha7 and Alpha4 Beta2 Nicotinic Receptor Agonists on Feature Based Reversal Learning in Macaque Monkeys
Selective and non-selective nicotinic agonists are associated with improvements in higher order cognitive functions. However, the effects of selectively activating nicotinic sub-receptors on attention and learning are not well understood. In my project, I used two agonists selective for alpha7 (7) …
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Pharmacological characterisation of selective Y4 and dual Y2/Y4 receptor agonists: novel targets for putative anti-obesity therapies
… current (Isc) recorded. In addition, receptor specificity of the most promising agonists was dissected using Y1 and Y2 antagonists. Furthermore, an assessment of Y4 receptor desensitisation was made by application of a subsequent addition of the native hormone, hPP. With a lysine …
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EFFECTS OF MU OPIOID RECEPTOR AGONISTS ON INTRACRANIAL SELF-STIMULATION IN THE ABSENCE AND PRESENCE OF “PAIN” IN RATS
Pain is a significant health problem. Mu opioid receptor agonists are used clinically as analgesics, but their use is constrained by high abuse liability. Intracranial self-stimulation (ICSS) is a preclinical behavioral procedure that has been used to assess abuse potential of opioids, and …
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Progress Towards Development Of Multifunctional, Dopamine D2/d3 Receptor Agonists As Symptomatic And Disease-Modifying Therapeutic Agents For Parkinson's Disease
… template to design novel, D3-preferring agonists, with a range of selectivity for D3 receptor, while also incorporating antioxidant moieties to provide antioxidant capacity to the molecule. In this dissertation, we investigate the potential of our D3-preferring agonists to not only …
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Evaluating the Mechanisms of 2-Hydroxypropyl-β-Cyclodextrin and Liver X Receptor Agonists as Potential Therapies for Niemann-Pick Type C Disease
… clarifies the molecular mechanism(s) of LXR agonists and cyclodextrins in Niemann-Pick Type C disease progression, which could lead to the development of more effective therapies for patients.
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Involvement of Cytochrome P450 1A in the toxicity of aryl hydrocarbon receptor agonists : alteration arachidonic acid metabolism and production of reactive oxygen species
… P4501A-dependent mechanisms of aryl hydrocarbon receptor (AhR) agonist toxicity were examined in the marine teleost scup (Stenotomus chrysops), alteration of arachidonic acid (AA) metabolism and production of reactive oxygen species (ROS). In scup hepatic microsomes, cytochrome P450s including …
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Understanding Patient Perceptions and Behavioral Intentions Toward GLP-1 Receptor Agonists for Weight Management in the United States: A Health Belief Model Approach
<p>Background: Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) are increasingly used for weight management in the United States; however, limited evidence exists regarding the perceptual and behavioral factors influencing medication adherence among adult users. Prior research has largely …
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Involvement of cytochrome P450 1A in the toxicity of aryl hydrocarbon receptor agonists : alteration of arachidonic and acid metabolism and production of reactive oxygen species
… P4501A-dependent mechanisms of aryl hydrocarbon receptor (AhR) agonist toxicity were examined in the marine teleost scup (Stenotomus chrysops), alteration of arachidonic acid (AA) metabolism and production of reactive oxygen species (ROS). In scup hepatic microsomes, cytochrome P450s including …
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The effect of glucagon-like peptide-1 (GLP-1) receptor agonists on cell viability, ADAM10 maturation and the proteolysis of ADAM10 substrates in SH-SY5Y cells
Arguably the causative agent of Alzheimer's disease (AD), amyloid beta (Aβ)- peptides, are generated by sequential proteolysis of the amyloid precursor protein (APP) by β- and γ-secretase activities. Alternatively, APP can be processed nonamyloidogenically by an α-secretase activity that cleaves …
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Cardiovascular Effects of GLP-1 and Glucagon Dual Receptor Agonism in Humans
… IV inhibitors, glucagon like peptide-1 (GLP-1) receptor agonists and selective sodium-glucose transporter-2 inhibitors (SGLT2i). These medications have transformed treatment pathways and prognosis for individuals with T2DM as well as obesity (GLP-1 receptor agonists), heart failure (SGLT2i) and …
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Role of the dorsomedial and ventrolateral medulla in the regulation of pain sensitivity in the endotoxemic organism
… Micro-injections of glutamate or vanilloid receptor agonists in toxic concentrations into the nucleus tractus solitarii (NTS) and the caudal ventrolateral medulla (CVLM) lead to the similar effect. Both types of intervention – vagotomy, and central microinjections – were followed by …
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Characterisation of a Novel GABA Signalling System in the Human Cerebral Vasculature
… and in the human peripheral vasculature, but the receptor systems and cellular machinery underlying this regulation have not been characterised. And as yet, there have been no attempts to confirm the existence of this putative vascular GABA signalling system in the human brain. In this thesis, we …
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