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 24 for “"Sigma 1"”.
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EFFECTS OF SIGMA-1 RECEPTOR AGONISTS ON COMPULSIVE BEHAVIOR AND NEUROPLASTICITY
… (mTOR). Preclinical 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, …
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Progettazione e sintesi di nuovi ligandi sigma-1 bifunzionali con attività antiossidante
… stato suggerito il coinvolgimento del recettore sigma-1 nei meccanismi che mediano la neuroprotezione. Questa proteina è localizzata a livello della Mitochondrial Associated Membranes (MAM), dove modula il flusso di ioni Ca2+ dal reticolo endoplasmatico (ER) ai mitocondri, agendo da chaperone …
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Involvement of the Sigma-1 Receptor in Neuronal Cell Death and Alzheimer's Disease
Dysfunction in the Sigma-1 receptor (Sig-1R) is implicated in many neurodegenerative diseases such as Alzheimer’s Disease (AD). Recently, agonists of the Sig-1R have been found to be neuroprotective in AD and provide significant improvements in symptoms. The hallmarks of AD are aggregation of …
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Pharmacophore derivation using discotech and comparison of semi-emperical, AB initio and density functional CoMFA studies for sigma 1 and sigma 2 receptor-ligands
… of pharmacophore and CoMFA models for sigma receptor ligands. CoMFA studies were performed for 48 bioactive sigma 1 receptorligands using [H^3 ](+) pentazocine as the radioligand, for 30 PCP derivatives for sigma 1 receptor-ligands using [^3H](+)SK-F 10047 as the radioligand and for 24 …
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PROGETTAZIONE E SINTESI DI LIGANDI IBRIDI SIGMA-NO LIGHT-ACTIVATED A POTENZIALE ATTIVITA ANTIPROLIFERATIVA. NIH 10495 E DERIVATI: MODULAZIONE DELL ATTIVITA OPPIOIDE, SIGMA-1 ED HDAC NEL DOLORE NEUROPATICO.
… la progettazione e sintesi di ligandi ibridi NO/sigma attivati dalla luce a potenziale attività antitumorale, sfruttando l'overespressione dei recettori sigma in molte linee cellulari tumorali umane. Dato il crescente interesse per i ligandi sigma come potenziali agenti chemioterapici e sulla …
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Molecular modeling of sigma 1 and sigma 2 receptor ligands: pharmacophore development and comparison using discotech and bioactivity prediction comparison of ab initio and density functional comfa studies for spiro and other receptor ligands
… by researchers in medicine. Information about sigma receptors in particular can be gained by studying the ligands associated with each type, sigma 1 or sigma 2. Sigma 1 receptor ligands consist of drug candidates that often have psychiatric and neurological applications; sigma 2 receptor …
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role of pentazocine in an in vitro model of hypoxia/reoxygenation
… toxic and protective brain innate immunity. Sigma-1 receptor is expressed in both neurons and glia is a unique class of intracellular proteins and is involved in neurodegeneration. Our aim was to evaluate the biological effects of sigma-1 selective ligands, and bifunctional sigma-1 selective …
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Effects of Dextromethorphan on Neurite Outgrowth and Marble Burying Behavior
… acting on glutamate, NMDA receptors, and sigma-1, instead of serotonin, may be effective in treating OCD. One drug in particular, dextromethorphan (DM), provides antidepressant-like effects by possibly inhibiting glutamate and activating sigma-1 receptors. Common preclinical approaches for …
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Expression of sigma receptors in human cancer cell lines and effects of novel sigma-2 ligands on their proliferation
Sigma receptors originally thought to be an opioid receptor is now categorized as a distinct class of receptor. There are two main subtypes, the sigma-1 receptor and an uncharacterised binding site, named the sigma-2 binding site. The presence of the sigma-2 binding site shows high correlation with …
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Progettazione e sintesi di ligandi sigma selettivi
ABSTRACT Ligandi selettivi per recettori sigma-1 e sigma-2, possono essere farmaci potenzialmente utili per il trattamento di diverse condizioni patologiche, quali disturbi psichiatrici, abuso di cocaina, memoria e disturbi di apprendimento, discinesia e reazioni distoniche indotte da farmaci …
