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 573 for “"agonists"”.
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Novel Agonists and Antagonists of Platelet Receptors
Platelets are central for the primary haemostatis. The platelet has surface bound receptors that are vital for the platelet activation. One of these receptors, the purinergic ADP-activated G-protein coupled receptor (GPCR) P2Y12 is a key receptor for platelet activation, and thus for thrombus …
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Ligand Bias by the Endogenous Agonists of CCR7
… system. CCL19 and CCL21 are endogenous agonists for the chemokine receptor CCR7. They are known to be equipotent in promoting Gi/o mediated calcium mobilization, chemotaxis and inhibition of adenylyl cyclase activity. Here we test the hypothesis that these ligands are biased agonists …
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Design, synthesis and pharmacological evaluation of certain GABAB agonists
Ziel dieser Arbeit war die Synthese von (RS)-5-Amino-3-aryl(methyl)-pentansäure Hydrochloride, 3-Aminomethyl-5-chlor-benzolsäure Hydrochlorid und(RS)-4-Amino-3-(4´-ethynyl(jod)-phenyl)-butansäure Hydrochloride und die Testung der pharmakologischen Aktivität dieser Verbindungen. Die synthetisierten …
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Effects of beta-2 adrenoceptor agonists on the diaphragm
Contains fulltext : 146605.pdf (Publisher’s version ) (Open Access)
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Synthesis of Novel Glycolipid Agonists of the Protein CD1d
… synthesis of recently discovered natural agonists of iNKT cells from pathogenic origin, namely \(\alpha\)-galactosyl diacylglycerol (\(\alpha\)GalDAG).
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Soft [beta]-adrenoceptor agonists for topical use in psoriasis
… surface receptors are stimulated by β-adrenergic agonists, intracellular ATP is transformed into c-AMP, thus restoring the c~AMP/c~GMP levels. This thesis describes a series of β-adrenoceptor agonists for topical delivery based upon the soft-drug approach. Soft drugs are defined as biologically …
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Diverse Kappa Opioid Receptor Agonists: Relationships Between Signaling and Behavior
… drug target for addictive diseases. KOR agonists are of particular interest for the treatment of cocaine and other psychostimulant addictions, because there are currently no available medications for these diseases. Studies in humans and animals, however, have shown that activation of the …
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Functionally selective receptor signaling and endocytosis by dopamine D1 receptor agonists
… 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 essential for voluntary movement, cognition and reward processes. As …
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MOLECULAR FACTORS THAT INFLUENCE THE BINDING OF AGONISTS TO AMPA RECEPTORS
… also increase the affinity of receptors for agonists. Importantly, the efficacy of these drugs to increase synaptic responses and agonist binding exhibit a positive correlation. Indeed, we have found that the increase in agonist binding (Emax) induced by the prototypical ampakine CX546 is …
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EFFECTS OF SIGMA-1 RECEPTOR AGONISTS ON COMPULSIVE BEHAVIOR AND NEUROPLASTICITY
… 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 receptor …
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Investigating toll-like receptor agonists as an immunotherapeutic for metastatic osteosarcoma
… 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 disease has …
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Defining Novel Clusters of PPAR gamma Partial Agonists for Virtual Screening
… mellitus (T2D). Thiazolidinediones (TZDs) are agonists of PPARγ which have an insulin sensitizing effect, and are therefore used as a treatment for T2D. However, TZDs cause negative side effects in patients, such as weight gain, edema, and increased risk of bone fracture. Partial agonists could …
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Synthesis and evaluation of CYP27A1 inhibitors and NR0B2 agonists as anticancer immunomodulators
Submission published under a 24 month embargo labeled 'Closed Access', the embargo will last until 2026-08-01
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Identifying Potential Agonists Of TRPA1 Using A Heterologous Expression System And Transgenic Mice
… Of these stimuli, eight were potentially novel agonists of TRPA1. Using a fluorescent plate reader and the calcium-sensitive fluorescent dye FLUO-3AM, intracellular calcium levels of naive HEK and hTRPA1-HEK cells were monitored after exposure to a stimulus of interest. If a stimulus activated …
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Exploration of Toll-like Receptor 7 and 8 Agonists as Potential Vaccine Adjuvants
… as well as synthetic small molecules. TLR7/8 agonists hold promise as potential vaccine adjuvants, since they directly activate antigen-presenting cells and enhance T helper 1-driven immune responses. A general introduction to TLRs, with an emphasis on the role of TLR7/8 activation in innate …
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Studies in the synthesis and analysis of novel heterocyclic synthetic cannabinoid receptor agonists
… 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
… on EAE, I examined the role of various TLR agonists in the development of autoimmunity using direct immunization and adoptive transfer of encephalitogenic T cells. Mice developed EAE following immunization with myelin antigen emulsified in IFA with various PAMPs, indicating that various …
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Combination of STING and TLR 7/8 agonists as vaccine adjuvants for cancer immunotherapy
… immunoadjuvants such as toll-like receptor (TLR) agonists, exosomes, and metallic immunoadjuvants have been studied for their immunological effects. However, the clinical use of immunoadjuvants is limited by transient responses and various side-effects. Therefore, there is a need for exploring …
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The Effects of Cholinergic Agonists and Antagonists on Self-Stimulation Behavior in The Rat
Made available in DSpace on 2014-12-10T21:07:06Z (GMT). No. of bitstreams: 1 7114890.pdf: 4997567 bytes, checksum: 519c991c5c0525840a60e8f548f01765 (MD5) Previous issue date: 1970
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INTRACRANIAL INFUSIONS OF NEUROTENSIN AGONISTS PRODUCE AN ANXIOLYTIC PROFILE IN A RAT ULTRASONIC VOCALIZATION MODEL
… that neurotensin type 1 and type 2 receptor agonists influence animal models of psychological disorders and pain regulation, respectively. It has already been shown that the systemic administration of the selective neurotensin type 1 receptor agonist PD149163 can attenuate the number of …
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