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 99 for “"receptor antagonists"”.
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Directed Evolution of T Cell Receptor Antagonists
In Chapter 4, further engineering of TCR stability mutants to produce increased affinity binding for SAg is described. An optimized TCR fragment (containing nine mutations) was isolated after mutagenesis and selection, and was found to have approximately 1000-fold improved affinity for SAg. A …
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Configurationally restricted bis-tetraazamacrocyclic complexes: chemokine receptor antagonists
The chemokine receptor CXCR4 is a trans-membrane protein which has been implicated in many physiological and pathological processes including cancer, rheumatoid arthritis and most significantly HIV replication. CXCR4 plays a vital role in embryonic development but is not essential at the …
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Engineering Soluble, High Affinity Receptor Antagonists for Bacterial Exotoxins
Chapter four describes the engineering of murine Vbeta8.2 for picomolar affinity to staphylococcal enterotoxin B (SEB). As the known contact regions had already been heavily mutagenized, additional engineering of the Vbeta was performed through extension of the CDR1 loop. Soluble forms of the …
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Effects of Single and Dual Orexin Receptor Antagonists on Trigeminal Nociception
… membrane excitability. There are two orexin receptors that differentially bind orexin peptides. Single and dual orexin receptor antagonists have been synthesized to selectively block the activity of these orexinergic receptors. I hypothesized that a single orexin receptor antagonist blocking …
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Effects of selective neurotensin receptor antagonists on responding for brain stimulation reward
… of systemic administration of two selective NT antagonists, SR-48692 and SR-142948a, on responding for medial mesencephalic electrical stimulation. The curve-shift method adapted to operant responding for brain stimulation reward was used to assess reward and performance changes following …
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Design, Synthesis and Pharmacological Characterization of Novel Calcitonin Gene-Related Peptide Receptor Antagonists
… the activation of signal transduction by CGRP receptors. Truncation of the N-terminal ring, resulting in CGRP(8-37), leads to loss of agonist activity while retaining the ability to bind to the receptor and CGRP(8-37) became the primary research tool used to investigate CGRP receptors. The …
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Determination of Dissociation Constants for GABAA Receptor Antagonists using Spontaneously Active Neuronal Networks in vitro
… the dissociation constant (KB) of three GABAA antagonists. Neuronal networks were treated with fixed concentrations of GABAA antagonists and titrated with muscimol, a GABAA receptor agonist. Muscimol decreased spike activity in a concentration dependent manner with full efficacy (100% spike …
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Effects of NMDA Receptor Antagonists on the Differential-Reinforcement-of-Low-Rate 72 Second (DRL 72) Responding in Rats
<p>The noncompetitive NMDA receptor antagonist dextromethorphan and its metabolite dextrorphan have widespread effects on the central nervous system. Dextromethorphan alone and with quinidine (a CYP-450 2D6 inhibitor) have been shown to produce antidepressant effects in preclinical and clinical …
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Design and synthesis of 3-[N-(cyclopropylmethyl) amino]-7-(methoxy or hydroxy)-2, 2-dimethyl-1-tetralone analogs as potential opioid receptor antagonists
… were synthesized as potential opioid antagonists. Each proposed target compound was based on a 3-(mono- or dialkylamino )-7 -(hydroxy or methoxy)-2, 2-dimethyl-1-tetralone parent structure. Three synthetic schemes were developed utilizing the common intermediate, ethyl3-benzylamino-2, …
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Ionic dysregulation in white matter damage
… attention was paid to consequences of glutamate receptor activity. Using the oxygen glucose deprivation model of ischaemia, in the mouse brain slice, it was found that ischaemia-induced potassium release is greater in cortical grey than in corpus callosum white matter. This distinction is …
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Pre-clinical Targets for Ischemic Brain Injury
… resulting in demyelination. Glutamate receptor antagonists have been trialled in stroke patients but fall short due to adverse side effects from high dose preparations. Stroke is largely a disease of ageing, and may occur in the presence of other diseases, such as primary age related …
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Pharmacological and Non-pharmacological Prevention of Fentanyl-Induced Cough : A meta-analysis
… (CI) 0.21 – 0.39], N-methyl-D-aspartate (NMDA) receptor antagonists [OR = 0.09, 95% CI 0.02 – 0.42], propofol [OR = 0.07, 95% CI 0.01 – 0.36], α2 agonists [OR = 0.32, 95% CI 0.21 – 0.48], β2 agonists [OR = 0.10, 95% CI 0.03 – 0.30], fentanyl priming [OR = 0.33, 95% CI 0.19 – 0.56], and slow …
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THE EFFECT OF NALTREXONE ON NICOTINE-INDUCED CONDITIONED PLACE PREFERENCE IN RATS
… One strategy involves the use of opioid receptor antagonists. For instance, naloxone has been shown to reduce place preference for nicotine in rats, and other experimental opioid antagonists have also been shown to affect place preference for nicotine. The present study sought to extend …
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Characterisation of PACAP-responsive receptor pharmacology and expression in cell models and the spinal cord
… three different class B G protein-coupled receptors; the PAC1, VPAC1 and VPAC2 receptors. To add further complexity, the PAC1 receptor may be alternatively spliced, generating variants that can differ in their agonist or signalling profiles. The PACAP peptide family show promise for the …
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Cholinergic Regulation of Circadian Rhythms in the SCN: Characterization of Signaling Mechanisms and the Role of Intracellular Calcium in the Directionality of Clock Resetting
… phase advance, while InsP3 , but not ryanodine, receptor antagonists block it. In contrast, selective activation of CICR with ryanodine results in glutamate-like delay. Ca 2+ imaging using multiphoton microscopy revealed signal-specific differences in Ca2+ transients. Cholinergic-stimulated Ca2+ …
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Site-directed mutagenesis and molecular modeling studies of h5-HT7(a) receptor reveal important residues for binding and activation
… on knockout animals and using selective 5-HT7 receptor antagonists have provided strong support that the G-protein-coupled 5-HT7 receptor plays a role in the onset of depression. To better understand the process of ligand binding to and activation of the 5-HT7 receptor and which essential …
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DESIGN, SYNTHESES, AND BIOLOGICAL EVALUATION OF 14-N-SUBSTITUTED NALTREXONE DERIVATIVES AS OPIOID RECEPTOR LIGANDS
… their effects through activating the mu opioid receptor. Studies involving the mu opioid receptor knockout mice showed that the interaction with the mu opioid receptor is also responsible for many notorious side effects associated with these drugs including dependence and addiction. Therefore, …
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Regional and temporal differential regulation of the N-methyl-D-aspartate receptor by phencyclidine during development
… phencyclidine (PCP)-induced changes in the NMDA receptor subunit composition and the relationship of these changes to the deficits in pre-pulse inhibition (PPI) caused by PCP treatment. Postnatal rats were treated with atypical or typical antipsychotics or selective dopamine or serotonin receptor …
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Design and Synthesis of CB1 Receptor Ligands and Synthesis of Amphibian Alkaloids
… at the development of novel CB1 cannabinoid receptor antagonists that may have clinical applications for the treatment of cannabinoid and psychostimulant addiction. In this study, we designed, synthesized, and established the CB1 affinity for the 1,5-diaryl-1,2,3- triazole esters, a series of …
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