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Design, Synthesis, Biological Evaluation and Metabolic Stability Studies of Sigma Receptor Ligands
Sigma receptors represent a unique family of proteins that includes two subtypes: sigma-1 and sigma-2. Sigma-1 receptors have been implicated in the behavioral and motivational effects of psychostimulants as well as in the pathophysiology of depression and Alzheimer's disease. Sigma-2 receptors are …
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Metabolism And Pharmacokinetics In The Development Of New Therapeutics For Cocaine And Opioid Abuse
… the development of new pharmacotherapies, CM304 (sigma-1 receptor antagonist), mitragynine and 7-hydroxymitragynine (μ-opioid receptor agonists), for the treatment of drug abuse. The affinity of cocaine to sigma-1 receptors render the hypothesis that targeting sigma-1 receptors using antagonists …
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Rewriting Products of Group Elements
… if there is a nontrivial permutation $\sigma$ in Sym(n) such that ${\rm x\sb1\dots x\sb{n} = x\sb{\sigma (1)}\dots x\sb{\sigma (n)}}.$ A subset $\{ {\rm x\sb1,\dots, x\sb{n}}\}$ of n elements of G is said to be rewriteable if there exist distinct permutations $\sigma$ and $\tau$ in …
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Pharmacokinetic Evaluation of a Novel Compound, Sn79, a Putative Sigma-2 Receptor Antagonist, By Intravenous and Oral Administration in Rats
… and addiction. The affinity of cocaine to sigma receptors (sigma-1 and sigma-2) rendered the hypothesis that blocking sigma receptors could be a possible mechanism to attenuate cocaine-induced toxicity and addiction. In this view, SN79, a synthetic compound with selectivity to both sigma-1 …
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Design, synthesis, and biological evaluation of sigma receptors (σRS) ligands as potential pharmacotherapy for cancer and drug addiction
Sigma receptors are a well-defined unique class of receptors and are highly expressed in the central nervous system and also widely distributed in peripheral organs and tissues. There are two subtypes of sigma receptors: sigma-1 and sigma-2. These receptors are thought to be associated with …
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Second and Third Order Systems of Integrable Equations of the Davey-Stewartson Type
… z}{-1}v\sb{z}-v\sb{z}$$where $z=x+\sigma y,\ \bar z=x-\sigma y$ (when $\sigma=1$ this applies to the case I and when $\sigma=i$ to case II) maps a solution of the mod-NVN equation to a solution of NVN.
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Polytopes, generating functions, and new statistics related to descents and inversions in permutations
… the alternating descent set of a permutation [sigma] = [sigma] 1 [sigma] 2 an defined as the set of indices i such that either i is odd and ai > ui+l, or i is even and au < au+l. We show that this statistic is equidistributed with the 3-descent set statistic on permutations [sigma] = [sigma] 1 …
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Physical symmetry enhanced neural networks
… efficient parametrization method that requires [sigma] (1) complexity per parameter. Our unitary RNN model has shown optimal long-term memory ability. Next, we combine the above model with a gated mechanism. This model outperform popular recurrent neural networks like long short-term memory …
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Studies on Macrophage Migration in Pathological Contexts
… an extracellular matrix. The well-characterised Sigma-1 Receptor chaperone, previously implicated in BDNF function, was shown to be an important overall regulator of macrophage invasion, and to be potentially implicated in BDNF suppression of ATP-induced invasion. BDNF may thus have a …
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From Forest Floors to Pharmacology: Elucidating Millipede Defensive Alkaloids for Drug Discovery
… that a subset of the alkaloids potently binds to sigma-1 receptor (ischnocybine A: Ki 14 nM), while others bind to sigma-2 (homo-hydrogosodesmine hydrate: Ki 260 nM). Furthermore, ecology studies revealed that the alkaloid production is conserved over large geographical regions, accumulated as the …
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