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 15 of 15 for “"Positive allosteric modulator"”.
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Pharmacological and Pharmacokinetic Studies of a K<sub>Ca</sub>2.2 Positive Allosteric Modulator
… channel rescued by a K<sub>Ca</sub>2.2 positive modulator. A positive allosteric modulator of K<sub>Ca</sub>2.2/K<sub>Ca</sub>2.3 channels (compound <strong>2q</strong>) has been developed, and a method for quantitating it in mouse plasma has been validated using FDA guidelines. The …
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Role of Microglial α7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulator in Neuroinflammatory Pain Models in Mice
… We hypothesized that microglial α7 nAChRs positive allosteric modulation in the hippocampus will decrease neuroinflammatory pain at behavioral, cellular, biochemical, and molecular level. The primary objective of current study was to examine the role of an α7 nAChR positive allosteric …
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Testing the efficacy of LSN2463359, a metabotropic glutamate 5 receptor positive allosteric modulator, in animal models of schizophrenia
… of the metabotropic glutamate 5 receptor modulator LSN2463359, previously shown to act as an indirect agonist of the NMDA receptor, in two different animal models of schizophrenia. Our study found that when LSN2463359 was administered to rats given SDZ 220-581 (an NMDA antagonist) levels …
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Structural and molecular determinants of the sensitivity of alpha4beta2 nicotinic acetylcholine receptors to the allosteric ligand desformylflustrabromine
Allosteric modulation of neuronal nicotinic acetylcholine receptors (nAChRs) is considered to be one of the most promising approaches for therapeutics. By binding to a site of the receptor distinct from the neurotransmitter binding site, allosteric modulators alter the response of the receptors to …
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Design, Synthesis, and Pharmacological Characterization of Serotonin (5-HT) 5-HT2C Receptor (5-HT2CR) Positive Allosteric Modulators
… and pharmacologically evaluated as 5-HT2CR positive allosteric modulators (PAMs). Several analogues potentiated intracellular calcium release by 5-HT in h5-HT2CR-CHO cells. Several compounds exhibited a favorable overall pharmacokinetic profile and modulated 5-HT2CRassociated behaviors …
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Neonatal exposure to estradiol in female rats influences neuroactive steroid concentrations and behaviour in the adult rat
… to changes in the behavioural sensitivity to the positive allosteric modulator of the GABAA receptor, diazepam. These effects of estradiol suggest that it plays a major role in pharmacological regulation both of GABAergic transmission and of the abundance of endogenous modulators of such …
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The Emergence of Network Hyperexcitability and Functional Impairment in a Mouse Model of Alzheimer’s Disease
… novel GABAΑ-R α1-selective nanobody, acting as a positive allosteric modulator, was shown to decrease activity in WT networks but paradoxically exacerbate burst-driven hyperexcitability in AppNL-G-F networks in a dose-dependent manner. Perturbed excitation-inhibition balance, and consequent …
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PATHOLOGICAL IMPLICATIONS OF ANTI-GLUA3 ANTIBODIES IN FRONTOTEMPORAL DEMENTIA: FROM ANIMAL MODEL TO RESCUE STRATEGY
… levels in cerebrospinal fluid of FTD patients positive for anti-GluA3 hIgGs (anti-GluA3-Ab+) compared with negative ones. In addition, mice chronically treated with anti-GluA3 hIgGs exhibited behavioral disturbances that mostly reflected the deficits detected in anti-GluA3-Ab+ patients, such as …
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Role of group II metabotropic glutamate receptor subtype 2 (mGluR2) in appetitive and consummatory aspects of ethanol reinforcement
… agonist LY379268 (LY37) and selective mGluR2 positive allosteric modulator (PAM) BINA were used to determine the relative contribution of mGlu2 and mGlu3 receptors on EtOH seeking and consumption. Following characterization of the agonist and PAM on EtOH reinforcement, a microinjection study …
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Structural and molecular determinants of the sensitivity of alpha4beta2 nicotinic acetylcholine receptors to the allosteric ligand desformylflustrabromine
Allosteric modulation of neuronal nicotinic acetylcholine receptors (nAChRs) is considered to be one of the most promising approaches for therapeutics. By binding to a site of the receptor distinct from the neurotransmitter binding site allosteric modulators alter the response of the receptors to …
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Characterisation and pharmacological regulation of GLP-1-mediated glucose homeostasis
… glucose homeostasis through the action of positive allosteric modulator (PAM). Here, compound 249, which was identified previously as a small molecule GLP-1R PAM, was further pharmacologically validated using various signal transduction assaying techniques in recombinant cell lines. It was …
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Influence of a Nicotinic Treatment on Auditory Sensory Processing in Schizophrenia
… with prominent and intrusive experiences of positive (e.g., hallucinations) and negative symptoms (e.g., social withdrawal) in addition to widespread psychosocial, cognitive and sensory processing dysfunctions, which are generally experienced before the onset of the first psychotic episode. …
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Exploration of cognitive and neurochemical deficits in an animal model of schizophrenia. Investigation into sub-chronic PCP-induced cognitive deficits using behavioural, neurochemical and electrophysiological techniques; and use of receptor-selective agents to study the pharmacology of antipsychotics in female rats.
… often persist when other symptoms, particularly positive symptoms, may be improved with drug treatment. The non-competitive NMDA receptor antagonist, phencyclidine (PCP), is a psychomotor stimulant drug that has been shown to induce symptoms characteristic of schizophrenia in humans and animals. …
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Validation of an animal model of cognitive dysfunction associated with schizophrenia. Development and validation of the novel object recognition task using behavioural manipulations and psychotomimetic dosing regimens to induce cognitive deficits of relevance to schizophrenia in hooded-Lister rats.
… full agonist nicotine, and full agonist and positive allosteric modulator of the ¿7 nAChR (PNU-282987 and PNU120596 respectively) reversed the recognition memory deficit induced by sub-chronic PCP treatment in the NOR test. Isolation rearing of rats at weaning is an environmental stressor …
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SK Channel Modulators as Drug Candidates and Pharmacological Tools
… nervous system. In animal models, SK/IK channel positive modulators have been shown to be effective in reducing the symptoms of neurological diseases such as ataxia. Ataxia is a lethal neurological rare disease characterized by lack of balance and incoordination of muscle movements, often as a …