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Synthesis and evaluation of fluorescently linked polycyclic cage derivatives for application in neurodegenerative disordersFourie, Locarno Lawrence January 2020 (has links)
Magister Pharmaceuticae - MPharm / Neurodegenerative diseases (ND) are chronic and progressive in nature, and
characterized by the gradual loss of neurons in various regions of the central
nervous system (CNS). ND include Alzheimer's disease (AD), Parkinson's disease
(PD), Huntington's disease (HD), multiple sclerosis (MS), amyotrophic lateral
sclerosis (ALS) and cerebral ischemia/reperfusion (CIR). They have various
progressive neurodegenerative pathologies that can result in several severe
functional impairments for patients, and ultimately lead to serious health-related
issues. According to more recent data, AD accounts for the most common cause of
dementia and is believed to contribute to approximately 60–70% of cases. AD is thus
seen as the most common form of dementia.
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Design and synthesis of polycyclic amine derivatives for sigma receptor activityStrydom, Natasha January 2013 (has links)
>Magister Scientiae - MSc / New therapeutic strategies are needed for a diverse array of poorly understood neurological impairments. These include neurodegenerative disorders such as Parkinson’s disease and Alzheimer’s disease, and the psychiatric disorders such as depression, anxiety and drug dependence. Popular neuropharmacotherapies
have focused on dopamine (DA), serotonin (5HT), γ-aminobutric acid (GABA) and glutamate systems (Jupp & Lawrence, 2010). However recent research points to the sigma receptor (σR) as a possible neuromodulatory system. Due to its multi-receptor action, the σR can trigger several significant biological pathways. This indicates its ideal potential as a drug target to effectively minimise drug dosage and potential side effects.
Currently there are a limited number of σR ligands available and few possess the selectivity to significantly show σR’s role in neurological processes. Polycyclic amines have shown notable sigma activity and provide an advantageous scaffold for drug design that can improve pharmacodynamic and pharmacokinetic properties (Banister et al., 2010; Geldenhuys et al., 2005). Aryl-heterocycle amine groups were also shown to improve σR activity (Piergentili et al., 2009).
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