Design and synthesis of polycyclic amine derivatives for sigma receptor activity

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dc.contributor.advisorMalan, S.F.
dc.contributor.advisorJoubert, J.
dc.contributor.authorStrydom, Natasha
dc.date.accessioned2014-11-18T11:51:55Z
dc.date.accessioned2024-05-08T12:56:17Z
dc.date.available2014-11-18T11:51:55Z
dc.date.available2024-05-08T12:56:17Z
dc.date.issued2013
dc.description>Magister Scientiae - MScen_US
dc.description.abstractNew 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).en_US
dc.identifier.urihttps://hdl.handle.net/10566/13176
dc.language.isoenen_US
dc.rights.holderUniversity of Western Capeen_US
dc.subjectPolycyclic amineen_US
dc.subjectPentacycloundecaneen_US
dc.subjectAmantadineen_US
dc.subjectHeterocyclic aminesen_US
dc.subjectSigma receptoren_US
dc.subjectNeurodegenerationen_US
dc.subjectDrug addictionen_US
dc.subjectBlood brain permeabilityen_US
dc.subjectDrug designen_US
dc.subjectLigand baseden_US
dc.subjectStructure activity relationshipen_US
dc.titleDesign and synthesis of polycyclic amine derivatives for sigma receptor activityen_US

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