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 10 of 10 for “"partial agonism"”.
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ALPHA4BETA2 NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS: FROM SUBTYPE SELECTIVE TO STOICHIOMETRIC ISOPHORM SELECTIVE PARTIAL AGONISM.
… and Ser108àAla mutants using the most promising partial agonists synthesized previously. The second goal was the synthesis and pharmacological evaluation of the naked and hydroxy/methoxy decorated benzofuran-based compound in order to study the implications of the flexibility reduction, …
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Agonist-Induced Conformational Changes In The Nmda Receptor
… of the receptor and the mechanism controlling partial agonism. Past studies utilizing static structural snapshots of the receptor or isolated domains of the receptor have provided insufficient insights to fully understand these issues. Herein, I have conducted Förster Resonance Energy Transfer …
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Evaluation of new succinimide-based small molecules as alphavbeta3 integrin antagonists: from design to preliminary biological testing
… designed as antagonists based on RGD have shown partial agonism. This limit may be overpassed by switching from RGD to isoDGR motif. Here, some isoDGR analogues prodrugs have been designed and synthesised, by a multi-step route to obtain the different fragments (isoAsp, Gly and Arg) subsequently …
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Fret-Based Investigations of The Structure-Function Relationships In The Nmda Receptor
… that gap. We have examined the question of partial agonism of the NMDA receptor, noting a mechanism of a dynamically graded cleft closure. We have pushed the bounds of the temporal resolution of such methods and been able to resolve fast dynamics of the ligand-binding domain, noting the …
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Cognitive dysfunction and schizophrenia : Modelling attentional impairment with psychotomimetics. Investigating attentional impairment and structural brain abnormalities following phencyclidine administration: Enhancing translatability between preclinical and clinical tests of attention utilising the modified 5-choice task in rats - the 5-Choice Continuous Performance Test.
… was investigated. It was revealed that D1 partial agonism improved attentional performance in a baseline-dependent manner. Following successful acquisition of the task, it was shown that repeated PCP treatment induced cognitive disruption that was cognitive-specific, and not confounded by …
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EFFECT OF COMBINATION OF THE MAMMALIAN LIGNAN, ENTEROLACTONE, WITH TYROSINE KINASE INHIBITORS ON MARKERS OF HEPATIC FIBROSIS
… assays, provided evidence of potential PPARγ partial agonism by gefitinib and ENL. Evaluation of the expression changes of several fibrotic markers (e.g., collagen I, -SMA, MMP2/MMP9, and TIMP-1,) using human hepatic stellate cells (HSC), LX-2 cells, at both mRNA and protein level by …
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Investigating the molecular signatures of β1-adrenergic receptor activation
… interaction with G-proteins, which may underpin partial agonism. It was also observed that ligand binding affects the dynamics and rigidity of the receptor, with a full agonist bound receptor exhibiting extensive µs to ms timescale dynamics, compared to a more rigid nanobody bound state. The …
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The development of small molecule inhibitors for fibrosis drug discovery
… RGD integrin (αIIbβ3) have been shown to cause partial agonism, leading to the opposite pharmacological effect.The challenge of obtaining oral activity and synthetic tractability with RGD-mimetic molecules, along with the issues relating to pharmacology, has left integrintherapeutics in need of …
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Modelling Β2Ar Regulation
<p>The β2 adrenergic receptor (β2AR) regulates smooth muscle relaxation in the vasculature and airways. Long- and Short-acting β-agonists (LABAs/SABAs) are widely used in treatment of chronic obstructive pulmonary disorder (COPD) and asthma. Despite their widespread clinical use we do not …
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Modulation of The Receptor Gating Mechanism and Allosteric Communication In Ionotropic Glutamate Receptors
<p>Ionotropic glutamate receptors (iGluRs) found in mammalian brain are primarily known to mediate excitatory synaptic transmission crucial for learning and memory formation. The family of iGluRs consists of AMPA receptors, NMDA receptors and kainate receptors with each member having distinct …